A specific category of drugs that prevent sleepiness by specifically targeting sleep-mechanisms in the brain. They are used to treat DISORDERS OF EXCESSIVE SOMNOLENCE such as NARCOLEPSY. Note that this drug category does not include broadly-acting central nervous system stimulants such as AMPHETAMINES.
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.
A family of hexahydropyridines.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Agents inhibiting the effect of narcotics on the central nervous system.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.
Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.
Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.
Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
Biphenyl compounds are a class of organic compounds consisting of two phenyl rings attached to a central carbon atom, with potential medical applications as anti-inflammatory and anti-cancer agents.
Compounds with BENZENE fused to AZEPINES.
Tetrazoles are a class of heterocyclic compounds with potential medicinal applications, including as antimicrobial agents, anticancer drugs, and anesthetics.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Purine bases found in body tissues and fluids and in some plants.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.
Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).
A group of compounds that contain the structure SO2NH2.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
Hypoxia-inducible factor 1, alpha subunit is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.
Quinoxalines are a class of heterocyclic compounds with two nitrogen atoms in a six-membered ring, which have potential medicinal applications as antimicrobial, antiviral, and anticancer agents.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Seven membered heterocyclic rings containing a NITROGEN atom.
Elements of limited time intervals, contributing to particular results or situations.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
Piperazines are a class of psychoactive drugs that act as anticholinergics, antispasmodics, and central nervous system stimulants, and are sometimes used in the treatment of various medical conditions.
The observable response an animal makes to any situation.
Pyrrolidines are a class of organic compounds containing a five-membered ring with four carbon atoms and one nitrogen atom, which are used in various medical applications such as as analgesics, anti-inflammatory agents, and muscle relaxants.
A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.
A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.
Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.
A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.
Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.
A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.
The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
Use of electric potential or currents to elicit biological responses.
Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
Compounds with a BENZENE fused to IMIDAZOLES.
C57BL mice are a commonly used strain of laboratory mice that are inbred to produce consistent and predictable results in scientific research.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
Injections into the cerebral ventricles.
Drugs that selectively bind to and activate alpha adrenergic receptors.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
Quinuclidines are a class of psychoactive drugs that act as dopamine agonists and antagonists, and have been used in the treatment of Parkinson's disease and schizophrenia.
Benzodiazepinones are a class of drugs that are similar in structure to benzodiazepines and have similar sedative, anxiolytic, and muscle relaxant effects.
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
An interleukin-1 subtype that occurs as a membrane-bound pro-protein form that is cleaved by proteases to form a secreted mature form. Unlike INTERLEUKIN-1BETA both membrane-bound and secreted forms of interleukin-1alpha are biologically active.
Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.

Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. (1/222)

The antimigraine drugs methysergide, ergotamine and dihydroergotamine (DHE) produce selective vasoconstriction in the external carotid bed of vagosympathectomized dogs anaesthetized with pentobarbital and artificially respired, but the receptors involved have not yet been completely characterized. Since the above drugs display affinity for several binding sites, including alpha-adrenoceptors and several 5-HT1 and 5-HT2 receptor subtypes, this study has analysed the mechanisms involved in the above responses. Intracarotid (i.c.) infusions during 1 min of methysergide (31-310 microg min(-1)), ergotamine (0.56-5.6 microg min(-1)) or DHE (5.6-31 microg min(-1)) dose-dependently reduced external carotid blood flow (ECBF) by up to 46+/-4, 37+/-4 and 49+/-5%, respectively. Blood pressure and heart rate remained unchanged. The reductions in ECBF by methysergide were abolished and even reversed to increases in animals pre-treated with GR127935 (10 microg kg(-1), i.v.). The reductions in ECBF by ergotamine and DHE remained unchanged in animals pre-treated (i.v.) with prazosin (300 microg kg(-1)), but were partly antagonized in animals pre-treated with either GR127935 (10 or 30 microg kg(-1)) or yohimbine (1000 microg kg(-1)). Pre-treatment with a combination of GR127935 (30 microg kg(-1)) and yohimbine (1000 microg kg(-1)) abolished the responses to both ergotamine and DHE. The above doses of antagonists were shown to produce selective antagonism at their respective receptors. These results suggest that the external carotid vasoconstrictor responses to methysergide primarily involve 5-HT1B/1D receptors, whereas those to ergotamine and DHE are mediated by 5-HT1B/1D receptors as well as alpha2-adrenoceptors.  (+info)

G-protein activation by putative antagonists at mutant Thr373Lys alpha2A adrenergic receptors. (2/222)

1. Replacement of a threonine by a lysine at position 373 in the C-terminal portion of the third intracellular loop of the human alpha2A-adrenergic receptor (alpha2A AR) has been reported to generate a constitutively active mutant receptor in analogy with similar mutations in the alpha1B and beta2 AR (Ren et al., 1993). In the present study, the mutant Thr373Lys alpha2A AR receptor was investigated by measuring the formation of inositol phosphates in either the absence or presence of mouse G(alpha)15 protein in Cos-7 cells. 2. Increased affinity, potency and/or efficacy for the agonists [(-)-adrenaline, UK 14304, clonidine, guanabenz and oxymetazoline] was observed, consistent with a precoupled mutant alpha2A AR: G-protein state. The basal inositol phosphates response was similar at the wild-type (wt) and mutant alpha2A AR, but was enhanced at the mutant alpha2A AR upon co-expression with the mouse G(alpha)15 protein. This enhanced response could not be attenuated in the presence of any of the tested alpha2 AR antagonists (10 microM), suggesting that inverse agonist activity did not occur at the mutant alpha2A AR. 3. Ligands that so far have been identified as antagonists at the wt alpha2A AR demonstrated either no intrinsic activity (MK 912, WB 4101, RS 15385, RX 811059 and RX 821002) or positive efficacy [Emax, % vs. 1 microM UK 14304: dexefaroxan (27+/-7), idazoxan (34+/-9), atipamezole (27+/-4), BRL 44408 (59+/-5) and SKF 86466 (54+/-9)] at the mutant alpha2A AR, but only in the presence of the mouse G(alpha)15 protein. The ligand potencies corresponded with their respective pKi values at the mutant alpha2A AR receptor. 4. The partial agonist effect of SKF 86466 was resistant to pertussis toxin treatment (100 ng ml(-1)) and not affected by co-expression of the rat G(alpha)i1 protein. It was virtually absent in the presence of 10 microM RS 15385. SKF 86466 was without intrinsic activity upon co-expression of the mouse G(alpha)q protein. 5. Some putative alpha2 AR antagonists exerted a partial agonist activity that was highly dependent on the presence of specific G-protein alpha-subunits, suggesting that these ligands cause selective G-protein activation at the mutant alpha2A AR.  (+info)

Clonidine evokes vasodepressor responses via alpha2-adrenergic receptors in gigantocellular reticular formation. (3/222)

The gigantocellular depressor area (GiDA) is a functionally defined subdivision of the medullary gigantocellular reticular formation where vasodepressor responses are evoked by glutamate nanoinjections. The GiDA also contains reticulospinal neurons that contain the alpha2A-adrenergic receptor (alpha2A-AR). In the present study, we sought to determine whether nanoinjections of the alpha2-AR agonist clonidine into the GiDA evoke cardiovascular responses and whether these responses can be attributed to the alpha2-AR. We found that nanoinjections of clonidine into the GiDA evoke dose-dependent decreases in arterial pressure and heart rate. These responses were equivalent in magnitude to responses produced by clonidine nanoinjections into the sympathoexcitatory region of the rostral ventrolateral medulla. Furthermore, the vasodepressor and bradycardic responses produced by clonidine injections into the GiDA were blocked in a dose-dependent fashion by the highly selective alpha2-AR antagonist 2-methoxyidazoxan, but not by prazosin, which is an antagonist at both the alpha1-AR and the 2B subtype of the alpha-AR. The antagonism by 2-methoxyidazoxan was site specific because injections of the antagonist into the rostral ventrolateral medulla failed to block the responses evoked by clonidine injections into the GiDA. These findings support the notion that clonidine produces sympathoinhibition through multiple sites within the medullary reticular formation, which is consistent with the wide distribution of the alpha2A-AR in reticulospinal neurons. These data also suggest that clonidine may have multiple mechanisms of action because it evokes a cardiovascular depressive response from regions containing neurons that have been determined to be both sympathoinhibitory and sympathoexcitatory.  (+info)

Effects of GABA on noradrenaline release and vasoconstriction induced by renal nerve stimulation in isolated perfused rat kidney. (4/222)

We examined effects of gamma-aminobutyric acid (GABA) on vasoconstriction and noradrenaline (NA) release induced by electrical renal nerve stimulation (RNS) in the isolated pump-perfused rat kidney. RNS (1 and 2 Hz for 2.5 min each, 0.5-ms duration, supramaximal voltage) increased renal perfusion pressure (PP) and renal NA efflux. GABA (3, 10 and 100 microM) attenuated the RNS-induced increases in PP by 10-40% (P<0.01) and NA efflux by 10-30% (P<0.01). GABA did not affect exogenous NA (40 and 60 nM)-induced increases in PP. The selective GABA(B) agonist baclofen (3, 10 and 100 microM) also attenuated the RNS-induced increases in PP and NA efflux, whereas the RNS-induced responses were relatively resistant to the selective GABA(A) agonist muscimol (3, 10 and 100 microM). The selective GABA(B) antagonist 2-hydroxysaclofen (50 microM), but not the selective GABA(A) antagonist bicuculline (50 microM), abolished the inhibitory effects of GABA (10 microM) on the RNS-induced responses. The selective alpha2-adrenoceptor antagonist rauwolscine (10 nM) enhanced the RNS-induced responses. GABA (3, 10 and 100 microM) potently attenuated the RNS-induced increases in PP by 40-60% (P<0.01) and NA efflux by 20-50% (P<0.01) in the presence of rauwolscine. Prazosin (10 and 30 nM) suppressed the RNS-induced increases in PP by about 70-80%. Neither rauwolscine (10 nM) nor GABA (10 microM) suppressed the residual prazosin-resistant PP response. These results suggest that GABA suppresses sympathetic neurotransmitter release via presynaptic GABA(B) receptors, and thereby attenuates adrenergically induced vasoconstriction in the rat kidney.  (+info)

Blocking effects of phentolamine on L-type calcium current and ATP-sensitive potassium current in guinea pig ventricular myocytes. (5/222)

AIM: To study the effect of phentolamine on L-type calcium currents (ICa) and ATP-sensitive K+ currents (IK,ATP) in ventricular myocytes. METHODS: ICa and IK,ATP were observed using patch clamp techniques in whole-cell recording configuration. RESULTS: Phentolamine reduced ICa of ventricular myocytes in concentration-dependent and voltage-independent manners. Phentolamine 5, 25, and 100 mumol.L-1 decreased ICa from 370 +/- 99 nA to 310 +/- 95 nA (17% block, n = 6, P < 0.01), from 230 +/- 98 nA to 180 +/- 73 nA (23% block, n = 5, P < 0.05), and from 293 +/- 66 nA to 206 +/- 44 nA (30% block, n = 5, P < 0.01), respectively, without affecting the current-voltage relationship. Prazosin 100 mumol.L-1 and yohimbine 100 mumol.L-1, which were specific blockers of alpha 1 and alpha 2 adrenoceptors respectively, did not show the inhibitory effect on ICa. Phentolamine 100 mumol.L-1 also inhibited the IK,ATP induced by 2, 4-dinitrophenol (DNP) at 0 mV from 3.2 +/- 0.6 nA to 0.8 +/- 0.5 nA (75% block, n = 4, P < 0.01). CONCLUSION: Phentolamine directly inhibits ICa and IK,ATP in guinea pig ventricular myocytes.  (+info)

Differential cotransmission in sympathetic nerves: role of frequency of stimulation and prejunctional autoreceptors. (6/222)

Recent reports have suggested that sympathetic nerves may store separately and release independently the cotransmitters ATP and norepinephrine (NE). It is conceivable therefore that the quantity of each neurotransmitter that is released from the nerves is not fixed but rather may vary, possibly with the frequency of stimulation. To test this hypothesis we studied the concomitant release at various frequencies and cooperative postjunctional actions of ATP and NE during the first 10 s of electrical field stimulation of the guinea pig vas deferens. We found that at lower frequencies (8 Hz), prejunctional inhibition of the release of NE, which occurs via alpha2-adrenoceptors, modulates the ultimate composition of the cocktail of cotransmitters by limiting the amount of NE that is coreleased with ATP. As the frequency of stimulation increases (above 8 Hz), the autoinhibition of the release of NE is overridden and the amount of NE relative to ATP increases. The smooth muscle of the guinea pig vas deferens reacts to changes in composition of the sympathetic neurochemical messages by increasing the amplitude of its contractions due to the enhancement by NE of the contractile responses triggered by ATP. This evidence suggests that the prejunctional alpha2-adrenoceptor may function as a sensor that "reads" the frequency of action potentials produced during a burst of neuronal activity and converts that information into discrete neurochemical messages with varying proportions of cotransmitters. The mechanism for decoding the informational content of these messages is based on the cooperative postjunctional interactions of the participating cotransmitters.  (+info)

Electrochemical and electrophysiological characterization of neurotransmitter release from sympathetic nerves supplying rat mesenteric arteries. (7/222)

1. Characteristic features of noradrenaline (NA) and adenosine 5'-triphosphate (ATP) release from postganglionic sympathetic nerves in rat small mesenteric arteries in vitro have been investigated on an impulse-by-impulse basis. NA release was measured using continuous amperometry and ATP release was monitored by intracellular recording of excitatory junction potentials (e.j.ps). 2. Electrical stimuli evoked transient increases in oxidation current. During trains of ten stimuli at 0.5 - 4 Hz there was a depression in the amplitude of oxidation currents evoked following the first stimulus in the train. 3. The neuronal NA uptake inhibitor, desmethylimipramine (1 microM), increased the amplitude of the summed oxidation current evoked by ten stimuli at 1 Hz and slowed the decay of oxidation currents evoked by trains of ten stimuli at 1 and 10 Hz. 4. The alpha2-adrenoceptor antagonist, idazoxan (1 microM), increased the amplitudes of the oxidation currents evoked during trains of ten stimuli at 0.5 - 10 Hz but had no effect on the oxidation currents evoked by the first stimulus in the train. 5. Idazoxan (1 microM) increased the amplitude of all e.j.ps evoked during trains of stimuli at 0.5 and 1 Hz. In addition, the facilitatory effect of idazoxan on e.j.ps was significantly greater than that on oxidation currents. 6. The findings indicate that NA release from sympathetic nerves supplying small mesenteric arteries is regulated by activation of presynaptic alpha2-adrenoceptors and that clearance of released NA in this tissue depends, in part, upon neuronal uptake. The different effects of idazoxan on the oxidation currents and e.j.ps may indicate that the release of NA and ATP is differentially modulated.  (+info)

Enhanced cortical dopamine output and antipsychotic-like effects of raclopride by alpha2 adrenoceptor blockade. (8/222)

Clozapine exerts superior clinical efficacy and markedly enhances cortical dopamine output compared with classical antipsychotic drugs. Here the alpha2 adrenoceptor antagonist idazoxan was administered to rats alone or in combination with the D2/3 dopamine receptor antagonist raclopride. Dopamine efflux in the medial prefrontal cortex and conditioned avoidance responding were analyzed. Idazoxan selectively potentiated the cortical output of dopamine and augmented the suppression of conditioned avoidance responding induced by raclopride. These results challenge basic assumptions underlying the dopamine hypothesis of schizophrenia and provide insight into clozapine's mode of action.  (+info)

Receptors, Adrenergic, alpha-2 are a type of protein found on the surface of cells in the body that bind to and respond to a class of hormones called catecholamines, including adrenaline and noradrenaline. These receptors are part of the body's autonomic nervous system and play a role in regulating a variety of physiological processes, including blood pressure, heart rate, and inflammation. Activation of alpha-2 receptors can cause a decrease in heart rate and blood pressure, as well as a decrease in inflammation and pain. They are found in many different tissues throughout the body, including the brain, heart, and blood vessels.

Interleukin 1 Receptor Antagonist Protein (IL-1Ra) is a protein that acts as an antagonist to the Interleukin 1 (IL-1) cytokine family. IL-1 is a group of signaling molecules that play a crucial role in the immune response and inflammation. IL-1Ra binds to the IL-1 receptor and prevents IL-1 from binding to its receptor, thereby inhibiting its pro-inflammatory effects. IL-1Ra is produced by various cells in the body, including monocytes, macrophages, and fibroblasts, and is released in response to inflammation or injury. It is also found in high concentrations in synovial fluid, which is the fluid that lubricates the joints. IL-1Ra has been shown to have anti-inflammatory and immunosuppressive effects, and it has been used in clinical trials to treat various inflammatory and autoimmune diseases, such as rheumatoid arthritis, psoriasis, and inflammatory bowel disease. It is also being studied as a potential treatment for COVID-19, as it may help to reduce inflammation and prevent severe illness.

Piperidines are a class of organic compounds that contain a six-membered ring with nitrogen atoms at positions 1 and 4. They are commonly used in the pharmaceutical industry as a building block for the synthesis of a wide range of drugs, including analgesics, anti-inflammatory agents, and antihistamines. Piperidines are also found in natural products, such as alkaloids, and have been used in traditional medicine for their various therapeutic effects. In the medical field, piperidines are often used as a starting point for the development of new drugs, as they can be easily modified to produce a wide range of pharmacological activities.

Angiotensin receptor antagonists (ARAs) are a class of medications used in the medical field to treat high blood pressure (hypertension) and heart failure. These drugs work by blocking the action of angiotensin II, a hormone that narrows blood vessels and increases blood pressure. By blocking this hormone, ARAs help to relax blood vessels and lower blood pressure, which can reduce the risk of heart attack, stroke, and other complications associated with hypertension and heart failure. ARAs are available in both oral and injectable forms and are often used in combination with other blood pressure-lowering medications.

Adenosine A2 receptor antagonists are a class of drugs that block the action of adenosine A2 receptors in the body. Adenosine is a naturally occurring molecule that plays a role in regulating various physiological processes, including blood flow, heart rate, and inflammation. The A2 receptors are a subfamily of adenosine receptors that are found in many different tissues throughout the body. Adenosine A2 receptor antagonists are used to treat a variety of conditions, including hypertension (high blood pressure), heart failure, and asthma. They work by blocking the action of adenosine on the A2 receptors, which can help to relax blood vessels and reduce blood pressure. In heart failure, A2 receptor antagonists can help to improve heart function and reduce the workload on the heart. In asthma, they can help to reduce inflammation and bronchoconstriction (narrowing of the airways). Some examples of adenosine A2 receptor antagonists include cilostazol, pirenzepine, and ZM-241385. These drugs are typically administered orally or intravenously, and their side effects can include headache, nausea, and dizziness. It is important to note that the use of adenosine A2 receptor antagonists should be closely monitored by a healthcare provider, as they can interact with other medications and may have potential side effects.

Hormone antagonists are medications that block or inhibit the effects of hormones in the body. They are often used in medical treatments to counteract the effects of hormones that are either overactive or underactive. Examples of hormone antagonists include: 1. Selective estrogen receptor modulators (SERMs): These medications block the effects of estrogen in some tissues but not others. They are used to treat conditions such as breast cancer and osteoporosis. 2. Progestins: These medications mimic the effects of the hormone progesterone and are used to treat conditions such as menopause symptoms and endometriosis. 3. Androgens: These medications block the effects of testosterone and are used to treat conditions such as prostate cancer and hirsutism (excessive hair growth in women). 4. Gonadotropin-releasing hormone (GnRH) antagonists: These medications block the release of gonadotropins, hormones that stimulate the ovaries and testes to produce sex hormones. They are used to treat conditions such as endometriosis and prostate cancer. Overall, hormone antagonists are an important tool in the medical field for treating a variety of conditions related to hormonal imbalances.

Adenosine A1 receptor antagonists are a class of drugs that block the action of adenosine A1 receptors in the body. Adenosine is a naturally occurring molecule that plays a role in regulating various physiological processes, including heart rate, blood pressure, and sleep. Adenosine A1 receptors are found in many different tissues throughout the body, including the brain, heart, and lungs. Adenosine A1 receptor antagonists are used to treat a variety of conditions, including Parkinson's disease, schizophrenia, and overactive bladder. They work by blocking the action of adenosine at A1 receptors, which can help to improve symptoms and reduce the risk of side effects associated with other treatments. Some examples of adenosine A1 receptor antagonists include caffeine, theophylline, and modafinil.

Receptors, Endothelin are a type of protein receptors found on the surface of cells in the endothelium, which is the inner lining of blood vessels. These receptors are activated by the hormone endothelin, which is produced by cells in the walls of blood vessels and plays a role in regulating blood pressure and blood vessel tone. Activation of endothelin receptors can cause blood vessels to constrict, which can increase blood pressure and reduce blood flow to organs and tissues. Endothelin receptors are also involved in the development of certain cardiovascular diseases, such as hypertension and heart failure.

Adrenergic alpha-1 receptor antagonists are a class of medications that block the action of alpha-1 adrenergic receptors in the body. These receptors are found in various tissues, including blood vessels, the heart, and the smooth muscle of the bronchial tubes. When activated by the hormone adrenaline (also known as epinephrine), alpha-1 receptors cause constriction of blood vessels, increased heart rate, and bronchoconstriction. Adrenergic alpha-1 receptor antagonists are used to treat a variety of conditions, including high blood pressure, heart disease, and certain types of anxiety disorders. They work by relaxing blood vessels, reducing blood pressure, and slowing the heart rate. They can also help to relieve symptoms of anxiety and panic attacks by reducing the physical symptoms of stress, such as rapid heart rate and sweating. Some examples of adrenergic alpha-1 receptor antagonists include prazosin (Minipress), doxazosin (Cardura), and terazosin (Hytrin). These medications are usually taken by mouth and are generally well-tolerated, although they can cause side effects such as dizziness, lightheadedness, and low blood pressure.

Sialoglycoproteins are a type of glycoprotein that are found in the saliva of humans and other animals. They are composed of a protein core and one or more carbohydrate chains attached to the protein. Sialoglycoproteins play important roles in a variety of biological processes, including the lubrication and protection of the oral mucosa, the breakdown of food in the mouth, and the immune response. They are also involved in the development and progression of certain diseases, such as cancer and autoimmune disorders. In the medical field, sialoglycoproteins are often studied as potential biomarkers for these and other conditions.

Receptors, Adrenergic, alpha (α-adrenergic receptors) are a type of protein found on the surface of cells in the body that bind to and respond to signaling molecules called catecholamines, such as adrenaline and noradrenaline. These receptors are involved in a wide range of physiological processes, including the regulation of blood pressure, heart rate, and metabolism. There are several different subtypes of α-adrenergic receptors, including α1A, α1B, and α1D receptors, which are found in different tissues throughout the body. Activation of these receptors can have a variety of effects, depending on the specific subtype and the tissue in which it is located. For example, activation of α1-adrenergic receptors in the heart can cause the heart to beat faster and stronger, while activation of α1-adrenergic receptors in the blood vessels can cause them to constrict, leading to an increase in blood pressure. α-adrenergic receptors are also involved in the body's response to stress and can be activated by the release of stress hormones such as cortisol. Activation of these receptors can help to prepare the body for the "fight or flight" response by increasing heart rate and blood pressure and redirecting blood flow to the muscles.

Alpha 1-Antitrypsin (AAT) is a protein produced by the liver that plays a crucial role in protecting the lungs from damage caused by enzymes called proteases. Proteases are enzymes that break down proteins, and in the lungs, they can cause inflammation and damage to the airways and lung tissue. AAT acts as a protease inhibitor, binding to and neutralizing proteases that would otherwise cause damage to the lungs. It is particularly important in protecting the lungs from damage caused by cigarette smoke, air pollution, and other irritants. Deficiency in AAT can lead to a condition called alpha 1-antitrypsin deficiency, which is a genetic disorder that can cause lung disease, liver disease, and other health problems. People with alpha 1-antitrypsin deficiency produce low levels of AAT or produce AAT that is not functional, leading to an increased risk of lung damage and other health problems.

Leukotriene antagonists are a class of medications that block the action of leukotrienes, which are chemical messengers produced by the immune system. These drugs are used to treat a variety of conditions, including asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis (hay fever). Leukotrienes play a role in the inflammatory response and can cause constriction of the airways, leading to difficulty breathing. By blocking the action of leukotrienes, leukotriene antagonists can help to relax the airways and improve breathing in people with asthma or COPD. There are several different types of leukotriene antagonists available, including montelukast (Singulair) and zafirlukast (Accolate). These drugs are usually taken by mouth and are generally well-tolerated. However, like all medications, they can cause side effects, such as headache, nausea, and dizziness. It is important to talk to a healthcare provider about the potential benefits and risks of leukotriene antagonists before starting treatment.

The Endothelin A receptor (ETA receptor) is a protein that is found on the surface of cells in the body, particularly in the endothelium (the inner lining of blood vessels). It is a type of G protein-coupled receptor, which means that it is activated by a molecule called an agonist, such as endothelin-1, and triggers a series of cellular responses. The ETA receptor plays a role in regulating blood pressure and blood vessel tone, and is also involved in the development and progression of certain diseases, such as hypertension, heart failure, and atherosclerosis. Activation of the ETA receptor can cause vasoconstriction (narrowing of blood vessels), which can increase blood pressure, and can also stimulate the release of other signaling molecules that can contribute to inflammation and tissue damage. In the medical field, the ETA receptor is an important target for the development of drugs that are used to treat cardiovascular diseases. For example, some drugs that block the ETA receptor, such as bosentan and ambrisentan, are used to treat pulmonary hypertension, a condition in which blood pressure in the lungs is abnormally high.

Receptors, Serotonin are proteins found on the surface of cells in the body that bind to serotonin, a neurotransmitter that plays a role in regulating mood, appetite, and other bodily functions. There are several different types of serotonin receptors, each of which has a specific function and is activated by different types of serotonin molecules. Dysfunction of serotonin receptors has been implicated in a number of mental health conditions, including depression, anxiety, and obsessive-compulsive disorder. Medications that target serotonin receptors, such as selective serotonin reuptake inhibitors (SSRIs), are commonly used to treat these conditions.

Receptors, N-Methyl-D-Aspartate (NMDA) are a type of ionotropic glutamate receptor found in the central nervous system. They are named after the agonist N-methyl-D-aspartate (NMDA), which binds to and activates these receptors. NMDA receptors are important for a variety of physiological processes, including learning and memory, synaptic plasticity, and neuroprotection. They are also involved in various neurological and psychiatric disorders, such as schizophrenia, depression, and addiction. NMDA receptors are heteromeric complexes composed of two subunits, NR1 and NR2, which can be differentially expressed in various brain regions and cell types. The NR2 subunit determines the pharmacological properties and functional profile of the receptor, while the NR1 subunit is essential for receptor function. Activation of NMDA receptors requires the binding of both glutamate and a co-agonist, such as glycine or d-serine, as well as the depolarization of the postsynaptic membrane. This leads to the opening of a cation-permeable channel that allows the influx of calcium ions, which can trigger various intracellular signaling pathways and modulate gene expression. In summary, NMDA receptors are a type of glutamate receptor that play a crucial role in various physiological and pathological processes in the central nervous system.

Dizocilpine maleate, also known as dizocilpine or dizocilpine dibromide, is a drug that belongs to a class of compounds called N-methyl-D-aspartate (NMDA) receptor antagonists. It is used in scientific research to study the effects of NMDA receptor antagonists on the brain and nervous system. In the medical field, dizocilpine maleate has been studied for its potential therapeutic effects in a variety of neurological and psychiatric conditions, including Parkinson's disease, Huntington's disease, and schizophrenia. However, it has not been approved for use in humans by regulatory agencies such as the US Food and Drug Administration (FDA) due to concerns about its safety and efficacy. Dizocilpine maleate is a potent and selective NMDA receptor antagonist that blocks the action of glutamate, a neurotransmitter that plays a key role in learning, memory, and other cognitive functions. It is believed that by blocking NMDA receptors, dizocilpine maleate can reduce the overactivity of neurons in the brain that is thought to contribute to the symptoms of certain neurological and psychiatric conditions. However, dizocilpine maleate has also been associated with a range of side effects, including cognitive impairment, psychosis, and motor dysfunction. As a result, its use in humans is limited and is typically only conducted in controlled clinical trials under the supervision of a qualified healthcare professional.

Receptors, Interleukin-1 (IL-1R) are a type of cell surface receptor that are activated by the cytokine interleukin-1 (IL-1). IL-1 is a signaling molecule that plays a key role in the immune response and inflammation. It is produced by immune cells in response to infection or injury and can stimulate the production of other cytokines, as well as activate immune cells such as macrophages and T cells. IL-1R are expressed on a variety of cell types, including immune cells, endothelial cells, and fibroblasts. When IL-1 binds to its receptor, it triggers a signaling cascade that leads to the activation of various intracellular signaling pathways, including the NF-κB pathway and the MAPK pathway. These pathways can activate genes that produce pro-inflammatory molecules, such as cytokines and chemokines, as well as genes that regulate cell survival and proliferation. IL-1R are important in the regulation of the immune response and inflammation, and are also involved in the development of various diseases, including autoimmune diseases, inflammatory bowel disease, and cancer. Inhibitors of IL-1R or its downstream signaling pathways are being developed as potential therapeutic agents for these diseases.

Adrenergic alpha-2 receptor antagonists are a class of medications that block the action of adrenergic alpha-2 receptors in the body. These receptors are found in various tissues, including the heart, blood vessels, and central nervous system, and play a role in regulating blood pressure, heart rate, and other physiological processes. When adrenergic alpha-2 receptor antagonists are taken, they block the action of these receptors, leading to a variety of effects. For example, they can cause blood vessels to dilate, which can lower blood pressure, and they can increase heart rate and contractility, which can improve cardiac output. They can also have central nervous system effects, such as increasing alertness and reducing sedation. Adrenergic alpha-2 receptor antagonists are used to treat a variety of conditions, including hypertension, heart failure, and anxiety. They are also used in some cases of shock and as part of the treatment of certain types of cancer. Some examples of adrenergic alpha-2 receptor antagonists include clonidine, guanfacine, and moxonidine.

Adrenergic alpha-antagonists are a class of drugs that block the action of alpha-adrenergic receptors, which are a type of receptor found in the body that respond to the neurotransmitter norepinephrine (also known as noradrenaline). These receptors are found in various tissues throughout the body, including the blood vessels, heart, and bronchial muscles. When alpha-adrenergic receptors are activated by norepinephrine, they cause a variety of physiological responses, including constriction of blood vessels, increased heart rate and contractility, and bronchoconstriction. Adrenergic alpha-antagonists work by binding to these receptors and blocking their action, thereby reversing these effects. Adrenergic alpha-antagonists are used to treat a variety of conditions, including high blood pressure, heart disease, and glaucoma. They are also used to treat certain types of anxiety disorders and to prevent migraine headaches. Some examples of adrenergic alpha-antagonists include prazosin (Minipress), doxazosin (Cardura), and phentolamine (Regitine).

Biphenyl compounds are a class of organic compounds that consist of two benzene rings joined together by a single carbon-carbon bond. They are commonly used as industrial solvents, plasticizers, and flame retardants. In the medical field, biphenyl compounds have been studied for their potential therapeutic effects, including anti-inflammatory, anti-cancer, and anti-viral properties. Some biphenyl compounds have also been used as diagnostic agents in medical imaging. However, some biphenyl compounds have been associated with adverse health effects, including endocrine disruption, neurotoxicity, and carcinogenicity, and their use is regulated in many countries.

Benzazepines are a class of psychoactive drugs that are structurally related to benzodiazepines. They are characterized by the presence of a benzene ring fused to an azepine ring, which gives them their unique chemical structure and pharmacological properties. Benzazepines are primarily used as anxiolytics, sedatives, and hypnotics to treat conditions such as anxiety, insomnia, and agitation. They work by enhancing the activity of the neurotransmitter gamma-aminobutyric acid (GABA) in the brain, which helps to reduce anxiety and promote relaxation. Some examples of benzazepines include thienotriazolodiazepines (e.g., flunitrazepam), dibenzazepines (e.g., zolpidem), and benzodiazepine-like compounds (e.g., alprazolam). However, benzazepines are generally less commonly used than benzodiazepines due to their potential for abuse and dependence, as well as their side effects, which can include drowsiness, dizziness, and impaired coordination.

Tetrazoles are a class of organic compounds that contain a five-membered ring with four nitrogen atoms and one carbon atom. They have a variety of applications in the medical field, including as antimicrobial agents, anticancer drugs, and as inhibitors of enzymes involved in various biological processes. One example of a tetrazole-based drug is linezolid, which is an antibiotic used to treat bacterial infections, including pneumonia, skin infections, and bone and joint infections. Linezolid works by inhibiting the production of bacterial proteins, which are essential for the bacteria's survival. Tetrazoles are also being investigated as potential treatments for cancer. For example, some tetrazole derivatives have been shown to selectively target and kill cancer cells, while sparing healthy cells. Additionally, tetrazoles have been found to have anti-inflammatory and analgesic properties, which could make them useful in the treatment of pain and other inflammatory conditions. Overall, tetrazoles are a versatile class of compounds with a wide range of potential applications in the medical field.

Pyridines are a class of heterocyclic aromatic compounds that contain a six-membered ring with one nitrogen atom and five carbon atoms. They are commonly used in the medical field as precursors for the synthesis of various drugs and as ligands in metal complexes that have potential therapeutic applications. Some examples of drugs that contain pyridine rings include the antihistamine loratadine, the antipsychotic drug chlorpromazine, and the anti-inflammatory drug ibuprofen. Pyridines are also used as chelating agents to remove heavy metals from the body, and as corrosion inhibitors in the manufacturing of metal products.

Xanthines are a group of compounds that include caffeine, theophylline, and theobromine. They are naturally occurring alkaloids found in plants such as coffee, tea, and cocoa. In the medical field, xanthines are used as bronchodilators to treat conditions such as asthma and chronic obstructive pulmonary disease (COPD). They work by relaxing the muscles in the airways, allowing air to flow more easily. Xanthines can also be used to treat heart rhythm disorders and to prevent blood clots. However, they can have side effects such as nausea, vomiting, and increased heart rate, and may interact with other medications.

In the medical field, peptides are short chains of amino acids that are linked together by peptide bonds. Cyclic peptides are a type of peptide in which the amino acids are linked in a ring-like structure, rather than in a linear chain. These cyclic peptides can have a variety of biological activities, including antimicrobial, antiviral, and anti-inflammatory effects. They are being studied for their potential use in the development of new drugs and therapies.

Sulfonamides are a class of synthetic antimicrobial drugs that were first discovered in the 1930s. They are commonly used to treat a variety of bacterial infections, including urinary tract infections, respiratory infections, and skin infections. Sulfonamides work by inhibiting the production of folic acid by bacteria, which is essential for their growth and reproduction. They are often used in combination with other antibiotics to increase their effectiveness. Sulfonamides are generally well-tolerated, but can cause side effects such as nausea, vomiting, and allergic reactions in some people.

Indoles are a class of organic compounds that contain a six-membered aromatic ring with a nitrogen atom at one of the corners of the ring. They are commonly found in a variety of natural products, including some plants, bacteria, and fungi. In the medical field, indoles have been studied for their potential therapeutic effects, particularly in the treatment of cancer. Some indoles have been shown to have anti-inflammatory, anti-cancer, and anti-bacterial properties, and are being investigated as potential drugs for the treatment of various diseases.

In the medical field, "binding, competitive" refers to a type of interaction between a ligand (a molecule that binds to a receptor) and a receptor. Competitive binding occurs when two or more ligands can bind to the same receptor, but they do so in a way that limits the maximum amount of ligand that can bind to the receptor at any given time. In other words, when a ligand binds to a receptor, it competes with other ligands that may also be trying to bind to the same receptor. The binding of one ligand can prevent or reduce the binding of other ligands, depending on the relative affinities of the ligands for the receptor. Competitive binding is an important concept in pharmacology, as it helps to explain how drugs can interact with receptors in the body and how their effects can be influenced by other drugs or substances that may also be present. It is also important in the study of biological systems, where it can help to explain how molecules interact with each other in complex biological networks.

Pyrazoles are a class of heterocyclic compounds that contain a five-membered ring with one nitrogen atom and two carbon atoms. They are commonly used in the medical field as pharmaceuticals and as active ingredients in various drugs. Pyrazoles have a wide range of biological activities, including anti-inflammatory, antifungal, antiviral, and antihypertensive properties. Some examples of drugs that contain pyrazoles include: 1. Metformin: A medication used to treat type 2 diabetes. 2. Etoricoxib: A nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation. 3. Ritonavir: An antiretroviral drug used to treat HIV/AIDS. 4. Alendronate: A medication used to treat osteoporosis. 5. Cilostazol: A medication used to treat peripheral arterial disease. Pyrazoles are also used as research tools in the field of medicinal chemistry to develop new drugs with specific biological activities.

Hypoxia-inducible factor 1, alpha subunit (HIF-1α) is a protein that plays a critical role in the body's response to low oxygen levels (hypoxia). It is a transcription factor that regulates the expression of genes involved in oxygen transport, metabolism, and angiogenesis (the formation of new blood vessels). Under normal oxygen conditions, HIF-1α is rapidly degraded by the proteasome, a protein complex that breaks down unnecessary or damaged proteins. However, when oxygen levels drop, HIF-1α is stabilized and accumulates in the cell. This allows it to bind to specific DNA sequences and activate the transcription of genes involved in the body's response to hypoxia. HIF-1α is involved in a wide range of physiological processes, including erythropoiesis (the production of red blood cells), angiogenesis, and glucose metabolism. It is also implicated in the development of several diseases, including cancer, cardiovascular disease, and neurodegenerative disorders. In the medical field, HIF-1α is a target for drug development, as modulating its activity has the potential to treat a variety of conditions. For example, drugs that inhibit HIF-1α activity may be useful in treating cancer, as many tumors rely on HIF-1α to survive in low-oxygen environments. On the other hand, drugs that activate HIF-1α may be useful in treating conditions such as anemia or heart failure, where increased oxygen delivery is needed.

Quinoxalines are a class of heterocyclic compounds that contain two nitrogen atoms in a six-membered ring. They are often used as intermediates in the synthesis of other compounds, such as pharmaceuticals and agrochemicals. In the medical field, quinoxalines have been studied for their potential use as antiviral, antifungal, and antiparasitic agents. Some quinoxalines have also been shown to have anti-inflammatory and analgesic properties, and are being investigated as potential treatments for a variety of conditions, including cancer, Alzheimer's disease, and Parkinson's disease. However, more research is needed to fully understand the potential therapeutic applications of quinoxalines.

In the medical field, "Cells, Cultured" refers to cells that have been grown and maintained in a controlled environment outside of their natural biological context, typically in a laboratory setting. This process is known as cell culture and involves the isolation of cells from a tissue or organism, followed by their growth and proliferation in a nutrient-rich medium. Cultured cells can be derived from a variety of sources, including human or animal tissues, and can be used for a wide range of applications in medicine and research. For example, cultured cells can be used to study the behavior and function of specific cell types, to develop new drugs and therapies, and to test the safety and efficacy of medical products. Cultured cells can be grown in various types of containers, such as flasks or Petri dishes, and can be maintained at different temperatures and humidity levels to optimize their growth and survival. The medium used to culture cells typically contains a combination of nutrients, growth factors, and other substances that support cell growth and proliferation. Overall, the use of cultured cells has revolutionized medical research and has led to many important discoveries and advancements in the field of medicine.

Azepines are a class of organic compounds that contain a seven-membered ring with four nitrogen atoms and three carbon atoms. They are often used as a building block for the synthesis of other drugs and are also used as anticonvulsants, anxiolytics, and sedatives in the medical field. Some common examples of azepines include triazolam (a benzodiazepine used to treat anxiety and insomnia), alprazolam (another benzodiazepine used to treat anxiety and panic disorder), and meprobamate (an antianxiety medication).

Losartan is a medication used to treat high blood pressure (hypertension) and to reduce the risk of stroke in people with high blood pressure and diabetes. It belongs to a class of drugs called angiotensin II receptor blockers (ARBs), which work by relaxing blood vessels and decreasing the workload on the heart. Losartan is also used to treat heart failure and to reduce the risk of heart attack in people who have had a heart attack or who have certain risk factors for heart disease. It is usually taken once or twice a day, with or without food. Common side effects of losartan include headache, dizziness, and cough.

Endothelin-1 (ET-1) is a potent vasoconstrictor peptide hormone that is primarily produced by endothelial cells in the walls of blood vessels. It plays a key role in regulating blood pressure and blood vessel tone, and is also involved in a variety of other physiological processes, including cell growth and differentiation, inflammation, and angiogenesis (the formation of new blood vessels). In the medical field, ET-1 is often measured as a biomarker for various cardiovascular diseases, such as hypertension, heart failure, and atherosclerosis. It is also used as a therapeutic target in the treatment of these conditions, with drugs such as endothelin receptor antagonists (ERAs) being developed to block the effects of ET-1 and improve cardiovascular outcomes. Additionally, ET-1 has been implicated in the pathogenesis of other diseases, such as cancer and fibrosis, and is being studied as a potential therapeutic target in these conditions as well.

Substance P is a neuropeptide that is involved in the transmission of pain signals in the nervous system. It is a small protein that is produced by sensory neurons in the peripheral nervous system and is released into the spinal cord and brain when these neurons are activated by noxious stimuli such as injury or inflammation. Substance P acts on specific receptors on nerve cells in the spinal cord and brain, triggering the release of other neurotransmitters and hormones that contribute to the perception of pain. It is also involved in other physiological processes, such as regulating blood pressure and heart rate. In the medical field, substance P is often studied in the context of pain management and the development of new pain medications. It is also used as a diagnostic tool in certain conditions, such as inflammatory bowel disease and irritable bowel syndrome, where it may be present in higher levels in the body.

The alpha7 nicotinic acetylcholine receptor (α7nAChR) is a type of ion channel protein found on the surface of certain cells in the nervous system. It is activated by the neurotransmitter acetylcholine, which is released by nerve cells (neurons) to communicate with each other. The α7nAChR plays a role in a number of important functions in the brain and body, including learning and memory, mood regulation, and muscle movement. It is also involved in the development and progression of certain neurological disorders, such as Alzheimer's disease, Parkinson's disease, and schizophrenia. In the medical field, the α7nAChR is being studied as a potential target for the development of new treatments for these and other conditions. For example, drugs that selectively activate the α7nAChR are being investigated as potential treatments for cognitive decline and other symptoms associated with Alzheimer's disease.

Serotonin is a neurotransmitter, a chemical messenger that transmits signals between nerve cells in the brain and throughout the body. It plays a crucial role in regulating mood, appetite, sleep, and other bodily functions. In the medical field, serotonin is often studied in relation to mental health conditions such as depression, anxiety, and obsessive-compulsive disorder (OCD). Low levels of serotonin have been linked to these conditions, and medications such as selective serotonin reuptake inhibitors (SSRIs) are often prescribed to increase serotonin levels in the brain and improve symptoms. Serotonin is also involved in the regulation of pain perception, blood pressure, and other bodily functions. Imbalances in serotonin levels have been implicated in a variety of medical conditions, including migraines, fibromyalgia, and irritable bowel syndrome (IBS).

Receptors, Bradykinin are a type of protein receptors found on the surface of cells in the body that bind to and respond to the hormone bradykinin. Bradykinin is a peptide hormone that plays a role in the inflammatory response and is involved in the regulation of blood pressure, pain, and other physiological processes. When bradykinin binds to its receptors, it triggers a cascade of chemical reactions within the cell that leads to various physiological effects. There are two main types of bradykinin receptors: B1 receptors and B2 receptors. B1 receptors are primarily found in the immune system and are involved in the inflammatory response, while B2 receptors are found in a wide range of tissues and are involved in a variety of physiological processes, including blood pressure regulation and pain perception.

Cimetidine is a medication that is primarily used to treat ulcers in the stomach and esophagus. It works by blocking the production of stomach acid, which can help to reduce pain and inflammation associated with ulcers. Cimetidine is also sometimes used to treat other conditions, such as heartburn, GERD (gastroesophageal reflux disease), and certain types of cancer. It is available in both oral and intravenous forms, and is typically taken two to four times per day. Side effects of cimetidine may include headache, dizziness, nausea, and constipation. It is important to follow the dosage instructions provided by your healthcare provider and to let them know if you experience any side effects while taking this medication.

Receptors, Neurokinin-1 (NK1 receptors) are a type of G protein-coupled receptor found on the surface of certain cells in the body, including nerve cells (neurons) and immune cells. These receptors are activated by a group of signaling molecules called neurokinins, which are released by nerve cells in response to various stimuli, such as injury, stress, or inflammation. NK1 receptors play a role in a number of physiological processes, including pain perception, inflammation, and regulation of the immune system. They are also involved in the development of certain diseases, such as chronic pain, asthma, and irritable bowel syndrome. In the medical field, NK1 receptors are targeted by drugs used to treat a variety of conditions, including pain, nausea, and inflammation. One example of a drug that targets NK1 receptors is aprepitant, which is used to prevent nausea and vomiting caused by chemotherapy. Other drugs that target NK1 receptors include telaprevir and maraviroc, which are used to treat hepatitis C and HIV, respectively.

Adenosine A3 receptor antagonists are a class of drugs that block the action of adenosine A3 receptors, which are a type of cell receptor found in various tissues throughout the body. These receptors play a role in regulating a number of physiological processes, including inflammation, pain, and cardiovascular function. Adenosine A3 receptor antagonists are being studied for their potential therapeutic applications in a variety of conditions, including chronic obstructive pulmonary disease (COPD), asthma, and cardiovascular disease. They may also have potential as treatments for certain types of cancer and neurological disorders. Some examples of adenosine A3 receptor antagonists that have been studied in clinical trials include MRS1191, MRS1522, and MRS1754. These drugs are typically administered orally or intravenously, and their side effects and potential interactions with other medications will depend on the specific drug being used.

The Endothelin B receptor (ETB) is a protein that is found on the surface of cells in the body, including cells in the cardiovascular system. It is a type of G protein-coupled receptor, which means that it is activated by the binding of a signaling molecule called an agonist, such as endothelin-1 or endothelin-3. When the ETB receptor is activated, it triggers a series of intracellular signaling events that can have a variety of effects on the cell, depending on the specific cell type and the context in which the receptor is activated. In the cardiovascular system, the ETB receptor is thought to play a role in regulating blood pressure and blood vessel tone, and it has been implicated in a number of cardiovascular diseases, including hypertension, heart failure, and atherosclerosis.

Piperazines are a class of organic compounds that contain a six-membered ring with two nitrogen atoms. They are commonly used in the medical field as drugs and are known for their anticholinergic, antispasmodic, and sedative properties. Some examples of piperazine-based drugs include antihistamines, antipsychotics, and antidiarrheals. Piperazines can also be used as intermediates in the synthesis of other drugs.

In the medical field, "Behavior, Animal" refers to the study of the actions, responses, and interactions of animals, including humans, with their environment. This field encompasses a wide range of topics, including animal behavior in the wild, animal behavior in captivity, animal behavior in domestic settings, and animal behavior in laboratory settings. Animal behaviorists study a variety of behaviors, including social behavior, mating behavior, feeding behavior, communication behavior, and aggression. They use a variety of research methods, including observational studies, experiments, and surveys, to understand the underlying mechanisms that drive animal behavior. Animal behavior research has important applications in fields such as conservation biology, animal welfare, and veterinary medicine. For example, understanding animal behavior can help conservationists develop effective strategies for protecting endangered species, and it can help veterinarians develop more effective treatments for behavioral disorders in animals.

Pyrrolidines are a class of organic compounds that contain a five-membered ring with four carbon atoms and one nitrogen atom. They are commonly used in the medical field as pharmaceuticals, as well as in the synthesis of other drugs and chemicals. One example of a pyrrolidine used in medicine is metoclopramide, which is used to treat nausea and vomiting. Another example is pyrilamine, which is used to treat allergies and hay fever. Pyrrolidines can also be used as chiral auxiliaries in organic synthesis, which allows for the synthesis of enantiomerically pure compounds. This is important in the pharmaceutical industry, as many drugs are effective only when administered in a specific enantiomer. Overall, pyrrolidines are a versatile class of compounds with a wide range of applications in the medical field.

Receptors, Adrenergic, alpha-1 are a type of protein receptors found on the surface of cells in the body that bind to and respond to certain hormones and neurotransmitters, specifically norepinephrine and epinephrine. These receptors are classified as alpha-1 receptors because they are activated by alpha-1 adrenergic agonists, which are drugs that mimic the effects of norepinephrine and epinephrine. Alpha-1 receptors are found in many different tissues throughout the body, including the heart, blood vessels, lungs, and urinary bladder. They play a role in a variety of physiological processes, including regulating blood pressure, heart rate, and smooth muscle contraction. When norepinephrine or epinephrine binds to an alpha-1 receptor, it triggers a series of chemical reactions within the cell that ultimately lead to the activation of various signaling pathways. These pathways can have a variety of effects, depending on the specific type of alpha-1 receptor and the tissue in which it is located. Alpha-1 receptors are also targeted by certain drugs, such as alpha-1 adrenergic blockers, which are used to treat conditions such as high blood pressure, benign prostatic hyperplasia, and urinary incontinence. These drugs work by blocking the binding of norepinephrine and epinephrine to alpha-1 receptors, thereby reducing their effects on the body.

Interleukin-1 (IL-1) is a type of cytokine, which is a signaling molecule that plays a crucial role in the immune system. IL-1 is produced by various types of immune cells, including macrophages, monocytes, and dendritic cells, in response to infection, injury, or inflammation. IL-1 has multiple functions in the immune system, including promoting the activation and proliferation of immune cells, enhancing the production of other cytokines, and regulating the inflammatory response. It can also stimulate the production of fever, which helps to fight off infections. In the medical field, IL-1 is often studied in the context of various diseases, including autoimmune disorders, inflammatory bowel disease, and rheumatoid arthritis. It is also being investigated as a potential target for the development of new treatments for these conditions.

Receptors, Cholecystokinin (CCK) are a type of protein receptor found in the cells of various organs in the body, including the pancreas, small intestine, and brain. These receptors are activated by the hormone cholecystokinin, which is produced by the cells of the small intestine in response to the presence of food in the stomach. When cholecystokinin binds to its receptors, it triggers a series of chemical reactions that lead to the release of digestive enzymes from the pancreas and the contraction of the muscles of the small intestine. This helps to move food through the digestive system and prepare it for absorption. In addition to its role in digestion, cholecystokinin has been found to play a role in regulating appetite, mood, and other physiological processes. It is also involved in the development of certain types of cancer, including pancreatic cancer. Overall, receptors, cholecystokinin are an important part of the body's digestive system and play a role in regulating a variety of physiological processes.

Devazepide is a medication used to treat high blood pressure (hypertension) and to reduce the risk of stroke and heart attack in people with high blood pressure and diabetes. It belongs to a class of drugs called diuretics, which work by increasing the amount of urine produced by the kidneys, which helps to lower blood pressure. Devazepide is taken by mouth and is usually prescribed once or twice a day. It is important to follow the instructions of your healthcare provider and to take the medication as directed. Devazepide may cause side effects, such as dizziness, headache, and stomach upset. It is important to talk to your healthcare provider if you experience any side effects while taking this medication.

Adrenergic antagonists are a class of drugs that block the action of adrenalin or noradrenaline, which are hormones that stimulate the sympathetic nervous system. These drugs are used to treat a variety of conditions, including high blood pressure, heart disease, and anxiety disorders. They work by blocking the receptors on cells that respond to adrenalin and noradrenaline, preventing these hormones from triggering a response. There are several different types of adrenergic antagonists, including beta blockers, alpha blockers, and mixed alpha and beta blockers. Beta blockers are used to treat high blood pressure, heart disease, and certain types of tremors, while alpha blockers are used to treat conditions such as high blood pressure, benign prostatic hyperplasia, and urinary incontinence. Mixed alpha and beta blockers are used to treat conditions such as hypertension and angina.

Prazosin is a medication that is used to treat high blood pressure (hypertension) and certain heart conditions, such as angina (chest pain) and heart failure. It belongs to a class of drugs called alpha blockers, which work by relaxing blood vessels and decreasing the workload on the heart. Prazosin is usually taken by mouth, and the dosage and duration of treatment will depend on the specific condition being treated and the individual patient's response to the medication. Common side effects of prazosin include dizziness, lightheadedness, and low blood pressure. It is important to follow the instructions of a healthcare provider when taking prazosin and to report any side effects that occur.

Receptors, Thromboxane are a type of protein receptors found on the surface of cells in the body that bind to and respond to thromboxane, a hormone-like substance that plays a role in blood clotting and inflammation. These receptors are involved in a variety of physiological processes, including platelet aggregation, vasoconstriction, and smooth muscle contraction. In the medical field, the study of thromboxane receptors is important for understanding the pathophysiology of various diseases, including cardiovascular disease, asthma, and inflammatory disorders.

Receptors, Vasopressin are proteins found on the surface of cells in the body that bind to and respond to the hormone vasopressin. Vasopressin is produced by the hypothalamus and released by the posterior pituitary gland. It plays a role in regulating water balance in the body by constricting blood vessels and increasing the reabsorption of water in the kidneys. Vasopressin receptors are also found in other parts of the body, including the brain, heart, and blood vessels, where they can have a variety of effects, including regulating blood pressure and promoting the growth of blood vessels.

Ketanserin is a medication that belongs to a class of drugs called serotonin receptor antagonists. It is primarily used to treat high blood pressure and Raynaud's phenomenon, a condition characterized by cold, white fingers and toes. Ketanserin works by blocking the action of serotonin, a neurotransmitter that plays a role in regulating blood pressure and blood vessel constriction. It is available in both oral and intravenous forms.

2-Amino-5-phosphonovalerate (APV) is a chemical compound that is used in the medical field as a drug. It is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist, which means that it blocks the action of NMDA receptors in the brain. NMDA receptors are a type of ion channel that are involved in a variety of brain functions, including learning, memory, and mood regulation. By blocking NMDA receptors, APV can have a range of effects on the brain, including reducing seizures, improving mood, and reducing anxiety. APV is sometimes used as a treatment for conditions such as epilepsy, depression, and anxiety disorders. It is also being studied as a potential treatment for other neurological and psychiatric conditions.

In the medical field, "Disease Models, Animal" refers to the use of animals to study and understand human diseases. These models are created by introducing a disease or condition into an animal, either naturally or through experimental manipulation, in order to study its progression, symptoms, and potential treatments. Animal models are used in medical research because they allow scientists to study diseases in a controlled environment and to test potential treatments before they are tested in humans. They can also provide insights into the underlying mechanisms of a disease and help to identify new therapeutic targets. There are many different types of animal models used in medical research, including mice, rats, rabbits, dogs, and monkeys. Each type of animal has its own advantages and disadvantages, and the choice of model depends on the specific disease being studied and the research question being addressed.

The term "Receptor, Cannabinoid, CB1" refers to a specific type of protein found on the surface of certain cells in the human body. These proteins, called CB1 receptors, are activated by a class of chemicals called cannabinoids, which are found in the plant Cannabis sativa (marijuana) and in the body itself. CB1 receptors are primarily located in the brain and central nervous system, but they are also found in other parts of the body, such as the immune system, the gastrointestinal tract, and the reproductive system. When activated by cannabinoids, CB1 receptors can affect a wide range of physiological processes, including mood, pain perception, appetite, memory, and movement. In the medical field, CB1 receptors have been the subject of extensive research due to their potential therapeutic applications. For example, some studies have suggested that drugs that block CB1 receptors may be effective in treating conditions such as obesity, anxiety, and depression. On the other hand, drugs that activate CB1 receptors may be useful in treating conditions such as chronic pain, nausea, and muscle spasms. However, the use of cannabis and cannabinoid-based medications is still a controversial issue, and more research is needed to fully understand their potential benefits and risks.

Benzimidazoles are a class of organic compounds that contain a six-membered ring with two nitrogen atoms and two carbon atoms. They are widely used in the medical field as drugs and as active ingredients in pesticides. In the medical field, benzimidazoles are used to treat a variety of conditions, including: 1. Helminth infections: Benzimidazoles are effective against a range of parasitic worms, including roundworms, tapeworms, and flukes. They work by interfering with the worms' ability to absorb glucose, which leads to their death. 2. Gastric ulcers: Benzimidazoles are used to treat stomach ulcers caused by the bacteria Helicobacter pylori. They work by inhibiting the production of enzymes that break down the stomach lining, allowing the ulcers to heal. 3. Migraines: Benzimidazoles are sometimes used to prevent migraines by reducing inflammation in the brain. 4. Cancers: Some benzimidazoles are being studied as potential treatments for certain types of cancer, including colon cancer and ovarian cancer. Overall, benzimidazoles are a versatile class of compounds with a wide range of potential medical applications.

Receptors, Dopamine D2 are a type of protein found on the surface of cells in the brain and other parts of the body. These receptors are activated by the neurotransmitter dopamine, which is a chemical that helps to regulate a variety of functions in the brain, including movement, motivation, and reward. When dopamine binds to D2 receptors, it can cause a variety of effects, including reducing the activity of certain neurons and increasing the activity of others. This can lead to changes in behavior, mood, and other physiological processes. D2 receptors are also involved in the treatment of certain medical conditions, such as Parkinson's disease and schizophrenia, and are the target of many medications used to treat these conditions.

Adenosine is a naturally occurring nucleoside that plays a crucial role in various physiological processes in the human body. It is a component of the nucleic acids DNA and RNA and is also found in high concentrations in the cells of the heart, brain, and other organs. In the medical field, adenosine is often used as a medication to treat certain heart conditions, such as supraventricular tachycardia (SVT) and atrial fibrillation (AFib). Adenosine works by blocking the electrical signals that cause the heart to beat too fast or irregularly. It is typically administered as an intravenous injection and has a short duration of action, lasting only a few minutes. Adenosine is also used in research to study the function of various cells and tissues in the body, including the nervous system, immune system, and cardiovascular system. It has been shown to have a wide range of effects on cellular signaling pathways, including the regulation of gene expression, cell proliferation, and apoptosis (cell death).

Naltrexone is a medication that is used to treat alcohol and opioid addiction. It works by blocking the effects of opioids and alcohol on the brain, which can help reduce cravings and prevent relapse. Naltrexone is available in both oral and injectable forms, and it is typically prescribed as part of a comprehensive treatment plan that may also include counseling and support. It is important to note that naltrexone is not effective for everyone, and it may not be suitable for people with certain medical conditions or who are taking certain medications. It is always important to discuss the potential risks and benefits of any medication with a healthcare provider before starting treatment.

Adrenergic alpha-agonists are drugs that bind to and activate alpha-adrenergic receptors, which are a type of G protein-coupled receptor found in various tissues throughout the body. These receptors are involved in a wide range of physiological processes, including the regulation of blood pressure, heart rate, and smooth muscle contraction. When an adrenergic alpha-agonist binds to an alpha-adrenergic receptor, it causes the receptor to activate a signaling cascade that ultimately leads to the production of cyclic AMP (cAMP). This increase in cAMP can cause a variety of effects, depending on the specific tissue and receptor subtype involved. For example, in the heart, alpha-adrenergic receptor activation can increase heart rate and contractility, while in the blood vessels, it can cause vasoconstriction (narrowing of the blood vessels). Adrenergic alpha-agonists are used in a variety of medical settings, including the treatment of hypertension, heart failure, and bronchospasm (narrowing of the airways in the lungs). They are also used as part of anesthesia to help control blood pressure and heart rate during surgery. Some examples of adrenergic alpha-agonists include epinephrine, norepinephrine, and phenylephrine.

Famotidine is a medication that is used to treat conditions such as heartburn, acid reflux, and stomach ulcers. It works by blocking the production of stomach acid, which helps to reduce symptoms such as heartburn and acid reflux. Famotidine is available in both over-the-counter and prescription forms, and is typically taken by mouth. It is generally considered to be safe and effective when used as directed, but like all medications, it can cause side effects in some people. Some common side effects of famotidine include headache, dizziness, and nausea.

Receptors, Neurokinin-2 (NK2) are a type of G protein-coupled receptor found in the nervous system. They are activated by the neuropeptide substance P, which is involved in pain transmission and regulation of the immune system. Activation of NK2 receptors can lead to a variety of physiological responses, including vasodilation, increased heart rate, and bronchoconstriction. These receptors are also involved in the regulation of mood and anxiety, and have been implicated in the pathophysiology of certain neurological disorders, such as depression and schizophrenia.

Calcium is a chemical element with the symbol Ca and atomic number 20. It is a vital mineral for the human body and is essential for many bodily functions, including bone health, muscle function, nerve transmission, and blood clotting. In the medical field, calcium is often used to diagnose and treat conditions related to calcium deficiency or excess. For example, low levels of calcium in the blood (hypocalcemia) can cause muscle cramps, numbness, and tingling, while high levels (hypercalcemia) can lead to kidney stones, bone loss, and other complications. Calcium supplements are often prescribed to people who are at risk of developing calcium deficiency, such as older adults, vegetarians, and people with certain medical conditions. However, it is important to note that excessive calcium intake can also be harmful, and it is important to follow recommended dosages and consult with a healthcare provider before taking any supplements.

Bradykinin is a peptide hormone that plays a role in the regulation of blood pressure, inflammation, and pain. It is produced in the body by the breakdown of larger proteins called kinins, which are released from blood vessels and other tissues in response to injury or inflammation. Bradykinin acts on various types of cells in the body, including blood vessels, smooth muscle cells, and nerve cells, to cause a range of physiological effects. In the blood vessels, bradykinin causes them to dilate, or widen, which can lead to a drop in blood pressure. It also increases the permeability of blood vessels, allowing fluid and other substances to leak out and cause swelling. In addition to its effects on blood vessels, bradykinin is also involved in the body's inflammatory response. It stimulates the release of other inflammatory mediators, such as prostaglandins and leukotrienes, which can cause redness, swelling, and pain. Overall, bradykinin plays an important role in the body's response to injury and inflammation, and its activity is tightly regulated by various enzymes and other factors in the body.

Cannabinoid Receptor Antagonists are a class of drugs that block the effects of cannabinoids, which are naturally occurring chemicals found in the cannabis plant. These drugs work by binding to the same receptors in the brain as cannabinoids, but they prevent the cannabinoids from activating these receptors and producing their effects. Cannabinoid receptor antagonists are used in the medical field to treat a variety of conditions, including anxiety, depression, and addiction. They are also being studied for their potential use in treating other conditions, such as chronic pain, multiple sclerosis, and epilepsy. Some examples of cannabinoid receptor antagonists include rimonabant (which was withdrawn from the market due to safety concerns), nabilone, and dronabinol. These drugs are typically administered orally and can produce side effects such as nausea, insomnia, and anxiety.

Naloxone is a medication used to reverse the effects of opioid overdose. It works by binding to opioid receptors in the brain and body, blocking the effects of opioids and causing the person to breathe normally again. Naloxone is often administered as an injection, but it can also be administered nasally or intravenously. It is commonly used in emergency medical settings to treat opioid overdose, but it can also be used in non-emergency situations, such as in the management of chronic pain or opioid addiction.

Quinuclidines are a class of organic compounds that contain a quinuclidine ring, which is a six-membered ring with four nitrogen atoms and two carbon atoms. They are structurally related to the amphetamines and have been used as stimulants and nootropics. Some quinuclidines, such as pyrovalerone, have also been used as analgesics and anticonvulsants. In the medical field, quinuclidines are not commonly used and their therapeutic potential is not well established.

Benzodiazepinones are a class of psychoactive drugs that are similar in structure to benzodiazepines, but with some key differences. Like benzodiazepines, benzodiazepinones are used to treat a variety of conditions, including anxiety, insomnia, and muscle spasms. However, benzodiazepinones are generally considered to be less potent and have a shorter duration of action than benzodiazepines. Benzodiazepinones are classified as Schedule IV controlled substances in the United States, meaning that they have a low potential for abuse and dependence. However, like all psychoactive drugs, benzodiazepinones can be habit-forming and should be used only under the guidance of a healthcare professional.

Histamine is a chemical substance that is produced by certain cells in the body, including immune cells and cells in the digestive system. It plays a role in a variety of physiological processes, including the contraction of smooth muscles, the dilation of blood vessels, and the stimulation of nerve endings. In the medical field, histamine is often used as a diagnostic tool to help identify conditions such as allergies, asthma, and certain types of infections. It is also used as a treatment for certain conditions, such as allergic reactions and certain types of digestive disorders.

Adrenergic beta-2 receptor antagonists, also known as beta blockers, are a class of medications that block the action of adrenaline (epinephrine) and noradrenaline (norepinephrine) on the beta-2 receptors in the body. These receptors are found in various organs and tissues, including the heart, lungs, and blood vessels. When adrenaline and noradrenaline bind to beta-2 receptors, they cause a number of physiological responses, such as increased heart rate, blood pressure, and bronchodilation (dilation of the airways in the lungs). Beta blockers work by blocking these receptors, thereby reducing the effects of adrenaline and noradrenaline on the body. Beta blockers are commonly used to treat a variety of conditions, including high blood pressure, heart disease, and certain types of tremors. They can also be used to treat anxiety and panic disorders, as well as to prevent migraines. However, they are not suitable for everyone and should only be taken under the guidance of a healthcare professional.

Bicuculline is a chemical compound that is commonly used in the medical field as a muscle relaxant and as a tool for studying the function of the central nervous system. It is a non-competitive antagonist of the gamma-aminobutyric acid (GABA) receptor, which is a type of ion channel that is involved in the regulation of muscle tone and other functions in the brain and spinal cord. Bicuculline is typically administered intravenously or intramuscularly, and it can cause a range of effects, including muscle relaxation, sedation, and changes in heart rate and blood pressure. It is also used in research to study the role of GABA receptors in various neurological disorders, such as epilepsy and anxiety disorders. It is important to note that bicuculline can be toxic in high doses and can cause serious side effects, including respiratory depression, seizures, and coma. As such, it is typically only used under the supervision of a qualified healthcare professional.

Receptors, Nicotinic are a type of neurotransmitter receptor found in the nervous system that are activated by the neurotransmitter acetylcholine. These receptors are involved in a variety of physiological processes, including muscle contraction, heart rate regulation, and the regulation of breathing. They are also found in the brain and are thought to play a role in learning, memory, and mood regulation. In the medical field, the study of nicotinic receptors is important for understanding the effects of nicotine, which is the primary psychoactive substance in tobacco, as well as for the development of drugs for the treatment of conditions such as Alzheimer's disease and schizophrenia.

Imidazoles are a class of organic compounds that contain a five-membered heterocyclic ring with two nitrogen atoms and three carbon atoms. In the medical field, imidazoles are commonly used as antifungal agents, particularly for the treatment of dermatophytic infections such as athlete's foot, ringworm, and jock itch. They work by inhibiting the growth of fungi by interfering with their metabolism. One of the most well-known imidazole antifungal agents is clotrimazole, which is used topically to treat skin and nail infections caused by fungi. Other imidazole antifungal agents include miconazole, ketoconazole, and itraconazole, which are used to treat a variety of fungal infections, including systemic infections such as cryptococcal meningitis and aspergillosis. Imidazoles are also used in other medical applications, such as in the treatment of parasitic infections, as well as in the development of new drugs for the treatment of cancer and other diseases.

Interleukin-1alpha (IL-1α) is a type of cytokine, which is a signaling molecule that plays a crucial role in the immune system. It is produced by a variety of cells, including macrophages, monocytes, and dendritic cells, in response to infection, injury, or inflammation. IL-1α is involved in the regulation of immune responses, including the activation of T cells, B cells, and natural killer cells. It also plays a role in the production of other cytokines and chemokines, which help to recruit immune cells to the site of infection or injury. In addition to its role in the immune system, IL-1α has been implicated in a number of other physiological processes, including the regulation of bone metabolism, the control of blood pressure, and the regulation of pain perception. Abnormal levels of IL-1α have been associated with a number of medical conditions, including inflammatory diseases such as rheumatoid arthritis and psoriasis, as well as neurodegenerative diseases such as Alzheimer's and Parkinson's. As such, IL-1α is an important target for the development of new therapeutic strategies for these conditions.

Mineralocorticoid receptor antagonists (MRAs) are a class of medications that block the action of aldosterone, a hormone produced by the adrenal gland that regulates the balance of salt and water in the body. Aldosterone acts on mineralocorticoid receptors in various tissues, including the kidney, heart, and blood vessels, to increase sodium reabsorption, reduce potassium excretion, and constrict blood vessels. MRAs are primarily used to treat hypertension (high blood pressure) by reducing sodium reabsorption in the kidneys and relaxing blood vessels. They are also used to treat heart failure, as they can reduce the workload on the heart by reducing blood volume and improving blood flow to the heart muscle. Additionally, MRAs are used to treat certain types of kidney disease, such as primary aldosteronism, by reducing the production of aldosterone. Examples of MRAs include spironolactone, eplerenone, and canrenone. These medications are typically taken orally and may be used alone or in combination with other antihypertensive medications. It is important to note that MRAs can cause side effects, such as potassium depletion, fluid retention, and gynecomastia (enlargement of the breasts in men), and should be used under the guidance of a healthcare provider.

Receptors, Histamine H3 are a type of protein found on the surface of cells in the body that bind to the neurotransmitter histamine. These receptors are classified as G protein-coupled receptors (GPCRs) and are activated by histamine, which is a chemical messenger that is involved in a variety of physiological processes, including allergic reactions, sleep regulation, and the regulation of appetite and body weight. There are two main types of histamine receptors: H1 receptors and H2 receptors. H1 receptors are found on cells in the immune system, the central nervous system, and other tissues throughout the body. They are involved in the mediation of allergic reactions and the regulation of sleep. H2 receptors are found on cells in the stomach and other organs and are involved in the regulation of gastric acid secretion. H3 receptors are a relatively recently discovered type of histamine receptor. They are found on cells in the brain and other tissues throughout the body and are thought to play a role in the regulation of various physiological processes, including sleep, appetite, and body weight. However, the exact function of H3 receptors is not yet fully understood, and more research is needed to fully understand their role in the body.

Blood pressure is the force exerted by the blood against the walls of the blood vessels as the heart pumps blood through the body. It is measured in millimeters of mercury (mmHg) and is typically expressed as two numbers: systolic pressure (the pressure when the heart beats) and diastolic pressure (the pressure when the heart is at rest between beats). Normal blood pressure is considered to be below 120/80 mmHg, while high blood pressure (hypertension) is defined as a systolic pressure of 140 mmHg or higher and/or a diastolic pressure of 90 mmHg or higher. High blood pressure is a major risk factor for heart disease, stroke, and other health problems.

Yohimbine is a chemical compound that is derived from the bark of the yohimbe tree (Pausinystalia johimbe). It has been used in traditional medicine for centuries to treat various conditions, including erectile dysfunction, depression, and weight loss. In the medical field, yohimbine is primarily used as a medication to treat erectile dysfunction. It works by blocking the action of an enzyme called alpha-2 adrenergic receptors, which can cause blood vessels to constrict and reduce blood flow to the penis. By blocking these receptors, yohimbine can help to increase blood flow to the penis and improve erectile function. Yohimbine is available as a prescription medication and is typically taken orally. It can cause side effects, including headache, nausea, dizziness, and increased heart rate. It is important to note that yohimbine can interact with other medications, including antidepressants and blood pressure medications, so it should only be taken under the supervision of a healthcare provider.

Receptors, Opioid are specialized proteins found on the surface of cells in the body that bind to opioid drugs, such as morphine, heroin, and oxycodone. These receptors are part of the body's natural pain-relieving system and are involved in regulating pain, mood, and reward. When opioid drugs bind to these receptors, they can produce a range of effects, including pain relief, sedation, and euphoria. However, long-term use of opioid drugs can lead to dependence and addiction, as the body becomes accustomed to the presence of the drug and requires more of it to achieve the same effect.

... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... Adrenergic receptor Graham RM, Perez DM, Hwa J, Piascik MT (May 1996). "alpha 1-adrenergic receptor subtypes. Molecular ... alpha-1 (α1) adrenergic receptors are G protein-coupled receptors (GPCRs) associated with the Gq heterotrimeric G protein. α1- ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ...
... acts predominantly as a α2-adrenergic receptor antagonist. It has also been shown to function as a 5-HT1A receptor ... Perry BD, U'Prichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha ... 5-HT2A antagonists, 5-HT2B antagonists, Methyl esters, Heterocyclic compounds with 5 rings). ... partial agonist and 5-HT2A and 5-HT2B receptor antagonist. Ajmalicine Corynanthine Spegatrine Yohimbine KOHLI JD, DE NN (June ...
The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ... alpha-2A-, receptor". Hein, Lutz; Altman, John D.; Kobilka, Brian K. (1999). "Two functionally distinct α2-adrenergic receptors ... Handy DE, Gavras H (Nov 1992). "Promoter region of the human alpha 2A adrenergic receptor gene". The Journal of Biological ...
Antagonists L-765,314 Risperidone Brexpiprazole Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in ... The alpha-1B adrenergic receptor (α1B-adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G- ...
5-HT1A antagonists, Alpha-2 adrenergic receptor agonists, Phytocannabinoids, CB1 receptor antagonists, Resorcinols, Terpeno- ... Cannabigerol has affinity and activity at CB1 and CB2 cannabinoid receptors in vitro. It appears to be unique among cannabinoid ... Although general effects of its use as a dietary supplement remain undefined, the activity of cannabigerol at alpha-2 ... adrenergic receptors in vitro raises concerns about its safety for human consumption, possibly having unintended effects, such ...
This drug is a non-selective α-adrenergic antagonist, which means it binds to both alpha receptors. There were few if any ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... Adrenergic competitive antagonists are shorter lasting than the other two types of antagonists. While the antagonists for alpha ... There are few non-cardiovascular uses for adrenergic antagonists. Alpha-adrenergic antagonists are also used for treatment of ...
... α2-adrenergic antagonist used to reverse the sedative and analgesic effects of alpha-2 adrenergic receptor agonists benazepril ... dopamine receptor agonist used for the treatment of pituitary pars intermedia dysfunction in horses phenobarbital - anti- ... mu agonist/kappa antagonist, used as a cough suppressant and for a muscle relaxation effect in horses bedinvetmab - anti-NGF ... α2-adrenergic agonist, used to temporarily sedate animals yohimbine - used to reverse effects of xylazine, also called an " ...
... also acts as a moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist). Clonidine (also I1 ... For example, the alpha-2A adrenergic receptor subtype is post-synaptic in the prefrontal cortex and these receptors strengthen ... signal through the α2-adrenergic receptor in the central and peripheral nervous systems. The α2A adrenergic receptor is ... where it sits alongside the more plentiful α1-adrenergic receptor. The α2-adrenergic receptor binds both norepinephrine ...
... are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly used in ... Media related to Alpha-2 blockers at Wikimedia Commons v t e (Articles with short description, Short description is different ... Alpha-2 blockers increase noradrenaline release. Yohimbine, historically used as an aphrodisiac, is sometimes used in ... Chopin P, Colpaert FC, Marien M (February 1999). "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior ...
... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... Such medications include antipsychotics, antidepressants, anticonvulsants, alpha agonists and anticholinergics. It should also ... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH antagonist, but is ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ...
Antagonists A-315456 BMY 7378 (also α2C antagonist) Adrenergic receptor GRCh38: Ensembl release 89: ENSG00000171873 - Ensembl, ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ...
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... denotes selective antagonist to the receptor. compound-6FA, PAM at intracellular binding site Beta-2 adrenergic receptor has ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ... "A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance ...
... has been shown to interact with Src. Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 ... Nisoli E, Tonello C, Landi M, Carruba MO (1996). "Functional studies of the first selective β3-adrenergic receptor antagonist ... The beta-3 adrenergic receptor (β3-adrenoceptor), also known as ADRB3, is a beta-adrenergic receptor, and also denotes the ... adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic receptor Beta blocker GRCh38: Ensembl release 89: ...
... acting as a partial agonist at µ-opioid receptors and as a competitive antagonist at δ- and κ-opioid receptors. It also acts on ... December 1994). "A New Indole Alkaloid, 7 alpha-Hydroxy-7H-mitragynine, from Mitragyna speciosa in Thailand". Planta Medica. 60 ... 7-Hydroxymitragynine, like mitragynine, appears to be a mixed opioid receptor agonist/antagonist, ... 7-OH binds to opioid receptors like mitragynine, but research suggests that 7-OH binds with greater potency and contributes ...
The adrenergic receptors exert opposite physiologic effects in the vascular smooth muscle under activation: alpha-1 receptors. ... Antagonists of alpha-1 receptors (doxazosin, prazosin) cause vasodilation (a decrease in vascular smooth muscle tone with ... See also receptor antagonist) alpha-2 receptors. Agonists of alpha-2 receptors in the vascular smooth muscle lead to ... Under NE binding alpha-1 receptors cause vasoconstriction (contraction of the vascular smooth muscle cells decreasing the ...
Day HE, Campeau S, Watson SJ, Akil H (July 1997). "Distribution of alpha 1a-, alpha 1b- and alpha 1d-adrenergic receptor mRNA ... Prazosin has been said to be the only selective α1-adrenergic receptor antagonist which has been used in the treatment of ... 13-398 nM for the α2B-adrenergic receptor, and 10-200 nM for the α2C-adrenergic receptor). The α1-adrenergic receptors are ... It has much lower affinity for the α2-adrenergic receptors (Ki = 210-5,012 nM for the α2A-adrenergic receptor, ...
... is a compound which acts as an antagonist at the α1B-adrenergic receptor. It was one of the first selective antagonists ... Morrow AL, Creese I (April 1986). "Characterization of alpha 1-adrenergic receptor subtypes in rat brain: a reevaluation of [3H ... March 2000). "Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety". Pharmaceutica Acta Helvetiae ... developed for this receptor and was invented in 1969, but is still commonly used in research into adrenergic receptors, ...
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic ... ADRB-1 antagonists are a class of drugs also referred to as Beta Blockers β1-selective antagonists are used to manage abnormal ... Inhibition of receptor internalization and facilitation of beta 1-adrenergic receptor interaction with N-methyl-D-aspartate ... or one of the four adrenergic receptors. It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein ...
... barbiturates and Alpha-adrenergic agonists, such as clonidine. Conversely, coadministration of NMDA-antagonists with alpha-2 ... NMDA receptor NMDA receptor antagonist Dissociative Neurotoxic drug Nakao S, Nagata A, Masuzawa M, Miyamoto E, Yamada M, ... NMDA receptor antagonists include physician-prescribed drugs for therapeutic treatment of human diseases such as memantine for ... Olney's lesions, also known as NMDA receptor antagonist neurotoxicity (NAT), is a form of brain damage observed in rats and ...
... is a calcium channel blocker and α1-adrenergic receptor antagonist. Boer R, Grassegger A, Schudt C, Glossmann H ( ... May 1989). "(+)-Niguldipine binds with very high affinity to Ca2+ channels and to a subtype of alpha 1-adrenoceptors". European ... Alpha-1 blockers, Calcium channel blockers, Carboxylate esters, Dihydropyridines, Nitrobenzenes, All stub articles, ... 172 (2): 131-45. doi:10.1016/0922-4106(89)90004-7. PMID 2548881. v t e (Chemical articles with multiple compound IDs, Multiple ...
... including alpha-1 adrenergic receptors, at which it functions as an antagonist, and GABA-A receptors, through positive ... Adrenergic receptor modulators, Alpha-1 blockers, Benzylisoquinoline alkaloids, D1 antagonists, D2 antagonists, Dopamine ... alpha adrenergic and serotonin receptors. The Ki values for l-THP at D1 and D2 dopamine receptors are approximately 124 nM (D1 ... Along with dopamine receptors, l-THP has been reported to interact with a number of other receptor types, ...
An alpha-adrenergic antagonist with equal affinity for α1 and α2 receptors, monotherapy with phentolamine has been ... Phentolamine is an alpha blocker that relaxes blood vessel muscles, allowing more blood to flow to the penis. While the active ... 23 (2-3): 149-55. doi:10.1385/ENDO:23:2-3:149. PMID 15146094. The vasoactive potential of phentolamine was discovered in 1978, ... 153 (2): 361-5. doi:10.1097/00005392-199502000-00019. PMID 7815584. Bella AJ, Brock GB (2004). "Intracavernous pharmacotherapy ...
BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist. Goetz AS, King HK, Ward ... "BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors". European Journal of Pharmacology. 272 (2-3): R5- ...
Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused ... This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices, as ... December 2003). "Progress in pursuit of therapeutic A2A antagonists: the adenosine A2A receptor selective antagonist KW6002: ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ...
"Alpha 1 Adrenergic Receptor Antagonists", LiverTox: Clinical and Research Information on Drug-Induced Liver Injury, Bethesda ( ... inhibiting the receptor-mediated effects. The beta-1 receptor is a G-protein-coupled receptor with the Gs alpha subunit as its ... Adrenergic neurone blockers, commonly known as adrenergic antagonists, are a group of drugs that inhibit the sympathetic ... Taylor, Bryce N.; Cassagnol, Manouchkathe (2023), "Alpha Adrenergic Receptors", StatPearls, Treasure Island (FL): StatPearls ...
"Do Centrally-Acting Antihypertensive Drugs Act at Non-Adrenergic as well as Alpha-2 Adrenoceptor Sites?". Clinical and ... inactivates I2 receptors) Efaroxan (I1, α2 adrenoceptor antagonist) Idazoxan (I1, I2 antagonist, α2 adrenoceptor antagonist) ... The only known antagonist for the receptor is idazoxan, which is non-selective. The I3 receptor regulates insulin secretion ... NMDA antagonist) Cimetidine (I1 agonist, H2 receptor antagonist) Clonidine (I1 agonist, α2 adrenoceptor agonist) LNP-509 LNP- ...
It is an analog of clonidine and an agonist at the α2 class of adrenergic receptor. In veterinary anesthesia, xylazine is often ... Xylazine is a potent α2 adrenergic agonist. When xylazine and other alpha-2 adrenergic receptor agonists are administered, they ... which are physiological antagonists to central nervous system depressants. Further research is needed to accurately identify ... Alpha-2 antagonists such as atipamezole and yohimbine may be used to reverse the effects of xylazine in animals. Side-effects ...
Phenibut is a GABAB receptor agonist, as well as an antagonist at α2δ subunit-containing voltage-dependent calcium channels ( ... The alpha-1 agonist prazosin could be effective for PTSD. The alpha-2 agonists clonidine and guanfacine have demonstrated both ... Jefferson, James W. (1974). "Beta-Adrenergic Receptor Blocking Drugs in Psychiatry". Archives of General Psychiatry. 31 (5): ... Benzodiazepines bind selectively to the GABA receptor, which is the receptor protein found in the nervous system and is in ...
Prazosin has been established as an effective and safe centrally active alpha-1 adrenergic receptor antagonist. It can be used ... Alpha-1 blockers (also called alpha-adrenergic blocking agents or alpha-1 antagonists) constitute a variety of drugs that block ... Drugs that act as selective antagonists at specific alpha-1 adrenergic receptor subtypes have also been developed. Benign ... a variety of drugs have been developed from non-selective alpha-1 antagonists to selective alpha-1 antagonists and alpha-1 ...
Like other alpha-1 receptor antagonists, it has a role in the peri-operative management of pheochromocytoma. Doxazosin is ... It is a α1-selective adrenergic blocker in the quinazoline class of compounds. Doxazosin was patented in 1977 and came into ... "Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension?". Journal of Hypertension. ... Yuan J, Liu Y, Yang Z, Qin X, Yang K, Mao C (March 2013). "The efficacy and safety of alpha-1 blockers for benign prostatic ...
Prazosin is an alpha-1 adrenergic blocker that is indicated for hypertension. Studies indicate that a nighttime dose of ... Alpha-1 Receptor Antagonists. Class Summary. Novel pilot studies in combat veterans suggest alpha-1 antagonists have efficacy ... Clonidine is a central alpha-adrenergic agonist that is commonly used as an antihypertensive agent. It stimulates alpha2- ... Propranolol is a nonselective beta-adrenergic receptor blocking agent. It has been found to relieve exaggerated startle ...
Prazosin is an alpha-1 adrenergic blocker that is indicated for hypertension. Studies indicate that a nighttime dose of ... Alpha-1 Receptor Antagonists. Class Summary. Novel pilot studies in combat veterans suggest alpha-1 antagonists have efficacy ... Clonidine is a central alpha-adrenergic agonist that is commonly used as an antihypertensive agent. It stimulates alpha2- ... Propranolol is a nonselective beta-adrenergic receptor blocking agent. It has been found to relieve exaggerated startle ...
... an NMDA receptor antagonist; Imalgene, Merial, Lyon, France, 80 mg/kg, i.p.) and tranquilizer (xylazine, alpha-2 adrenergic ... McDowell, K.A.; Shin, D.; Roos, K.P.; Chesselet, M.F. Sleep dysfunction and EEG alterations in mice overexpressing alpha- ... Figure 2. Sleep-wake characterization in neonatal mice. (A) Percentage of time spent, (B) total number of epochs, and (C) epoch ... Figure 2. Sleep-wake characterization in neonatal mice. (A) Percentage of time spent, (B) total number of epochs, and (C) epoch ...
Management of opioid withdrawal includes the use of other opioids, benzodiazepines and alpha-2 adrenergic receptor antagonist, ...
Another agent that inhibits noradrenergic function is the beta-adrenergic receptor antagonist propranolol (Inderal). Because ... which affect multiple receptor systems (alpha1 , alpha2 , ACh, histamine, and the like), fluoxetine use is not associated with ... A single dose in rats produces down-regulation of beta-adrenergic receptors, suggesting the possibility of more rapid onset of ... The antipsychotics block dopamine receptors; clonidine and propranolol appear to decrease alpha- and beta-noradrenergic ...
The enhanced sensitivity to alpha-adrenergic receptor blockade following TiO2 exposure suggests an augmented responsiveness to ... an alpha-adrenergic antagonist (1 microM), reduced sympathetic constriction in controls, but abolished this response in TiO2 ... Nanoparticle inhalation modulates arteriolar sympathetic constriction: role of nitric oxide, prostanoids, and alpha-adrenergic ... Advanced Search Search Help About NIOSHTIC-2 Feedback Terms: ultrafine* OR (nano* AND particle*) OR nanotech* OR ...
Muscarinic antagonist, Not A/B H target, Adrenergic-Receptor-ligand. Chemical_Nomenclature. N-[(2-methoxyphenyl)methyl]-N-[2-[ ... alpha 2-adrenergic receptors irreversible antagonist. Antagonize several receptors, including nicotinic receptors (nAChRs), ... were noncompetitive antagonists of nicotinic receptors while being, like 1, competitive antagonists at muscarinic M(2) and M(3 ... Title: Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists. Bolognesi ML, ...
By blocking the receptors, the ingredient promotes lipolysis (fat burning). It also improves blood flow. With its improved fat ... Alpha yohimbine: It is an alpha-2 adrenergic receptor antagonist. ... No.#3: Alpha Lean 7. It is a product from Hard Rock supplements aiming at weight loss by fat burning. The makers have ... Alpha Lean 7 vs Instant Knockout vs PrimeShred: Choose the Best fat Burner!!. January 18, 2021. By Stephanie Harper Leave a ...
Reversibly binds to alpha-1 adrenergic receptors on the iris dilator muscle, thereby reducing pupil diameter ... and indirectly reverses mydriasis induced by muscarinic antagonist effects on the iris sphincter muscle ... Phentolamine directly antagonizes mydriatic effect of an alpha-1 adrenergic agonist, ... Indicated for treatment of pharmacologically-induced mydriasis produced by adrenergic agonists (eg, phenylephrine) or ...
Alpha-blockers relax muscles throughout the body. They relax the smooth muscles surrounding blood vessels and permits blood to ... Yohimbine is a potent alpha-2 adrenergic receptor antagonist. ... Dosage Recommendation 2 capsules per day at the end of eating. ...
Long-term use downregulates alpha-1 adrenergic receptors on the postsynaptic membrane-a possible final common pathway of their ... Mirtazapine is a 5-HT antagonist and blocks alpha-2 adrenergic autoreceptors, as well as 5-HT2 and 5-HT3 receptors. The result ... Agomelatine is a melatonergic (MT1/MT2) agonist and a 5-HT2C receptor antagonist that is taken at bedtime. It is used for major ... SSRIs are selective to the 5-HT system but not specific for the different 5-HT receptors. They stimulate 5-HT1 receptors, with ...
Type 2 multiple endocrine neoplasia (MEN 2) is a rare familial cancer syndrome caused by mutations in the RET proto-oncogene. ... Doxazosin mesylate is a quinazoline compound that is a selective alpha1-adrenergic antagonist. It inhibits postsynaptic alpha- ... Alpha-Adrenergic Receptor Blockers. Class Summary. At low doses, alpha-adrenergic receptor blockers may be used as monotherapy ... This is a nonselective beta-adrenergic receptor blocker. After primary treatment with an alpha-receptor blocker, propranolol ...
Alpha Adrenergic ReceptorAntagonist (2 weeks pre-op). *Phenoxybenzamine (alpha blocker) orally twice daily ... Beta Blocker (only start after alpha blockade). *Propranolol orally four times daily ... Family History of Pheochromocytoma or predisposing syndromes (e.g. MEN 2, NF1, VHL. SDH) ...
Affinity DataKi: 1.90nMAssay Description:Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO ... TargetAlpha-2C adrenergic receptor(Homo sapiens (Human)). Pfizer Inc. Curated by ChEMBL. ... TargetAlpha-2C adrenergic receptor(Homo sapiens (Human)). Pfizer Inc. Curated by ChEMBL. ... TargetAlpha-2B adrenergic receptor(Homo sapiens (Human)). Pfizer Inc. Curated by ChEMBL. ...
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... receptor antagonists, they do not cross the bloodbrain barrier and do not bind to cholinergic, serotonin, or alpha-adrenergic ... These death receptors include TNFR1, Fas (CD95). Clinical investigations in the treatment oprions meningeal leukemia: radiation ... Interestingly, although some ionotropic acetylcholine receptors are postsynaptic, a relatively large proportion, much larger ... The CAG and GGC microsatellites of the androgen receptor gene are in linkage disequilibrium in men with prostate cancer. ...
Alpha-1 Adrenergic Receptor Antagonists for Preventing Acute Respiratory Distress Syndrome and Death from Cytokine Storm ... Faculty & Research Working Papers Alpha-1 Adrenergic Receptor Antagonists for Preventing Acute Respiratory Distress Syndrome ... We previously demonstrated that alpha-1 adrenergic receptor (α1-AR) antagonists can prevent cytokine storm syndrome in mice. ... These results highlight the urgent need for prospective trials testing whether prophylactic use of α1-AR antagonists ...
... and central nervous system regulation through stimulation of alpha and beta adrenergic and dopaminergic receptors. There are ... Antagonists of DA 1 receptors are SCH23390 and clozapine. Clozapine is used for treating schizophrenia. D4. RDS. D1+D2. ... Among DA 1 receptor agonists, we can mention fenoldopam, piribedil, ibopamine, SKF 3893, and apomorphine (nonspecific). ... Activation of these receptors decreases peripheral resistance, inducing lowering of arterial blood pressure and increases in ...
The opioid receptor antagonist, naloxone (3 mg/kg), but not the alpha-2 adrenergic receptor antagonist, yohimbine (3 mg/kg), ... Risk of bias will be assessed using the Cochrane risk-of-bias tool for randomised trials (RoB 2), Risk of Bias in Non- ... Notable changes included good evidence for greater percentage change in days for PN PP MOUD use from baseline to 2 months ... METHODS: The study was carried out with 255 male convicts in 2 different closed penal execution institutions in Izmir province ...
All effects were antagonized by the alpha 1-adrenoceptor antagonist prazosin (0.1 microM), indicating receptor-mediated effects ... Existence and alpha 1-adrenergic stimulation of inositol polyphosphates in mammalian heart.. J Scholz, U Troll, P Sandig, W ... Existence and alpha 1-adrenergic stimulation of inositol polyphosphates in mammalian heart.. J Scholz, U Troll, P Sandig, W ... Existence and alpha 1-adrenergic stimulation of inositol polyphosphates in mammalian heart.. J Scholz, U Troll, P Sandig, W ...
Albumin+alpha 2a Adrenergic Receptor (1). * Albumin+COX2 / Cyclooxygenase 2+VR1+Parkin+TPO+COX1 / Cyclooxygenase 1+Rab9+CYP1A1+ ... Agonists, activators, antagonists and inhibitors. Cell lines and Lysates. Multiplex Assays. By research area. Cancer. ... DAPK2+Src+TrkA+FER+c-Kit+PAK1 + PAK2 + PAK3+PDPK1+EGFR+GSK3 beta+AMPK alpha 1+AMPK alpha 2+PIP5K1 al (1). ... Anti-alpha smooth muscle Actin (acetyl E3) + ACTG2 (acetyl E3) antibody [E184] (ab32575) Reviews (22) Specific References (532) ...
... and adrenergic antagonists, also called adrenergic blockers or sympatholytics-along with their dosages and uses. Patient Safety ... adrenergic agonists and antagonists are high-alert medications because they can cause significant harm to a patient in the ... McCuistion/pharmacology This chapter discusses two groups of drugs that affect the sympathetic nervous system-adrenergic ... There are many adrenergic receptors. The four main receptors are alpha1, alpha2, beta1, and beta2, which mediate the major ...
The FDA considers the risk for IFIS to be a class effect for alpha-1 adrenergic receptor antagonists [8,9]. The prevalence of ... alpha1-adrenergic receptor antagonists and the iris: new mechanistic insights into floppy iris syndrome. Surv Ophthalmol. 2006 ... Alpha-receptor antagonist medications potentially interfere with iris muscle dilation, resulting in difficult lens removal and ... This level of risk was subsequently confirmed and was thereafter described with all currently used alpha-1 adrenergic receptor ...
These results suggest that CEC acts on two different subtypes of prejunctional alpha-2 autoreceptors; on one of them it acts as ... and to activate a nonadrenergic inhibitory receptor thus causing a reduction of the transmitter release. ... an antagonist and increases the electrically evoked overflow of tritium (and inhibits both the effect of UK-14,304 and ... Alternatively, one can admit that CEC is able to inhibit alpha-2 autoreceptors, which causes an increase of the transmitter ...
... adrenoceptor agonist and antagonist respectively in the tail flick and hot plate tests. A significant difference in tail flick ... the present study indicates the presence and involvement of noradrenergic receptors in thermal antinociception at spinal and ... This study was designed to investigate the effects of clonidine and yohimbine, an alpha-2 (α2) ... Reid J. Alpha-adrenergic receptors and blood pressure control. Am J Cardiol. 1986;57(9):6E-12E. https://doi.org/10.1016/0002- ...
... while an antagonist of the alpha-adrenergic receptor, phentolamine, and of the beta(2)- adrenergic receptor, butoxamine, had no ... Receptors, Adrenergic, beta-3. A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The beta-3 adrenergic ... ADRENERGIC BETA-ANTAGONISTS BUTOXAMINE ADRENERGIC BETA-ANTAGONISTS CARTEOLOL ADRENERGIC BETA-ANTAGONISTS CELIPROLOL ADRENERGIC ... Antagonists of the beta-adrenergic receptor, propranolol, and the beta(1)-adrenergic receptor, metoprolol, inhibited the ...
Beta Blockers with Alpha Blocking Activity. *Carvedilol (Coreg) (see Carvedilol, [[Carvedilol]]). *Labetalol (Normodyne, ... Beta Blockers with Intrinsic Sympathomimetic Activity (β-Adrenergic Receptor Antagonism + Low Level β-Adrenergic Receptor ... β-Adrenergic Receptor Antagonists (β Blockers). Agents. Non-Selective Beta Blockers. *Carteolol ... Therefore, in pheochromocytoma, beta blockers should only be initiated after alpha blockers have been initiated ...
Histamine H1 Antagonists. Anti-Anxiety Agents. Adrenergic alpha-2 Receptor Antagonists. Serotonin 5-HT2 Receptor Antagonists. ... It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the ... It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the ... Serotonin 5-HT3 Receptor Antagonists. Registry Number. A051Q2099Q. Related Numbers. 4685R51V7M. Public MeSH Note. 2019; ...
Erb, S., Hitchcott, P.K., Rajabi, H., Mueller, D., Shaham, Y., & Stewart, J. (2000) Alpha-2 adrenergic receptor agonists block ... Blockade of stress-induced but not cocaine-induced reinstatement by infusion of noradrenergic antagonists into the bed nucleus ... 151(2-3), 152-165. [abstract] [PDF]. Altier, N. & Stewart, J. (1999) The role of dopamine in the nucleus accumbens in analgesia ... 132(2), 245-248.[abstract] [PDF]. Amir, S., Lamont, E. W., Robinson, B., & Stewart, J. (2004) A circadian rhythm in the ...
  • These agents compete with beta-adrenergic agonists for available beta-receptor sites. (medscape.com)
  • It has been widely established that dopamine and its agonists play an important role in cardiovascular, renal, hormonal, and central nervous system regulation through stimulation of alpha and beta adrenergic and dopaminergic receptors. (biopsychiatry.com)
  • From a therapeutic point of view, the above-mentioned agonists are used for treating Parkinson's disease, acting over DA 2 dopaminergic receptors of the nigrostriatal system. (biopsychiatry.com)
  • Bromocriptine and the other dopaminergic agonists mentioned act over DA 2 receptors of the tuberoinfundibular system, inhibiting prolactin release and decreasing hyperprolactinemia and tumor size. (biopsychiatry.com)
  • This chapter discusses two groups of drugs that affect the sympathetic nervous system-adrenergic agonists, or sympathomimetics , and adrenergic antagonists, also called adrenergic blockers or sympatholytics -along with their dosages and uses. (basicmedicalkey.com)
  • Intravenous (IV) adrenergic agonists and antagonists are high-alert medications because they can cause significant harm to a patient in the event of a medication error. (basicmedicalkey.com)
  • Drugs that stimulate the sympathetic nervous system are called adrenergic agonists, adrenergics, or sympathomimetics because they mimic the sympathetic neurotransmitters norepinephrine and epinephrine. (basicmedicalkey.com)
  • Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. (lookformedical.com)
  • Alpha-2 agonists often have a sedating effect and are commonly used as anesthesia enhancers in surgery, as well as in treatment of drug or alcohol dependence . (wikipedia.org)
  • At low doses, alpha-adrenergic receptor blockers may be used as monotherapy in the treatment of hypertension. (medscape.com)
  • As a result, concurrent diuretic therapy may be required to maintain the hypotensive effects of alpha-receptor blockers. (medscape.com)
  • The "intra-operative floppy iris syndrome" cataract surgery complication has been reported in men using alpha-blockers. (urotoday.com)
  • The risk of complicated cataract surgery was 14.9% in patients using alpha-blockers, approximately 50% higher than those not receiving this medication (9.5%) (p=0.003). (urotoday.com)
  • Beta blockers , which counter some of the effects of noradrenaline by blocking their receptors, are frequently used to treat glaucoma , migraine , and a range of cardiovascular problems. (wikipedia.org)
  • Alpha blockers , which counter a different set of noradrenaline effects, are used to treat several cardiovascular and psychiatric conditions. (wikipedia.org)
  • Thus, polyamines tripitramine (9) and spirotramine (33), among others, were designed, which were shown to be highly selective for muscarinic M(2) and M(1) receptors, respectively. (inrae.fr)
  • SSRIs are selective to the 5-HT system but not specific for the different 5-HT receptors. (msdmanuals.com)
  • Doxazosin mesylate is a quinazoline compound that is a selective alpha1-adrenergic antagonist. (medscape.com)
  • A beta-2 selective adrenergic antagonist. (lookformedical.com)
  • The beta 2 receptors are found mostly in the smooth muscles of the lung and GI tract, the liver, and the uterine muscle. (basicmedicalkey.com)
  • FIG. 15.1 Effects of activation of alpha 1 , alpha 2 , beta 1 , and beta 2 receptors. (basicmedicalkey.com)
  • Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS. (lookformedical.com)
  • The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. (lookformedical.com)
  • This study was designed to investigate the effects of clonidine and yohimbine, an alpha-2 ( α 2 ) adrenoceptor agonist and antagonist respectively in the tail flick and hot plate tests. (biomedcentral.com)
  • The aim of the experiment was to study the role of the noradrenergic receptor system in the NMRs using the receptor agonist clonidine and antagonist yohimbine in the tail flick and hot plate tests, in order to establish whether NMR can be used as animal model for noradrenergic mechanisms in thermal antinociception. (biomedcentral.com)
  • Propranolol is a nonselective beta-adrenergic receptor blocking agent. (medscape.com)
  • This is a nonselective alpha-adrenergic blocking agent. (medscape.com)
  • This is a nonselective beta-adrenergic receptor blocker. (medscape.com)
  • Management of opioid withdrawal includes the use of other opioids, benzodiazepines and alpha-2 adrenergic receptor antagonist, clonidine. (nih.gov)
  • Phentolamine, an alpha-adrenergic antagonist (1 microM), reduced sympathetic constriction in controls, but abolished this response in TiO2 exposed rats (max % change -22.3+/-3.1 control, -9.7+/-2.9 TiO2). (cdc.gov)
  • Twenty four hours following exposure, the spinotrapezius muscle was prepared for intravital microscopy and sympathetic nerve stimulation (2, 4, 8, and 16 Hz) was performed. (cdc.gov)
  • It may be used to treat excessive beta-receptor stimulation in patients with inoperable metastatic pheochromocytoma. (medscape.com)
  • Existence and alpha 1-adrenergic stimulation of inositol polyphosphates in mammalian heart. (aspetjournals.org)
  • 1,4,5-IP3 (significant at 10 microM) and both IP4 isomers (significant at 1 microM) increased after alpha-adrenoceptor stimulation, whereas 1,3,4,5,6-IP5 and IP6 remained unaffected. (aspetjournals.org)
  • Increased inositol polyphosphate turnover may be involved in the mechanism(s) whereby alpha 1-adrenoceptor stimulation produces an increase in myocardial force of contraction. (aspetjournals.org)
  • Stimulation of the beta 1 receptors increases myocardial contractility and heart rate. (basicmedicalkey.com)
  • Results from using an in vitro tissue bath technique indicated that propranolol and preferential beta(2)-adrenoceptor antagonists (ICI-118,551 and butoxamine), in a concentration-dependent manner, blocked the relaxation induced by nicotine (100 microM) without affecting the relaxation elicited by transmural nerve stimulation (TNS, 8 Hz). (lookformedical.com)
  • After primary treatment with an alpha-receptor blocker, propranolol hydrochloride may be used as adjunctive therapy if control of tachycardia becomes necessary before or during surgery. (medscape.com)
  • The enhanced sensitivity to alpha-adrenergic receptor blockade following TiO2 exposure suggests an augmented responsiveness to tonic sympathetic activity. (cdc.gov)
  • Its drug action is transient and alpha-adrenergic blockade incomplete. (medscape.com)
  • Leri, F., Flores, J., Rodaros, D., & Stewart, J. (2002) Blockade of stress-induced but not cocaine-induced reinstatement by infusion of noradrenergic antagonists into the bed nucleus of the stria terminalis or the central nucleus of the amygdala. (concordia.ca)
  • Research has shown that it's mechanisms of action are similar to yohimbine, as it can act as an alpha(2) adrenergic antagonist, thus aiding in fat burning. (anybodysupplements.com)
  • By preventing reuptake of 5-HT presynaptically, SSRIs result in more 5-HT to stimulate postsynaptic 5-HT receptors. (msdmanuals.com)
  • It inhibits postsynaptic alpha-adrenergic receptors, resulting in the vasodilation of veins and arterioles and a decrease in total peripheral resistance and blood pressure. (medscape.com)
  • All effects were antagonized by the alpha 1-adrenoceptor antagonist prazosin (0.1 microM), indicating receptor-mediated effects. (aspetjournals.org)
  • Presynaptic beta(2)-adrenoceptors mediate nicotine-induced NOergic neurogenic dilation in porcine basilar arteries. (lookformedical.com)
  • A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS . (nih.gov)
  • structure to achieve specific recognition of muscarinic receptors that led to the discovery of methoctramine (2). (inrae.fr)
  • which is widely used as a pharmacological tool for muscarinic receptor characterization. (inrae.fr)
  • In turn, appropriate structural modifications performed on the structure of methoctramine led to the discovery of new polyamines endowed with high affinity and selectivity for (a). muscarinic receptor subtypes, (b). (inrae.fr)
  • Finally, the universal template approach formed the basis for modifying benextramine (1) structure to the design of ligands, which display affinity for acetylcholinesterase and muscarinic M(2) receptors. (inrae.fr)
  • It is an alpha1- and alpha2-adrenergic blocking agent that blocks circulating epinephrine and norepinephrine action, reducing hypertension that results from catecholamine effects on alpha receptors. (medscape.com)
  • [2] "Norepinephrine" is also the international nonproprietary name given to the drug . (wikipedia.org)
  • Regardless of how and where it is released, norepinephrine acts on target cells by binding to and activating adrenergic receptors located on the cell surface. (wikipedia.org)
  • Other adrenergic receptors are dopaminergic and are located in the renal, mesenteric, coronary, and cerebral arteries. (basicmedicalkey.com)
  • Since the tail-flick and hot plate tests mediate the effects at spinal and supraspinal levels respectively, the present study indicates the presence and involvement of noradrenergic receptors in thermal antinociception at spinal and supraspinal levels of the NMR, similar to what has been found in other mammals. (biomedcentral.com)
  • To our knowledge, the involvement of the noradrenergic receptor system in antinociception against thermal stimuli has not been previously studied in the NMR. (biomedcentral.com)
  • Unlike first-generation H1- receptor antagonists, they do not cross the bloodbrain barrier and do not bind to cholinergic, serotonin, or alpha-adrenergic re- ceptors.Dell, A. (forextrading-madeeasy.com)
  • It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. (nih.gov)
  • Nanoparticle inhalation modulates arteriolar sympathetic constriction: role of nitric oxide, prostanoids, and alpha-adrenergic receptors. (cdc.gov)
  • Antagonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilizatio. (bindingdb.org)
  • Antagonist activity at human recombinant adrenergic alpha2B receptor expressed in CHO cells assessed as inhibition of NE-induced calcium mobilization. (bindingdb.org)
  • Only dopamine can activate these receptors. (basicmedicalkey.com)
  • Alternatively, one can admit that CEC is able to inhibit alpha-2 autoreceptors, which causes an increase of the transmitter release, and to activate a nonadrenergic inhibitory receptor thus causing a reduction of the transmitter release. (unesp.br)
  • Drugs that selectively bind to and activate beta-adrenergic receptors. (lookformedical.com)
  • Alpha-blocker medications are the first line of therapy for men with these urinary symptoms. (urotoday.com)
  • If possible, alpha blocker medications should be discontinued prior to eye surgery in older patients. (urotoday.com)
  • As alpha-blocker medications are the first line of therapy for men with LUTS, these reports of IFIS led the Food and Drug Administration, American Urological Association, American Academy of Ophthalmology, and American Society of Cataract and Refractive Surgery to issue statements alerting physicians and patients to potential difficulties during cataract surgery in patients using alpha-1 blocker therapy [7,8,9]. (urotoday.com)
  • Alpha-receptor antagonist medications potentially interfere with iris muscle dilation, resulting in difficult lens removal and possibly increasing complications. (urotoday.com)
  • INT RODUCTIO N: Th e eld erly h ypert en si ve pa ti ent s of ten h aveincreased prevalence of cardiometabolic risk factors and their attendantco-morbidities. (bvsalud.org)
  • Preoperatively, prepare patients with pheochromocytomas by treating them with an alpha-blocker or a tyrosine hydroxylase inhibitor, such as metyrosine, for 1-2 weeks, after which administration of a beta-blocker can be considered. (medscape.com)
  • This is a long-acting adrenergic alpha-receptor blocker that can produce and maintain a chemical sympathectomy. (medscape.com)
  • To assess the frequency of cataract surgery complications arising from alpha-blocker therapy in a large patient population. (urotoday.com)
  • The purpose of this study was to assess the impact of alpha-blocker therapy on complications during cataract surgery in a large patient population. (urotoday.com)
  • Activation of these receptors decreases peripheral resistance, inducing lowering of arterial blood pressure and increases in heart rate, sympathetic tone, and activity of the renin aldosterone system. (biopsychiatry.com)
  • The alpha 2 receptors are located in the postganglionic sympathetic nerve endings. (basicmedicalkey.com)
  • They stimulate 5-HT 1 receptors, with antidepressant and anxiolytic effects, but they also stimulate 5-HT 2 receptors, commonly causing anxiety, insomnia, and sexual dysfunction, and 5-HT 3 receptors, commonly causing nausea and headache. (msdmanuals.com)
  • For reasons that are still unclear, some Alpha-2 drugs, such as guanfacine , have also been shown to be effective in the treatment of anxiety disorders and ADHD . (wikipedia.org)
  • It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. (lookformedical.com)
  • Sulfonylureas are generally ef- fective, safe, and inexpensive (generically available) drugs and, along with metformin, are mainstays of treatment for type 2 diabetes. (forextrading-madeeasy.com)
  • The increase in the force of contraction started at 2 min. (aspetjournals.org)
  • The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS. (lookformedical.com)
  • The beta 1 receptors are located primarily in the heart but are also found in the kidney. (basicmedicalkey.com)
  • It is used primarily in animal and tissue experiments to characterize BETA-2 ANDRENERGIC RECEPTORS. (lookformedical.com)
  • When these receptors are stimulated, the vessels dilate and blood flow increases. (basicmedicalkey.com)
  • A study published in 2005 described a new clinical entity, the "intra-operative floppy iris syndrome" (IFIS), and suggested that this syndrome was associated with tamsulosin, a drug used widely for the treatment of lower urinary tract symptoms (LUTS) due to benign prostate enlargement [2]. (urotoday.com)
  • A widely used non-cardioselective beta-adrenergic antagonist. (lookformedical.com)
  • These results highlight the urgent need for prospective trials testing whether prophylactic use of α1-AR antagonists ameliorates diseases associated with cytokine storm syndrome, such as COVID-19. (stanford.edu)
  • Due to these unique characteristics, researchers have been bio prospecting NMRs as research animal models for nociception with the aim to further understand mechanisms involved in various biological diseases affecting humans [ 2 , 3 , 5 ]. (biomedcentral.com)
  • Transmitters are inactivated by (1) reuptake of the transmitter back into the neuron (nerve cell terminal), (2) enzymatic transformation or degradation, and (3) diffusion away from the receptor. (basicmedicalkey.com)
  • Results of double-labeling studies indicated that beta(2)-adrenoceptor immunoreactivities and NADPH diaphorase reactivities were colocalized in the same nerve fibers in basilar and middle cerebral arteries. (lookformedical.com)
  • Moreover, the patient must have psychosis for at least 2 weeks without a mood disorder. (medscape.com)
  • The alpha-adrenergic receptors are located in the blood vessels, eyes, bladder, and prostate. (basicmedicalkey.com)
  • In contrast, preferential beta(1)-adrenoceptor antagonists (atenolol and CGP-20712A) did not affect either nicotine- or TNS-induced relaxation. (lookformedical.com)
  • The four main receptors are alpha 1 , alpha 2 , beta 1 , and beta 2 , which mediate the major responses described in Table 15.1 and illustrated in Fig. 15.1 . (basicmedicalkey.com)
  • They act on one or more adrenergic receptor sites located in the effector cells of muscles such as the heart, bronchiole walls, gastrointestinal (GI) tract, urinary bladder, and ciliary muscles of the eye. (basicmedicalkey.com)
  • We previously demonstrated that alpha-1 adrenergic receptor (α1-AR) antagonists can prevent cytokine storm syndrome in mice. (stanford.edu)
  • As a matter of fact, the insertion of different pharmacophores onto the polymethylene tetraamine backbone can tune both affinity and selectivity for any given receptor. (inrae.fr)
  • The FDA considers the risk for IFIS to be a class effect for alpha-1 adrenergic receptor antagonists [8,9]. (urotoday.com)
  • The present study was undertaken to look for the effect of chloroethylclonidine (CEC) on prejunctional alpha-2 autoreceptors of the canine saphenous vein. (unesp.br)
  • Risk of bias will be assessed using the Cochrane risk-of-bias tool for randomised trials (RoB 2), Risk of Bias in Non-randomised Studies of Interventions (ROBINS-I), and The Joanna Briggs Institute Critical Appraisal Checklist for Quasi-Experimental Studies and The Joanna Briggs Institute Critical Appraisal Checklist for Qualitative Research (CASP), depending on the study type. (bvsalud.org)
  • G(i) proteins, and (c). muscle-type nicotinic receptors. (inrae.fr)
  • The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS. (lookformedical.com)
  • Rauwolscine (1mg) Rauwolscine is an alpha-receptor antagonist that can block the action of receptors responsible for stopping fat breakdown. (anybodysupplements.com)
  • Federated across two ARD cohorts, our main result shows that patients using α1-AR antagonists, as compared to nonusers, had a 40% relative risk reduction for ventilation and dying (p=0.014). (stanford.edu)