Wakefulness-Promoting Agents: 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.Receptors, Adrenergic, alpha-2: 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.Interleukin 1 Receptor Antagonist Protein: 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.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Rats, Sprague-Dawley: 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.Histamine H2 Antagonists: 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.Serotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.Piperidines: A family of hexahydropyridines.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.Dopamine Antagonists: 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.Serotonin 5-HT2 Receptor Antagonists: 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.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Hormone Antagonists: 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.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Histamine H1 Antagonists: 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.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.Muscarinic Antagonists: 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.GABA-A Receptor Antagonists: Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.Sialoglycoproteins: 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.Histamine Antagonists: 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.Receptors, Adrenergic, alpha: 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.alpha 1-Antitrypsin: Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.Leukotriene Antagonists: A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.Receptor, Endothelin A: A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.Receptors, Serotonin: 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.Receptors, N-Methyl-D-Aspartate: 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.Serotonin 5-HT1 Receptor Antagonists: 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.Nicotinic Antagonists: 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.Dizocilpine Maleate: 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.Receptors, Interleukin-1: 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.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Adrenergic alpha-Antagonists: 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 CompoundsBenzazepines: Compounds with BENZENE fused to AZEPINES.TetrazolesRadioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Xanthines: Purine bases found in body tissues and fluids and in some plants.Guinea Pigs: 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.Serotonin Receptor Agonists: 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, Cyclic: 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).Sulfonamides: A group of compounds that contain the structure SO2NH2.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Indoles: 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.Histamine H3 Antagonists: Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.Binding, Competitive: 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.Pyrazoles: 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: 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.QuinoxalinesCells, Cultured: 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.Azepines: Seven membered heterocyclic rings containing a NITROGEN atom.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.Endothelin-1: 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)GABA-B Receptor Antagonists: Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.Substance P: 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.alpha7 Nicotinic Acetylcholine Receptor: 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.Serotonin: 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.Receptors, Bradykinin: 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.Signal Transduction: 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.Neurons: 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.Cimetidine: 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.Receptors, Neurokinin-1: 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.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.Receptor, Endothelin B: A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.Purinergic P2X Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.PiperazinesBehavior, Animal: The observable response an animal makes to any situation.PyrrolidinesReceptors, Adrenergic, alpha-1: 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.Interleukin-1: 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.Receptors, Cholecystokinin: 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.Devazepide: 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.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.Receptors, Thromboxane: 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.Receptors, Vasopressin: 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.Ketanserin: 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.2-Amino-5-phosphonovalerate: 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.Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Disease Models, Animal: 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.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Benzimidazoles: Compounds with a BENZENE fused to IMIDAZOLES.Mice, Inbred C57BLReceptors, Dopamine D2: 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.Adenosine: 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.Naltrexone: 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, Intraventricular: Injections into the cerebral ventricles.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Famotidine: A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.Receptors, Neurokinin-2: 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.Calcium: 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.Bradykinin: 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.Cannabinoid Receptor Antagonists: Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.QuinuclidinesBenzodiazepinonesHistamine: 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.Adrenergic beta-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.Receptors, Nicotinic: 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.Imidazoles: 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).Interleukin-1alpha: 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.Mineralocorticoid Receptor Antagonists: Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.Receptors, Histamine H3: 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)Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.Receptors, Opioid: 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)

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As described in the accompanying paper, the novel ligand S18327 (1-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperid-1-yl]ethyl}3-phenyl imidazolin-2-one) displays pronounced antagonist properties at α1-adrenergic receptors (ARs), serotonin [5-hydroxytryptamine (5-HT)2A], and D4 receptors, as well as less potent antagonist actions at α2-AR and D1and D2 receptors. Interestingly, the α2-AR antagonist properties of S18327 underlie a generalized enhancement of cerebral adrenergic transmission and a preferential facilitation of the activity of frontocortical compared with subcortical dopaminergic pathways. On the other hand, the inhibitory influence of S18327 on the activity of serotonergic neurons originating in the dorsal raphe nucleus may be attributed to its antagonist actions at α1-ARs. Notably, S18327 only weakly accelerates striatal turnover of dopamine (DA). In light of these observations, in the present study we examined the activity of S18327 in paradigms predictive of the control of ...
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Yohimbine Hydrochloride Alias: Corynine;Aphrodine CAS No: 65-19-0 Einecs No: 200-600-4 MF: C21H27ClN2O3 MW: 390.91 Purity: 98% Appearance:White crystalline
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Yohimbine HCL Synonyms: Yohimbin, Corynine, Quebrachin, Quebrachine, Aphrosol, Yohimex, Yohimbe HCL (commonly confused with)What is Yohimbine HCL Powder?Yohimbine is an alkaloid found in Yohimbe, a tall evergreen bark native to Africa. Yohimbine has some exciting possibilities, such as promoting and enhancing erectile function. However, many users primarily take Yohimbine as a fat loss aid.Yohimbine Powder BenefitsYohimbine directly aids weight loss. There are two types of adrenergic receptors, alpha and beta, and depending on which are activated, lipolysis (breakdown of fat) can be either stimulated or inhibited. Activation of the alpha 2 receptors inhibits the release of norepinephrine. This is not good if you are trying to reduce weight. Because alpha 2 receptors activate at lower catecholamine levels than the beta receptors, thermogenesis is basically always turned off. Even during exercise, alpha 2 receptors are still acting to inhibit lipolysis. This is where Yohimbine comes into play. Yohimbine
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Four 2-amino-3-methylimidazo[4,5-b][1,x]naphthyridines, x = 5-8 (6-9) have been obtained from aromatic aldehydes (11-14) and 2-amino-1-methyl-2-imidazolin-5-one (15) in one step. The N-1 - and N-3 -methyl isomers of 2-aminoimidazo-[4,5-b]quinoline (5 and 10) were prepared from 2-nitrobenzaldehyde via the isolated E-isomers of imidazolin-5-one (17) and imidazolin-4-one (20).. ...
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Based on the studies we have examined, I recommend working up to 0.2mg/Kg of bodyweight. So that means a 220lb bodybuilder (divide by 2.2 to get Kg) is 100Kg and would work up to a dose of 20mg of Yohimbine HCl, or eight capsules of MTS Nutrition Yohimbine HCl. I would typically start this person at one capsule and work up towards the full dose each consecutive session the person had no undesirable side effects. As I was discussing with Joe Daniels of Swing This Kettlebells, Yohimbine HCls effects work the best in the absence of insulin, and its effects start to diminish the more insulin is present. But this doesnt mean that you cannot eat carbs! Insulin will usually be under control on a lower carb diet, like most trainers will put you on. Obviously, cardio first thing in the morning is a good time (with a scoop of MTS Nutrition Whey in your belly) and even post workout. What you can do is take the Yohimbine HCl DURING your weight training workout 15-20 minutes before you are done. Then, hop ...
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Introduction CypHer ™ 5 a pH sensitive dye has shown utility in β2-adrenergic receptor agonist screening (1). CypHer5 has been used to obtain dose-response and rank-order potency data for both agonist and antagonist treatment of β2-adrenergic receptor expressing cells (2). For live-cell receptor internalization studies a,Screening,for,potential,beta,2-adrenergic,receptor,antagonists,using,CypHer5E,and,IN,Cell,Analyzer,1000,biological,advanced biology technology,biology laboratory technology,biology device technology,latest biology technology
Idazoxan (INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor.[1][2] Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia. ...
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This paper present ultraviolet-visible absorption spectra of imazamethabenz-methyl (IMBM) (mixture of the isomers methyl 6-[(RS)-4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl]-m-toluate, m-imazamethabenz, and methyl 2-[(RS)-4-isopropyl-4-methyl-5-oxo-2-imidazolin-2-yl]-p-toluate, p-imazamethabenz) and the corresponding carboxylic acid, imazamethabenz-acid (IMBA). The spectral characteristics are determined as functions of the pH. The appreciable absorbance in the visible (or near-ultraviolet) region of the spectra indicates ...
The IUPHAR/BPS Guide to Pharmacology. yohimbine ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
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This review evaluates the role of α-adrenoceptor antagonists as a potential treatment of prostate cancer (PCa). Cochrane, Google Scholar and Pubmed were accessed to retrieve sixty-two articles for analysis. In vitro studies demonstrate that doxazosin, prazosin and terazosin (quinazoline α-antagonists) induce apoptosis, decrease cell growth, and proliferation in PC-3, LNCaP and DU-145 cell lines. Similarly, the piperazine based naftopidil induced cell cycle arrest and death in LNCaP-E9 cell lines. In contrast, sulphonamide based tamsulosin did not exhibit these effects. In vivo data was consistent with in vitro findings as the quinazoline based α-antagonists prevented angiogenesis and decreased tumour mass in mice models of PCa. Mechanistically the cytotoxic and antitumor effects of the α-antagonists appear largely independent of α 1-blockade. The proposed targets include: VEGF, EGFR, HER2/Neu, caspase 8/3, topoisomerase 1 and other mitochondrial apoptotic inducing factors. These cytotoxic effects
Patane MA, Scott AL, Broten TP, Chang RS, Ransom RW, DiSalvo J, Forray C, Bock MG (1998). „4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist ". Journal of Medicinal Chemistry. 41 (8): 1205-8. PMID 9548811. doi:10.1021/jm980053f ...
Idazoxan hydrochloride,2-(1,4-Benzodioxan-2-yl)-2-imidazolinehydrochloride 79944-56-2 NMR spectrum, Idazoxan hydrochloride,2-(1,4-Benzodioxan-2-yl)-2-imidazolinehydrochloride H-NMR spectral analysis, Idazoxan hydrochloride,2-(1,4-Benzodioxan-2-yl)-2-imidazolinehydrochloride C-NMR spectral analysis ect.
Abanoquil: lt;p|> |||Abanoquil| (|INN|) is an |α1-adrenergic receptor| |antagonist|.|||[|1|]||| | ||See also... World Heritage Encyclopedia, the aggregation of the largest online encyclopedias available, and the most definitive collection ever assembled.
Yohimbine is an extract from the bark of the yohimbe tree that grows in the Southern African region. Yohimbine HCL (hydrochloride) is the main active...
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Save 38% Allmax Nutrition - Yohimbine + Rauwolscine 60 Capsules Yohimbe + Rauwolscine 3.5 mg a2 Adrenoreceptor Antagonist Supports Fat-Burning* Suppresses Appetite* Supports Sexual Performance* Pharmaceutical Grade Allmax Yohimbine + Rauwolscine (Alpha-Yohimbine) are the pure synthetic versions of Pausinystalia Yohimbe and Rauwolfia serpentina; thousands of times more powerful than the original herbal extracts from which they were isolated.* Most frequently used for rapid fat loss due to its targeted ability to act on stored fat. Yohimbine + Rauwolscine effectively shuts down fat storage and increases lipolysis, the release of fatty acids within stored fat.* Why Does It Work So Well? Yohimbine has an extremely high affinity for the a2-adrenoreceptor (a2-AR). These receptors (primarily in fat cells) control the rate of release of stored fat. As antagonists, Yohimbine & Rauwolscine lock on to a2 fat cell receptors. Fat storage is deactivated and rapid release of stored fat is initiated.* Rauwolscine (or
This review evaluates the role of α-adrenoceptor antagonists as a potential treatment of prostate cancer (PCa). Cochrane, Google Scholar and Pubmed were accessed to retrieve sixty-two articles for analysis. In vitro studies demonstrate that doxazosin, prazosin and terazosin (quinazoline α-antagonists) induce apoptosis, decrease cell growth, and proliferation in PC-3, LNCaP and DU-145 cell lines. Similarly, the piperazine based naftopidil induced cell cycle arrest and death in LNCaP-E9 cell lines. In contrast, sulphonamide based tamsulosin did not exhibit these effects. In vivo data was consistent with in vitro findings as the quinazoline based α-antagonists prevented angiogenesis and decreased tumour mass in mice models of PCa. Mechanistically the cytotoxic and antitumor effects of the α-antagonists appear largely independent of α 1-blockade. The proposed targets include: VEGF, EGFR, HER2/Neu, caspase 8/3, topoisomerase 1 and other mitochondrial apoptotic inducing factors. These cytotoxic effects
Transdermal neuromodulation of noradrenergic activity suppresses psychophysiological and biochemical stress responses in humans. Tyler, W.J., A. Boasso, H.M. Mortimore, R.S. Silva, J.D. Charlesworth, M.A. Marlin, K.A. Aebersold, L. Aven, D.Z. Wetmore, and S.K. Pal (2015). Scientific Reports 5, 13865, 1-17. PMID: 26353920. Is sham cTBS real cTBS? The effect on EEG dynamics. Opitz, A., W. Legon, J. Mueller, A. Barbour, W. Paulus, and W.J. Tyler (2015). Frontiers in Human Neuroscience 8, 1043. PMID: 25620925. Transcranial focused ultrasound modulates intrinsic and evoked EEG dynamics. Mueller, J., W. Legon, A. Opitz, T.F. Sato, W.J. Tyler (2014). Brain Stimulation 7(6), 900-908. PMID: 25265863. A quantitative overview of biophysical forces impinging on neural function. Mueller, J. and W.J. Tyler (2014). Physical Biology 11(5), 1-15. PMID: 25156965. Transcranial focused ultrasound modulates the activity of primary somatosensory cortex in humans. Legon, W., T.F. Sato, A. Opitz, J. Mueller, A. ...
Script error: No such module TemplatePar.Expression error: Unexpected , operator. Naftopidil (INN, marketed under the brand name Flivas) is an antihypertensive drug which acts as a selective α1-adrenergic receptor antagonist or alpha blocker. ...
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To test the hypothesis that alpha-2 adrenoceptor antagonists can modulate sympathetic nerve release of norepinephrine in vivo through blockade of peripheral prejunctional alpha-2 adrenoceptors, acute and chronic effects of the alpha-2 adrenoceptor antagonist idazoxan on mean arterial pressure (MAP), heart rate and plasma catecholamine concentrations have been investigated in conscious and anesthetized rats. In normotensive rats, a single i.v. dose of idazoxan (300 micrograms kg-1) caused an immediate 2-fold increase in plasma concentration of norepinephrine and epinephrine, a transient increase in heart rate but no significant change in MAP. Plasma norepinephrine concentration of conscious normotensive rats increased significantly during a 4-hr i.v. infusion of idazoxan (300 micrograms kg-1 hr-1) with no concomitant changes in MAP or heart rate. In anesthetized spontaneously hypertensive rats, the increases in plasma norepinephrine concentration and heart rate caused by i.v. idazoxan (300 ...
Macrophages play an integral role in eliminating infection during the inflammatory response. Catecholamines are known to alter macrophage function by binding to adrenergic receptors on the macrophage membrane. Stimulation through β-adrenergic receptors (β-AR) is known to decrease macrophage function while stimulation through the α-adrenergic receptor (α-AR) is thought to have a stimulatory effect on immune function. The RAW264.7 murine macrophage cell line is used as a model of macrophage function, but little is known about the expression of adrenergic receptors on these cells. In these studies, macrophages were treated with the catecholamine norepinephrine, the non-selective α-adrenergic receptor agonist clonidine, or the selective α2-adrenergic receptor antagonist RS79948 (RS), prior to lipopolysaccharide (LPS) activation, and then analyzed for the production of the proinflammatory cytokines TNF-α and IL-6. Low concentrations of clonidine increased cytokine production while RS reversed these
Looking for a-adrenergic antagonist? Find out information about a-adrenergic antagonist. 1. any muscle that opposes the action of another 2. a drug that counteracts the effects of another drug A molecule that bears sufficient structural... Explanation of a-adrenergic antagonist
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Unit 20 Sales Planning and Operations Qualification: Pearson BTEC Level 5 HND Diploma Business (Management) Unit Number and Title Unit 20: Sales Planning and Operations Assignment Brief Assessment ...
Central Ohios Only Jewish Jfcicspaper Headline Every Borne A WEEKLY NEWSPAPER FOR THE JEWISH HOME Devoted to American and Jevfish IdeaU ¦••••»«••¦•"••••• Pn»M«-««*ii"t-l, 4 Vohimc XVII-No. 216 C0LUMI5U.S, OHIO, ]FIJKLARY 11, W.I.S IlT Yoar .?.?.00; Per Copy 10c il 11^ ¦ ! Strictly Confidential Tidbits From Everywhere By rillNEAS i. BIRON JEWISH AFEAIKS Irivftte conferences aro Roinp on among the most imiiortant national ilcwinh or^anization,; with a view to forminj! a hort u£ Board of .Iew¬ ish Dciiuties, rcpic3entin(5 all these organiitations, which would bo the only authoritative American Jewish body for tlic defcnso of Jewish rights . . . Maurico Jacobs, whuso ivorlt ns executive secretary put tho Jewish Public.ition Society bn the map, discovered to hia amazement thnt a New York col¬ umnist reported that tlie Societys prize-winning Jewish novel, "To¬ morrows Bread," wus being issued by "another publijihing house after it hnd been refused ...
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Perry BD, U'Prichard DC (1981). „[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2- ... adrenergic receptors". European Journal of Pharmacology. 76 (4): 461-4. PMID 6276200. doi:10.1016/0014-2999(81)90123-0.. ... Rauvolscin deluje predominantno kao antagonist α2-adrenergičnog receptora.[2] On takođe deluje kao parcijalni agonist 5-HT1A ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (1998). „[3H]Rauwolscine: an antagonist radioligand for the ...
... 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 ... partial agonist and 5-HT2A and 5-HT2B receptor antagonist. Ajmalicine Corynanthine Spegatrine Yohimbine KOHLI JD, DE NN (June ... Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). "[3H]Rauwolscine: an antagonist radioligand ...
In medical settings, NMDA receptor antagonists are used as anesthetics, so GABAA receptor positive allosteric modulators are ... Conversely, coadministration of NMDA-antagonists with alpha-2 adrenergic antagonists, like yohimbine could theoretically ... Jansen writes: Neuroscience portal NMDA receptor NMDA receptor antagonist Dissociative Neurotoxic drug Olney J, Labruyere J, ... Olney's lesions, also known as NMDA receptor antagonist neurotoxicity (NAN), are a potential form of brain damage. They are ...
... 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 ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ... 66 (2): 283-286. ISSN 1534-7796. PMID 15039516. (subscription required) Lee, H. S.; Kwon, K. Y.; Alphs, L. D.; Meltzer, H. Y. ( ...
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ... This gene encodes alpha-1D-adrenergic receptor. Similar to alpha-1B-adrenergic receptor gene, this gene comprises 2 exons and a ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ...
... α2-adrenergic antagonist used to reverse the sedative and analgesic effects of alpha-2 adrenergic receptor agonists benazepril ... Crosses blood-brain barrier, useful in treatment of meningitis cimetidine - H2 antagonist used to reduce GI acid production ... mu agonist/kappa antagonist, used as a cough suppressant and for a muscle relaxation effect in horses carprofen - COX-2 ... α2-adrenergic agonist (used to temporarily sedate animals) yohimbine - used to reverse effects of xylazine, also called an " ...
... an alpha-adrenergic receptor blocker, had a higher incidence of heart failure events, and the doxazosin arm of the study was ... Angiotensin II receptor antagonists work by antagonizing the activation of angiotensin receptors. ... Central alpha agonists lower blood pressure by stimulating alpha-receptors in the brain which open peripheral arteries easing ... On the other hand, β-blockers, diuretics, ACE inhibitors, angiotensin receptor blockers, and aldosterone receptor antagonists ...
... and D3 receptors. It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and D2, and as a ... February 2000). "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, ... Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5- ... Yohimbine blocks the pre- and post-synaptic α2 receptors. Blockade of post-synaptic α2 receptors causes only minor corpus ...
... ketanserin such as ritanserin are more selective 5-HT2A receptor antagonists with low affinity for alpha-adrenergic receptors. ... Silent antagonistsEdit. *Trazodone is a potent 5-HT2A antagonist, as well as an antagonist on other serotonin receptors. ... but through its high affinity for alpha1 adrenergic receptors. It also has high affinity for H1 histaminergic receptors equal ... G-protein coupled receptor activity. • virus receptor activity. • signal transducer activity. • drug binding. • G-protein alpha ...
... presumptively also mediated by α2 adrenergic receptors because it is reversed by yohimbine, an α2 antagonist. α2A selective ... 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 ... adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. ...
Antagonists L-765,314 Risperidone Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in regulation of ... 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- ...
... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein. It ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... Adrenergic receptor Graham, Robert (May 1, 1996). "α1-Adrenergic Receptor Subtypes Molecular Structure, Function, and Signaling ...
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 ... ADRA2A adrenergic, alpha-2A-, receptor". "α2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union ... Handy DE, Gavras H (Nov 1992). "Promoter region of the human alpha 2A adrenergic receptor gene". The Journal of Biological ...
This drug is a non-selective α-adrenergic antagonist, which means it binds to both alpha receptors. There are 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 ...
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... The alpha-2C adrenergic receptor (α2C adrenoceptor), also known as ADRA2C, is an alpha-2 adrenergic receptor, and also denotes ... Klein U, Ramirez MT, Kobilka BK, von Zastrow M (1997). "A novel interaction between adrenergic receptors and the alpha-subunit ... Preferential coupling of the alpha 2C-adrenergic receptor to the guanine nucleotide-binding protein, Go". J. Biol. Chem. 267 ( ...
... is a compound which acts as an antagonist at the α1B-adrenergic receptor. It was one of the first selective antagonists ... Characterization of alpha 1-adrenergic receptor subtypes in rat brain: a reevaluation of [3H]WB4104 and [3H]prazosin binding. ... developed for this receptor and was invented in 1969, but is still commonly used in research into adrenergic receptors, ... Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism? Farmaco. 1998 Apr;53(4):278-86. ...
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... denotes selective antagonist to the receptor. Beta-2 adrenergic receptor has been shown to interact with: AKAP12, OPRD1, Grb2, ... "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 adrenoreceptor), 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: ...
... alpha 1b- and alpha 1d-adrenergic receptor mRNA in the rat brain and spinal cord". Journal of chemical neuroanatomy. 13 (2): ... melatonin receptor antagonist blocks melatonin-induced antinociception in rats". Neuroscience Letters. 282 (3): 161-4. PMID ... Osim njegove alfa blokatorske aktivnosti, prazosin je antagonist MT3 receptora (koji nije prisutan kod ljudi). On je selektivan ... Day, H. E.; Campeau, S.; Watson Jr, S. J.; Akil, H. (1997). „Distribution of alpha 1a-, ...
Antagonists of α 1 {\displaystyle \alpha _{1}} receptors (doxazosin, prazosin) cause vasodilation (i.e. decrease in vascular ... The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... receptors. Under NE binding α 1 {\displaystyle \alpha _{1}} receptors cause vasoconstriction (i.e. contraction of the vascular ... Vascular smooth muscle is innervated primarily by the sympathetic nervous system through adrenergic receptors (adrenoceptors). ...
α2-blockers are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly ... Increases the noradrenaline release due to blockade of alpha-2 receptors. Historically, yohimbine was used as an aphrodisiac, ... Chopin P, Colpaert FC, Marien M (February 1999). "Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior ... Lemke, KA (June 2004). "Perioperative use of selective alpha-2 agonists and antagonists in small animals". The Canadian ...
Naltrexone, a mu opioid receptor antagonist, has shown mixed results for cannabis use disorder-both increasing the subjective ... Combination therapy with dronabinol and the alpha 2 adrenergic receptor agonist lofexidine have shown mixed results, with ... The CB-1 receptor antagonist rimonabant has shown efficacy in reducing the effects of cannabis in users, but with a risk for ... 2 (5): 670-675. doi:10.1001/jamaoncol.2016.0155. PMID 26986677.. *^ a b c Budney AJ, Roffman R, Stephens RS, Walker D (December ...
... is a calcium channel blocker and a1-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 ...
Adrenergic antagonists (nonselective and selective Beta1-antagonists) Alpha 2 agonists Hyperosmotic agents Fotil is a ... a beta-adrenergic receptor antagonist Glaucoma Basic and clinical science course (2011-2012). Glaucoma. American Academy of ...
Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic ... β1-selective antagonists include: Acebutolol (in hypertension, angina pectoris and arrhythmias) Atenolol (in hypertension, ... The beta-1 adrenergic receptor (β1 adrenoreceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the ... "GIPC interacts with the beta1-adrenergic receptor and regulates beta1-adrenergic receptor-mediated ERK activation". The Journal ...
... of the SP preferring receptor, i.e., by drugs known as neurokinin type 1 antagonists (also termed: SP antagonists, or ... Azzolina A, Bongiovanni A, Lampiasi N (Dec 2003). "Substance P induces TNF-alpha and IL-6 production through NF kappa B in ... administered through the non-adrenergic, non-cholinergic nervous system (branch of the vagal system). ... ReceptorEdit. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).[8] It belongs to the ...
3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors.. Perry BD, ... These results suggest that [3H]rauwolscine specifically labels both the high and low affinity states of the alpha 2-receptor in ... 3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in ... rauwolscine labeled the alpha 2-receptor. Agonists inhibited [3H]rauwolscine binding in a shallow, GTP-sensitive manner. ...
Narcotic Antagonists. Adrenergic alpha-2 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Up to 2 grams per day of acetaminophen is allowed at the discretion of the principal investigator or his designee. ... Lofexidine HCl 0.2 mg tablets titrated in ascending doses of 0.2 mg (1 tablet) QID starting at 0.4 mg (2 tablets) QID [e.g. Day ... Lofexidine Area Under the Curve (AUC) [ Time Frame: plateau days pre-dose, 0.5, 1 , 2, 3, 4, and 5 hours post dose ]. AUC will ...
Narcotic Antagonists. Antihypertensive Agents. Sympatholytics. Autonomic Agents. Adrenergic alpha-2 Receptor Agonists. ... Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Sildenafil citrate (Viagra). Sildenafil citrate doses , 25mg should not be taken within 4 hours of taking an alpha blocker or ... stress-induced relapse to heroin and cocaine seeking is blocked by the alpha-2 adrenergic agonist clonidine. In this study, ...
Histamine H1 Antagonists. Histamine Antagonists. Histamine Agents. Anti-Anxiety Agents. Tranquilizing Agents. Adrenergic alpha- ... Change in Interaction of the serotonin receptor (5-HTR) type-2C Cys23Ser single nucleotide polymorphism (SNP) and a 5-HT2AR ... Change in Interaction of the 5-HT2CR Cys23Ser SNP and a 5-HT2AR antagonist on the functional circuitry underlying cue ... HT2AR antagonist [ Time Frame: Baseline to 1 week ]. Change in fMRI activation with other 5-HT2CR SNPs during Attentional bias ...
Narcotic Antagonists. Adrenergic alpha-2 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. ... Lofexidine is an alpha2-adrenergic-agonist with mild to moderate antihypertensive actions. It is mainly used in the alleviation ... Have a score greater than or equal to 2 on the Objective Opiate Withdrawal Scale-Handelsman (OOWS) immediately prior to ... 2 above), anticonvulsants, antihypertensives, antiarrhythmics, antiretroviral, and cholesterol lowering medications. Nicotine ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Serotonin 5-HT2 Receptor Antagonists. Serotonin ... Dopamine Antagonists. Dopamine Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. Anti-Dyskinesia ...
Narcotic Antagonists. Physiological Effects of Drugs. Sensory System Agents. Peripheral Nervous System Agents. Adrenergic alpha ... Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Every subject will be invited to 2 separate sessions. At least 24 hours will apart the two sessions. The test in each session ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Serotonin 5-HT2 Receptor Antagonists. Serotonin Antagonists. Serotonin Agents. Dopamine D2 Receptor Antagonists. Dopamine ... 2018 Feb;26(2):150-159. doi: 10.1016/j.jagp.2017.08.013. Epub 2017 Oct 10. ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Phase 2: Participants will then live on an inpatient research unit (located in Detroit Michigan) for at least 16 consecutive ...
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Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Serotonin 5-HT2 Receptor Antagonists. Serotonin Antagonists. Serotonin Agents. Dopamine D2 Receptor Antagonists. Dopamine ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Serotonin 5-HT2 Receptor Antagonists. Serotonin Antagonists. Serotonin Agents. Dopamine D2 Receptor Antagonists. Dopamine ... Subject with Type 2 diabetes is eligible for study inclusion if the following condition is met at screening:. if a subject is ... An anchored Likert scale from 1-7, where values of 2 and above indicate the presence of progressively more severe symptoms, is ...
Intracerebroventricular injection of the adrenergic alpha-2-receptor agonist, clonidine, stimulated food intake. ... The present study was designed to investigate the role of brain adrenergic alpha-2-receptors on feeding regulation of layer- ... 0/Adrenergic alpha-Agonists; 0/Adrenergic alpha-Antagonists; 0/Neuropeptide Y; 0/Neurotransmitter Agents; 0/Receptors, ... Adrenergic alpha-Agonists / pharmacology. Adrenergic alpha-Antagonists / pharmacology. Animals. Chickens / physiology*. ...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Brimonidine (selective alpha 2 adrenergic agonist): neuroprotection effect by suppression of aqueous humor production and ... Contact: Ki Ho Park, M.D., Ph.D. +82-2-2072-2438 ext 3172 [email protected] ... Contact: Jae Hoon Jeong, M.D. +82-2-2072-2438 ext 3110 [email protected] ...
To test the effects in humans, we assessed autonomic vasomotor tone and baroreflex regulation in 9 normal young adults on 2 ... We observed earlier that central alpha-2 adrenoceptor stimulation in mice greatly augments parasympathetic tone. ... 0/Adrenergic alpha-Agonists; 0/Adrenergic beta-Antagonists; 0/Antihypertensive Agents; 0/Cardiotonic Agents; 0/Receptors, ... Adrenergic alpha-Agonists / pharmacology*. Adrenergic beta-Antagonists / pharmacology. Adult. Antihypertensive Agents / ...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Serotonin 5-HT2 Receptor Antagonists. Serotonin Antagonists. Serotonin ... Histamine H1 Antagonists. Histamine Antagonists. Histamine Agents. Anti-Anxiety Agents. Tranquilizing Agents. Adrenergic alpha- ... Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Each patient received 30 mg mirtazapine tablet and a placebo tablet for clonidine orally with sips of water 2 h preoperatively. ...
NMDA receptor antagonists: The NMDA receptor antagonists are available on prescription. Although there is not a legal ... The alpha2-adrenergic receptor agonists: the alpha2-adrenergic receptor agonists are available on prescription. Although there ... Alpha 2-Adrenergic Receptor Agonists. The alpha2-adrenergic receptor agonists have been used extensively in animals to ... NMDA Receptor Antagonists. N-methyl-D-aspartate (NMDA) receptors are important for the transmission of some aspects of pain in ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... If data is normally distributed Student t-test will be applied for comparison of 2 groups. Mann-Whitney U-test will be used for ... Sample size was estimated based on previous studies with sedation in equally invasive procedures that in 2 groups difference in ...
... an opioid receptor agonist/norepinephrine reuptake inhibitor tapentadol (Ortho-McNeil); a dopamine receptor agonist sodium ... a sodium channel antagonist mexiletine (Boehringer Ingelheim); three glutamate / NMDA antagonists ketamine intranasal (Javelin ... an alpha-2 adrenergic receptor antagonist/norepinehrine reuptake inhibitor reboxetine (Pfizer); ... Eighteen drugs are in Phase III development in the US including two GABA receptor agonists pregabalin (Pfizer) and gabapentin ...
Adrenergic alpha-Agonists. Adrenergic Agonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... glutamate receptor. NMDA receptor hypofunction can disinhibit excitatory (cholinergic/glutamatergic) projections in key areas ... NMDA antagonist-induced psychosis. Children. Memory Impairment. Decreased cognitive function. Increased memory impairment. ... Prevention of N-methyl-D-aspartate (NMDA) Antagonist-induced Psychosis in Kids. This study has been completed. ...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Adrenergic alpha-2 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. To Top ...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Adrenergic alpha-2 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. Carbonic Anhydrase Inhibitors. Enzyme ... Period 2 : 9d 0h,23d 0h,37d 0h,51d 0h,65d 0h,79d 0h,93d 0h,99d 0h,99d 12h,100d 0h (pre-dose), 100d 0.25,0.5,0.75,1,1.5,2,2.5,3, ... Period 2 : 9d 0h,23d 0h,37d 0h,51d 0h,65d 0h,79d 0h,93d 0h,99d 0h,99d 12h, 100d 0h(pre-dose),100d 0.25, 0.5, 0.75, 1, 1.5, 2, ...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Active Comparator: 2 tmolol 50 patients receiving timolol maleate 0.5% drops in the operated eye ... who will be administered Brimonidine to 2 control groups (50 people in each group): ... Adrenergic alpha-2 Receptor Agonists. Adrenergic alpha-Agonists. Adrenergic Agonists. To Top ...
... chronic effects of phenylethanolamine N-methyltransferase inhibitors and alpha adrenergic receptor antagonists on brain ... Changes in brain alpha-adrenergic receptors after alpha-methyldopa administration to spontaneously hypertensive rats. ... Modulation of rat brain alpha- and beta-adrenergic receptor populations by lesion of the dorsal noradrenergic bundle. ... Strain differences in rat brain epinephrine synthesis: regulation of alpha-adrenergic receptor number by epinephrine. ...
  • In June of that year, Raymond Ahlquist, Professor of Pharmacology at Medical College of Georgia, published a paper concerning adrenergic nervous transmission. (wikipedia.org)
  • In 1954, he was able to incorporate his findings in a textbook, Drill's Pharmacology in Medicine, and thereby promulgate the role played by α and β receptor sites in the adrenaline/noradrenaline cellular mechanism. (wikipedia.org)
  • These cognitive and behavioral effects are dose-dependently induced by ketamine and other antagonists of the N-methyl-D-aspartate (NMDA) glutamate receptor. (clinicaltrials.gov)
  • NMDA receptor hypofunction can disinhibit excitatory (cholinergic/glutamatergic) projections in key areas of the brain, and this has been proposed to explain key features of schizophrenia. (clinicaltrials.gov)
  • Several treatments that block excessive excitatory transmitter release have also been shown to prevent cognitive and behavioral effects of ketamine-induced NMDA receptor hypofunction in humans. (clinicaltrials.gov)
  • Children currently receive clinically-indicated treatment with the NMDA antagonist, ketamine, and this age group is an important target for pharmacological strategies aimed at the prevention of schizophrenia. (clinicaltrials.gov)
  • The proposed experiments are relevant to future prevention trials for individuals at risk for schizophrenia, and to preventing adverse effects of NMDA antagonist anesthetic agents (ketamine, nitrous oxide). (clinicaltrials.gov)
  • The authors note the limited utility of NMDA receptor antagonists and alpha-2 adrenergic agonists. (lww.com)
  • Several investigations have demonstrated protection against neuronal damage following global and focal ischemia, using antagonist against the N-methyl-d-aspartate (NMDA) receptor. (springer.com)
  • However, we have not been able to demonstrate a decrease in neuronal damage in the rat following 10 min of bilateral common carotid artery occlusion combined with hypotension, when the animals were pre- or post-treated with the non-competitive NMDA antagonist MK-801. (springer.com)
  • We propose that an ischemic insult, severe enough to cause prolonged periods of membrane depolarization, induces changes in the membrane properties leading to cycling of calcium ions across the plasmamembrane, which cannot be blocked by noncompetitive NMDA receptor antagonist. (springer.com)
  • Olney's lesions, also known as NMDA receptor antagonist neurotoxicity (NAN), are a potential form of brain damage. (wikipedia.org)
  • discovered that neuronal vacuolation and other cytotoxic changes ("lesions") occurred in brains of rats administered NMDA antagonists, including PCP, MK-801 (dizocilpine) and ketamine. (wikipedia.org)
  • Examination of neurons in the posterior cingulate and retrosplenial cortices by electron micrograph revealed apparent lytic breakdown of mitochondria in the large vacuoles which had become apparent 2 hours after administration of an NMDA antagonist. (wikipedia.org)
  • After repeated doses of the NMDA antagonists MK-801 and PCP, the vacuolation reaction appeared consistent with the reaction after a single dose, so there was no evidence of a cumulative neurotoxic effect or that the reaction proceeded to an irreversible stage with repeated doses. (wikipedia.org)
  • The potency of the drugs in producing these neurotoxic changes corresponded with their potency as NMDA antagonists: i.e. (wikipedia.org)
  • Researcher Roland N. Auer conducted similar studies to look at the correlation between age and sex and the development of NMDA receptor antagonist neurotoxicity in test rats. (wikipedia.org)
  • However, oral administration of dextromethorphan hydrobromide (DXM HBr) to female rats in single doses as high as 120 mg/kg did not result in detectable neurotoxic changes at 4-6 hours or 24-26 hours post-dose (female rats are more sensitive to NMDA antagonist neurotoxicity). (wikipedia.org)
  • Even if the hypothesis of gross neural apoptosis proves to be false in humans, NMDA antagonists certainly have potential to permanently alter synaptic structure due to effects upon long term potentiation, which NMDA plays a crucial role in. (wikipedia.org)
  • In medical settings, NMDA receptor antagonists are used as anesthetics, so GABAA receptor positive allosteric modulators are used to effectively prevent any neurotoxicity caused by them. (wikipedia.org)
  • Jansen writes: Neuroscience portal NMDA receptor NMDA receptor antagonist Dissociative Neurotoxic drug Olney J, Labruyere J, Price M (1989). (wikipedia.org)
  • It appears to be a weak NMDA receptor antagonist as well as an anticholinergic, specifically a nicotinic alpha-7 antagonist like the similar pharmaceutical memantine. (wikipedia.org)
  • Adding to its complex toxicity, cocaine targets muscarinic acetylcholine, N-methyl-D-aspartate (NMDA), sigma, and kappa-opioid receptors. (wikipedia.org)
  • Further evidence to the contrary of the monoamine hypothesis are the recent findings that a single intravenous infusion with ketamine, an antagonist of the NMDA receptor - a type of glutamate receptor - produces rapid (within 2 hours), robust and sustained (lasting for up to a fortnight) antidepressant effects. (wikipedia.org)
  • Although their primary mechanisms of action are as NMDA receptor antagonists, ketamine and phencyclidine are also SNDRIs and are similarly encountered as drugs of abuse. (wikipedia.org)
  • In the current study, we used [35S]GTPgammaS incorporation to characterize the intrinsic activity and potency of agonists and antagonists at the cloned mouse alpha2a/d and human alpha2a, alpha2b, and alpha2c ARs. (nih.gov)
  • Research using the rotarod test with various chemical agonists and antagonists may help scientists determine which components of neurons mediate the effects of chemicals. (wikipedia.org)
  • Desensitization of alpha 2-receptor-mediated inhibition of cAMP production by epinephrine did not alter the response to either 5HT or oxymetazoline, indicating that these compounds do not produce their effect by activating alpha 2-adrenergic receptors. (aspetjournals.org)
  • In addition, the lack of any guanylylimidodiphosphate effect on the l-epinephrine competition curve observed in MHS rats suggests the uncoupling of these receptors from the guanosine 5'-triphosphate binding protein. (ahajournals.org)
  • Although α receptors are less sensitive to epinephrine, when activated at pharmacologic doses, they override the vasodilation mediated by β-adrenoreceptors because there are more peripheral α1 receptors than β-adrenoreceptors. (wikipedia.org)
  • Beta receptors are found on cells of the heart muscles, smooth muscles, airways, arteries, kidneys, and other tissues that are part of the sympathetic nervous system and lead to stress responses, especially when they are stimulated by epinephrine (adrenaline). (wikipedia.org)
  • Beta blockers interfere with the binding to the receptor of epinephrine and other stress hormones, and weaken the effects of stress hormones. (wikipedia.org)
  • An adrenergic agent is a drug, or other substance, which has effects similar to, or the same as, epinephrine (adrenaline). (wikipedia.org)
  • Alternatively, it may refer to something which is susceptible to epinephrine, or similar substances, such as a biological receptor (specifically, the adrenergic receptors). (wikipedia.org)
  • The A2A receptor is responsible for regulating myocardial blood flow by vasodilating the coronary arteries, which increases blood flow to the myocardium, but may lead to hypotension. (wikipedia.org)
  • Activation of the 5-HT2A receptor in hypothalamus causes increases in hormonal levels of oxytocin, prolactin, ACTH, corticosterone, and renin. (wikipedia.org)
  • As an example, when administered with amphetamine or methamphetamine, iprindole increases their brain concentrations and prolongs their terminal half-lives by 2- to 3-fold, strongly augmenting both their physiological effects and neurotoxicity in the process. (wikipedia.org)
  • However, the researchers argued against this possibility because it was delayed (by several hours) and of relatively small magnitude, whereas established D2 receptor antagonists promptly induce marked increases in prolactin levels. (wikipedia.org)
  • Inhibition of the reuptake of these neurotransmitters increases their extracellular concentrations and, therefore, results in an increase in serotonergic, adrenergic, and dopaminergic neurotransmission. (wikipedia.org)
  • Characterization of alkaline response induced by cholinergic agents in the rat duodenum: involvement of M2 receptors and the calcium-dependent process. (aspetjournals.org)
  • Muscarinic cholinergic receptors on cultured thyroid cells. (aspetjournals.org)
  • Neurologic: Headache (2%), Dizziness (11%) Gastrointestinal: Nausea (6%), Dyspepsia (3%) Cholinergic: Nasal congestion (3%), Ejaculation failure (2%) Respiratory: Dyspnea (2%) Other: Fatigue (5%), Vertigo (2%), Orthostatic hypotension Low blood pressure with standing is more severe and more common with IV formulation (58% vs 1%) and is often the reason larger doses of the oral formulation cannot be used. (wikipedia.org)
  • Very few parts of the sympathetic system use cholinergic receptors. (wikipedia.org)
  • As is typical with many vasodilators, it also has bronchoconstrictive properties, administered through the non-adrenergic, non-cholinergic nervous system (branch of the vagal system). (wikipedia.org)
  • Both the effect on glycemic level and the inhibition of insulin release by oxymetazoline were antagonized by the alpha-2 adrenoceptor antagonist idazoxan. (aspetjournals.org)
  • It was shown to possess central α2-adrenoceptor antagonist activity after oral doses in man and was patented as an antidepressant by Glaxo in the early 1980s, but its development was discontinued when the compound failed to show a clear clinical advantage over existing therapies. (wikipedia.org)
  • This in vivo PET evidence for alpha(2)/dopaminergic interaction may be relevant to putative actions of atypical antipsychotic medications via adrenergic receptors. (sigmaaldrich.com)
  • Mechanistically, α2-blockers significantly increase adrenergic, dopaminergic and serotonergic neurotransmitters, and induce insulin secretion and decreases blood sugar levels. (wikipedia.org)
  • Amantadine has been associated with several central nervous system (CNS) side effects, likely due to amantadine's dopaminergic and adrenergic activity, and to a lesser extent, its activity as an anticholinergic. (wikipedia.org)
  • In 2004, it was discovered that amantadine and memantine bind to and act as agonists of the σ1 receptor (Ki = 7.44 µM and 2.60 µM, respectively), and that activation of the σ1 receptor is involved in the dopaminergic effects of amantadine at therapeutically relevant concentrations. (wikipedia.org)
  • Role in memory and learning Activation of the 5-HT2A receptor is necessary for the effects of the "classic" psychedelics like LSD, psilocin and mescaline, which act as full or partial agonists at this receptor, and represent the three main classes of 5-HT2A agonists, the ergolines, tryptamines and phenethylamines, respectively. (wikipedia.org)
  • Alpha blockers work by blocking the effect of nerves in the sympathetic nervous system. (wikipedia.org)
  • Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system. (wikipedia.org)