AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and Processes
Wakefulness-Promoting AgentsReceptors, Adrenergic, alpha-2Interleukin 1 Receptor Antagonist ProteinNeurokinin-1 Receptor AntagonistsPurinergic P1 Receptor AntagonistsDose-Response Relationship, DrugRats, Sprague-DawleyHistamine H2 AntagonistsSerotonin 5-HT3 Receptor AntagonistsPiperidinesExcitatory Amino Acid AntagonistsAngiotensin Receptor AntagonistsDopamine AntagonistsSerotonin 5-HT2 Receptor AntagonistsAdenosine A2 Receptor AntagonistsHormone AntagonistsAdenosine A1 Receptor AntagonistsPurinergic P2 Receptor AntagonistsRats, WistarNarcotic AntagonistsHistamine H1 AntagonistsReceptors, EndothelinMuscarinic AntagonistsGABA-A Receptor AntagonistsAdrenergic alpha-1 Receptor AntagonistsSerotonin AntagonistsGABA AntagonistsSialoglycoproteinsHistamine AntagonistsReceptors, Adrenergic, alphaalpha 1-AntitrypsinLeukotriene AntagonistsReceptor, Endothelin AReceptors, SerotoninReceptors, N-Methyl-D-AspartateSerotonin 5-HT1 Receptor AntagonistsNicotinic AntagonistsDizocilpine MaleateReceptors, Interleukin-1Adrenergic alpha-2 Receptor AntagonistsAdrenergic alpha-AntagonistsBiphenyl CompoundsBenzazepinesTetrazolesRadioligand AssayPyridinesXanthinesGuinea PigsSerotonin Receptor AgonistsPeptides, CyclicSulfonamidesDrug InteractionsIndolesHistamine H3 AntagonistsBinding, CompetitivePyrazolesHypoxia-Inducible Factor 1, alpha SubunitQuinoxalinesCells, CulturedAzepinesTime FactorsLosartanEndothelin-1GABA-B Receptor AntagonistsSubstance Palpha7 Nicotinic Acetylcholine ReceptorSerotoninReceptors, BradykininSignal TransductionNeuronsCimetidineReceptors, Neurokinin-1Adenosine A3 Receptor AntagonistsReceptor, Endothelin BPurinergic P2X Receptor AntagonistsPiperazinesBehavior, AnimalPyrrolidinesReceptors, Adrenergic, alpha-1Interleukin-1Receptors, CholecystokininDevazepideAdrenergic AntagonistsPrazosinReceptors, ThromboxaneReceptors, VasopressinKetanserin2-Amino-5-phosphonovalerateSerotonin 5-HT4 Receptor AntagonistsElectric StimulationDisease Models, AnimalReceptor, Cannabinoid, CB1BenzimidazolesMice, Inbred C57BLReceptors, Dopamine D2AdenosineNaltrexoneInjections, IntraventricularAdrenergic alpha-AgonistsFamotidineReceptors, Neurokinin-2CalciumBradykininCannabinoid Receptor AntagonistsNaloxoneQuinuclidinesBenzodiazepinonesHistamineAdrenergic beta-2 Receptor AntagonistsBicucullineReceptors, NicotinicImidazolesInterleukin-1alphaMineralocorticoid Receptor AntagonistsReceptors, Histamine H3Blood PressureYohimbineReceptors, Opioid
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.

alpha1-adrenergic receptor subtypes in human peripheral blood lymphocytes. (1/356)

We investigated the expression of alpha1-adrenergic receptor subtypes in intact human peripheral blood lymphocytes using reverse transcription-polymerase chain reaction (RT-PCR) and radioligand binding assay techniques combined with antibodies against the three subtypes of alpha1-adrenergic receptors (alpha1A, alpha1B, and alpha1D). RT-PCR amplified in peripheral blood lymphocytes a 348-bp alpha1A-adrenergic receptor fragment, a 689-bp alpha1B-adrenergic receptor fragment, and a 540-bp alpha1D-adrenergic receptor fragment. Radioligand binding assay with [3H]prazosin as radioligand revealed a high-affinity binding with a dissociation constant value of 0. 65+/-0.05 nmol/L and a maximum density of binding sites of 175. 3+/-20.5 fmol/10(6) cells. The pharmacological profile of [3H]prazosin binding to human peripheral blood lymphocytes was consistent with the labeling of alpha1-adrenergic receptors. Antibodies against alpha1A-, alpha1B-, and alpha1D-receptor subtypes decreased [3H]prazosin binding to a different extent. This indicates that human peripheral blood lymphocytes express the three alpha1-adrenergic receptor subtypes. Of the three different alpha1-adrenergic receptor subtypes, the alpha1B is the most represented and the alpha1D, the least. Future studies should clarify the functional relevance of alpha1-adrenergic receptors expressed by peripheral blood lymphocytes. The identification of these sites may represent a step for evaluating whether they represent a marker of alpha1-adrenergic receptors in cardiovascular disorders or for assessing responses to drug treatment on these receptors.  (+info)

Modulation of basal intracellular calcium by inverse agonists and phorbol myristate acetate in rat-1 fibroblasts stably expressing alpha1d-adrenoceptors. (2/356)

In rat-1 fibroblasts stably expressing alpha1d-adrenoceptors BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil decreased basal [Ca2+]i. WB 4101 induced a very small effect on this parameter but when added before the other antagonists it blocked their effect. All these agents inhibited the action of norepinephrine. Phorbol myristate acetate also blocked the effect of norepinephrine and decreased basal [Ca2+]i. Staurosporine inhibited these effects of the phorbol ester. Our results suggest that: (1) alpha1d-adrenoceptors exhibit spontaneous ligand-independent activity, (2) BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil act as inverse agonists and (3) protein kinase C activation blocks spontaneous and agonist-stimulated alpha1d-adrenoceptor activity.  (+info)

Characterization of alpha1-adrenoceptor subtypes mediating vasoconstriction in human umbilical vein. (3/356)

1. The present study attempted to characterize pharmacologically the subtypes of alpha-adrenoceptors mediating contractions in human umbilical vein (HUV). 2. HUV rings were mounted in isolated organ baths and cumulative concentration-response curves were constructed for the alpha-adrenoceptor agonists phenylephrine and adrenaline. Adrenaline was more potent than phenylephrine (pD2=7.29 and 6.04 respectively). 3. Isoproterenol exhibited no agonism on KCl pre-contracted HUV rings. Propranolol (1 microM) and rauwolscine (0.1 microM) did not affect the concentration-response curves to adrenaline. These results demonstrate the lack of involvement of functional beta-or alpha2-adrenoceptors in adrenaline-induced vasoconstriction. 4. The non subtype selective alpha1-adrenoceptor antagonist prazosin was evaluated on phenylephrine and adrenaline concentration-response curves. The effects of the competitive alpha1A and alpha1D-adrenoceptor antagonists, 5-methyl urapidil and BMY 7378 and the irreversible alpha1B selective compound chloroethylclonidine (CEC) were also evaluated on adrenaline concentration-response curves. 5. The potencies of prazosin against responses mediated by adrenaline (pA2= 10.87) and phenylephrine (pA2= 10.70) indicate the involvement of prazosin-sensitive functional alpha1-adrenoceptor subtype in vasoconstriction of the HUV. 6. The potencies of 5-methyl urapidil (pA2 = 6.70) and BMY 7378 (pA2= 7.34) were not consistent with the activation of an alpha1A- or alpha1D-adrenoceptor population. 7. Exposure to a relatively low CEC concentration (3 microM) abolished the maximum response to adrenaline suggesting that this response was mediated by an alpha1B-adrenoceptor subtype. 8. We conclude that HUV express a prazosin-sensitive functional alpha1-adrenoceptor resembling the alpha1B-subtype according with the low pA2 values for both 5-methyl urapidil and BMY 7378 and the high sensitivity to CEC.  (+info)

Comparison of relaxation responses of cavernous and trigonal smooth muscles from rabbits by alpha1-adrenoceptor antagonists; prazosin, terazosin, doxazosin, and tamsulosin. (4/356)

Alpha1a-adrenergic receptor (AR) primarily mediates the contraction of the prostatic and cavernous smooth muscles. Among clinically available alpha1-AR antagonists for the medical management of benign prostatic hyperplasia (BPH), tamsulosin has a modest selectivity for alpha1A- and alpha1D- over alpha1B-ARs. To compare the effects of various alpha1-AR antagonists on relaxation responses of cavernous and trigonal smooth muscles, isometric tension studies with relatively selective (tamsulosin) and non-selective (prazosin, doxazosin, and terazosin) alpha1A-AR antagonists, were conducted in the cavernous and trigonal muscle strips of rabbits (n=10 each). Tamsulosin had the strongest inhibitory effect on contraction of trigonal smooth muscle among the various alpha1-AR antagonists, and the inhibitory activities of prazosin, doxazosin, and terazosin were not statistically different. All alpha1-AR antagonists caused concentration-dependent relaxation of the cavernous muscle strips. Tamsulosin was shown to have greater potency than prazosin (more than 100-fold), doxazosin (more than 1000-fold), and terazosin (more than 1000-fold), in relaxation of cavernous smooth muscle. In conclusion, tamsulosin might be the most effective drug among the four commonly used alpha1-AR antagonists for the medical management of BPH. Tamsulosin might be a potential substitute for phentolamine in combination with vasoactive agents as an intracavernous injection therapy for patients with erectile dysfunction.  (+info)

Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors. (5/356)

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)

alpha1-adrenergic receptor activation of c-fos expression in transfected rat-1 fibroblasts: role of Ca2+. (6/356)

alpha1-Adrenergic receptors mediate mitogenic responses and increase intracellular free Ca2+ ([Ca2+]i) in vascular smooth muscle cells. Induction of c-fos is a critical early event in cell growth; expression of this gene is regulated by a number of signaling pathways including Ca2+. We wondered whether Ca2+ signaling plays a critical role in the induction of c-fos gene by alpha1-adrenergic receptors. Using stably transfected rat-1 fibroblasts, we confirmed that PE induced c-fos mRNA expression in a time- and dose-dependent manner, and also increased [Ca2+]i (measured with Fura-2 AM). These responses were blocked by the alpha1-adrenergic receptor antagonist doxazosin. Both intracellular Ca2+ chelation (using BAPTA/AM) and extracellular Ca2+ depletion (using EGTA) significantly inhibited PE-induced c-fos expression by alpha1A and alpha1B receptors. Brief (1-min) stimulation of alpha1A and alpha1B receptors with PE did not maximally induce c-fos expression, suggesting that a sustained increase in [Ca2+]i due to Ca2+ influx is required. The calmodulin (CaM) antagonists, R24571, W7, and trifluoperazine, but not the CaM-dependent protein kinases inhibitor KN-62, significantly inhibited c-fos induction by alpha1A and alpha1B receptors. Neither inhibition of protein kinase C nor inhibition of adenylyl cyclase modified c-fos induction by PE. These results suggest that alpha1-adrenergic receptor-induced c-fos expression in rat-1 cells is dependent on a Ca2+/CaM-associated pathway.  (+info)

In vivo measurement by [3H]Tamsulosin of alpha1 adrenoceptors in rat tissues in relation to the pharmacokinetics. (7/356)

The present study was undertaken to simultaneously measure alpha1 adrenoceptors in rat tissues by [3H]tamsulosin in vivo. In vivo specific [3H]tamsulosin binding was observed in the prostate, vas deferens, aorta, submaxillary gland, spleen, heart, lung, and kidney after i.v. injection of the ligand but not in the cerebral cortex and liver. Specific [3H]tamsulosin binding in the kidney, lung, heart, and spleen was greatest at 3 min after i.v. injection and declined rapidly with the disappearance of [3H]tamsulosin from the plasma. On the other hand, [3H]tamsulosin binding in the prostate and aorta peaked at 10 to 60 min after i.v. injection, and a considerable level of specific binding in both tissues persisted up to 240 min. The most sustained binding of [3H]tamsulosin occurred in the submaxillary gland. In vivo specific [3H]tamsulosin binding in rat tissues was effectively inhibited by the coinjection of low doses of unlabeled tamsulosin, prazosin, and terazosin with the radioligand but not by relatively high doses of yohimbine and propranolol. Based on estimated ID50 values, in vivo inhibitory effect of tamsulosin compared with prazosin was 5 to 14 times greater in rat tissues except the spleen, which showed 1.6 times less potent than prazosin. From ratios of ID50 (spleen) to ID50 (submaxillary gland) or ID50 (prostate), tamsulosin was 9 and 19 times, respectively, greater than prazosin in selectivity of alpha1 adrenoceptors in the submaxillary gland and prostate versus the spleen, respectively, suggesting that tamsulosin binds to alpha1A subtype with higher affinity than alpha1B subtype in vivo. The present study suggests that [3H]tamsulosin is a useful radioligand for in vivo measurement of alpha1 adrenoceptors in rat tissues.  (+info)

Naftopidil, a novel alpha1-adrenoceptor antagonist, displays selective inhibition of canine prostatic pressure and high affinity binding to cloned human alpha1-adrenoceptors. (8/356)

The pharmacological profiles of the alpha1-adrenoceptor antagonists naftopidil, tamsulosin and prazosin were studied in an anesthetized dog model that allowed the simultaneous assessment of their antagonist potency against phenylephrine-mediated increases in prostatic pressure and mean blood pressure. The intravenous administration of each of these compounds dose-dependently inhibited phenylephrine-induced increases in prostatic pressure and mean blood pressure. To further assess the ability of the three compounds to inhibit phenylephrine-induced responses, the doses required to produce a 50% inhibition of the phenylephrine-induced increases in prostatic and mean blood pressure and the selectivity index obtained from the ratio of those two doses were determined for each test compound. Forty minutes after the intravenous administration of naftopidil, the selectivity index was 3.76, and those of tamsulosin and prazosin were 1.23 and 0.61, respectively. These findings demonstrated that naftopidil selectively inhibited the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. The selectivity of naftopidil for prostatic pressure was the most potent among the test compounds. In addition, using cloned human alpha1-adrenoceptor subtypes, naftopidil was selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. The selectivity of naftopidil for prostatic pressure may be attributable to its high binding affinity for alpha1a- and alpha1d-adrenoceptor subtypes.  (+info)

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Rats administered doses up to 43 mg/kg/day in males and 52 mg/kg/day in females had no increases in tumor incidence, with the exception of a modest increase in the frequency of mammary gland fibroadenomas in female rats receiving doses ≥5.4 mg/kg (P,0.015). The highest doses of tamsulosin hydrochloride evaluated in the rat carcinogenicity study produced systemic exposures (AUC) in rats 3 times the exposures in men receiving the maximum therapeutic dose of 0.8 mg/day.. Mice were administered doses up to 127 mg/kg/day in males and 158 mg/kg/day in females. There were no significant tumor findings in male mice. Female mice treated for 2 years with the two highest doses of 45 and 158 mg/kg/day had statistically significant increases in the incidence of mammary gland fibroadenomas (P,0.0001) and adenocarcinomas (P,0.0075). The highest dose levels of tamsulosin hydrochloride evaluated in the mice carcinogenicity study produced systemic exposures (AUC) in mice 8 times the exposures in men receiving ...
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Alpha1A-adrenoceptor antagonist improves underactive bladder associated with diabetic cystopathy via bladder blood flow in rats...Alpha1A-adrenoceptor antagonist improves underactive bladder associated with diabetic cystopathy via bladder blood flow in rats...
In this study, we examined the changes in bladder function and the effects of silodosin in STZ-induced DM rats. Nine weeks after STZ induction, urinary dysfunction was observed on a CMG. Increases in BC and RV were observed in the DM group, and the BC/BlaW ratio was high. Furthermore, BBF was decreased and both gene and protein expression levels of NF-M and peripherin, which are neuronal markers, were decreased in bladder tissue in the DM group. These results suggest that a decrease in BBF and bladder hyperextension with sensory disorder, i.e., UAB-like symptoms, occurred in the DM group. The alpha1A-AR antagonist silodosin showed inhibitory effects against all of these changes in the DM group. Silodosin shows preventive or curative effects against UAB-like symptoms in DM, and these effects may be caused by the improvement in the sensory disorder by preventing the decrease in BBF.. Autonomic nervous system disorders due to peripheral neuropathy, which is one of the 3 major complications of DM, ...
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This study will investigate the efficacy and safety of treatment with Dutasteride (0.5mg), administered once daily for one year in combination with Tamsulosin (0.4mg), administered once daily for 3 months, followed by counseling on flexible dosing of Tamsulosin on an as needed basis, on the improvement of symptoms and clinical outcome in men with moderate to severe symptomatic benign prostatic hyperplasia (BPH). At each scheduled visit (3, 6, and 9 months), the subject will be counseled on withdrawal of Tamsulosin.. A recently published, landmark study (MTOPS - Medical Therapy of Prostatic Symptoms), co-sponsored by the National Institute of Health and the National Institute of Diabetes, Digestive and Kidney Diseases (NIH-NIDDK), demonstrated that, in selected patients, combination therapy with Doxazosin and Finasteride provided additive symptomatic improvements, reduced the risk of acute urinary retention (AUR) and surgical intervention, and was a more effective treatment for reduction in the ...
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Forray C; Bard JA; Wetzel JM; et al. (1994). „The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype.". Mol. Pharmacol. 45 (4): 703-8. PMID 8183249 ...
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Alpha blocker - WikipediaAlpha blocker - Wikipedia
Alpha-blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha-blockers were used as a tool for pharmacologic research to develop a greater understanding of the autonomic nervous system. Using alpha blockers, scientists began characterizing arterial blood pressure and central vasomotor control in the autonomic nervous system. Today, they can be used as clinical treatments for a limited number of diseases. Although alpha blockers can only treat a small range of diseases, some of them have clinical uses, such as having the ability to treat hypertension, Raynauds disease, Congestive Heart Failure, erectile dysfunction, etc. Generally speaking, all of these treatments function by binding an α-blocker to α receptors in the arteries and smooth muscle. Ultimately, this relaxes the smooth muscle or blood vessels, which increases fluid flow in these entities. ...
Sandoz Alfuzosin / Acheter Clarithromycin En LigneSandoz Alfuzosin / Acheter Clarithromycin En Ligne
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The relation between baseline PSA and symptomatic progression in Egyptian BPH patients receiving tamsulosin monotherapy: an...The relation between baseline PSA and symptomatic progression in Egyptian BPH patients receiving tamsulosin monotherapy: an...
Background To examine the relation of baseline serum prostatic-specific antigen (PSA) to symptomatic changes in men with benign prostatic hyperplasia (BPH) receiving tamsulosin through its relation to...
Naftopidil - Self-sufficiencyNaftopidil - Self-sufficiency
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. ...
AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and Processes
Wakefulness-Promoting AgentsReceptors, Adrenergic, alpha-2Interleukin 1 Receptor Antagonist ProteinNeurokinin-1 Receptor AntagonistsPurinergic P1 Receptor AntagonistsDose-Response Relationship, DrugRats, Sprague-DawleyHistamine H2 AntagonistsSerotonin 5-HT3 Receptor AntagonistsPiperidinesExcitatory Amino Acid AntagonistsAngiotensin Receptor AntagonistsDopamine AntagonistsSerotonin 5-HT2 Receptor AntagonistsAdenosine A2 Receptor AntagonistsHormone AntagonistsAdenosine A1 Receptor AntagonistsPurinergic P2 Receptor AntagonistsRats, WistarNarcotic AntagonistsHistamine H1 AntagonistsReceptors, EndothelinMuscarinic AntagonistsGABA-A Receptor AntagonistsAdrenergic alpha-1 Receptor AntagonistsSerotonin AntagonistsGABA AntagonistsSialoglycoproteinsHistamine AntagonistsReceptors, Adrenergic, alphaalpha 1-AntitrypsinLeukotriene AntagonistsReceptor, Endothelin AReceptors, SerotoninReceptors, N-Methyl-D-AspartateSerotonin 5-HT1 Receptor AntagonistsNicotinic AntagonistsDizocilpine MaleateReceptors, Interleukin-1Adrenergic alpha-2 Receptor AntagonistsAdrenergic alpha-AntagonistsBiphenyl CompoundsBenzazepinesTetrazolesRadioligand AssayPyridinesXanthinesGuinea PigsSerotonin Receptor AgonistsPeptides, CyclicSulfonamidesDrug InteractionsIndolesHistamine H3 AntagonistsBinding, CompetitivePyrazolesHypoxia-Inducible Factor 1, alpha SubunitQuinoxalinesCells, CulturedAzepinesTime FactorsLosartanEndothelin-1GABA-B Receptor AntagonistsSubstance Palpha7 Nicotinic Acetylcholine ReceptorSerotoninReceptors, BradykininSignal TransductionNeuronsCimetidineReceptors, Neurokinin-1Adenosine A3 Receptor AntagonistsReceptor, Endothelin BPurinergic P2X Receptor AntagonistsPiperazinesBehavior, AnimalPyrrolidinesReceptors, Adrenergic, alpha-1Interleukin-1Receptors, CholecystokininDevazepideAdrenergic AntagonistsPrazosinReceptors, ThromboxaneReceptors, VasopressinKetanserin2-Amino-5-phosphonovalerateSerotonin 5-HT4 Receptor AntagonistsElectric StimulationDisease Models, AnimalReceptor, Cannabinoid, CB1BenzimidazolesMice, Inbred C57BLReceptors, Dopamine D2AdenosineNaltrexoneInjections, IntraventricularAdrenergic alpha-AgonistsFamotidineReceptors, Neurokinin-2CalciumBradykininCannabinoid Receptor AntagonistsNaloxoneQuinuclidinesBenzodiazepinonesHistamineAdrenergic beta-2 Receptor AntagonistsBicucullineReceptors, NicotinicImidazolesInterleukin-1alphaMineralocorticoid Receptor AntagonistsReceptors, Histamine H3Blood PressureYohimbineReceptors, Opioid
BunazosinBunazosin
Systemic Alpha-1 adrenergic receptor antagonists have been implicated in Intraoperative Floppy Iris Syndrome (IFIS). Bunazosin ... Bunazosin (INN) is an alpha 1 antagonist. Bunazosin was initially developed to treat benign prostatic hyperplasia (BPH). It has ...
2C-H2C-H
It features competitive antagonist activity at 5-HT serotonin receptor in Sprague-Dawley rat stomachs. It exhibits binding ... It was found to be an active Alpha-1 adrenergic receptor agonist in rabbit ear arteries. It has binding affinity towards 5-HT2C ... It exhibits agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with ... affinity against rat 5-hydroxytryptamine 2C receptors using [3H]mesulergine as a radioligand. As of October 31, 2016; 2C-H is a ...
L-765,314L-765,314
... a potent and selective alpha1b adrenergic receptor antagonist ". Journal of Medicinal Chemistry. 41 (8): 1205-8. doi:10.1021/ ... L-765,314 is a drug which acts as a potent and selective antagonist for the Alpha-1 adrenergic receptor subtype α1B. It has ... Yang XP, Chiba S (August 2002). "Effects of L-765,314, a selective and potent alpha 1B-adrenoceptor antagonist, on periarterial ... Hillman KL, Doze VA, Porter JE (June 2007). "Alpha1A-adrenergic receptors are functionally expressed by a subpopulation of ...
Post-traumatic amnesiaPost-traumatic amnesia
Administering a norepinephrine receptor agonist (a substance that initiates a cell response when it binds with a receptor) to ... Noradrenergic antagonists were not prescribed for the purposes of slowing the recovery of memory. Rather, these findings are ... The alpha-1 adrenergic receptor is specifically implicated. Although it has not yet been thoroughly investigated, there is ... Conversely, the administration of norpinephrine antagonists slowed recovery, and could lead to the reinstatement of deficits ...
TetrahydropalmatineTetrahydropalmatine
Additionally, l-THP displays significant binding to 5-HT1A and alpha-2 adrenergic receptors. In the case of 5-HT1A receptors, l ... at which it functions as an antagonist, and GABA-A receptors, through positive allosteric modulation. ... 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, including alpha-1 ...
Alpha-1 blockerAlpha-1 blocker
Silodosin shows high affinity and selectivity for alpha-1a adrenergic receptors found in the prostate which ensures that it ... Taylor, Fletcher; Raskind, Murray A. (February 2002). "The alpha1-adrenergic antagonist prazosin improves sleep and nightmares ... DrugDigest - Alpha blockers RxList.com - Tamsulosin alpha-Adrenergic Blockers at the US National Library of Medicine Medical ... Silodosin is the most selective for alpha-1a receptors. The affinity and selectivity for alpha-1 receptors seems to be ...
5-HT2A receptor5-HT2A receptor
... 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. ... G-protein coupled receptor activity. • virus receptor activity. • signal transducer activity. • drug binding. • G-protein alpha ... The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G ...
Alpha-2C adrenergic receptorAlpha-2C adrenergic receptor
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 ... "Human alpha 2-adrenergic receptor subtype distribution: widespread and subtype-selective expression of alpha 2C10, alpha 2C4, ... Alpha-2-adrenergic receptors include 3 highly homologous subtypes: alpha2A, alpha2B, and alpha2C. These receptors have a ...
Alpha-1 adrenergic receptorAlpha-1 adrenergic receptor
... relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists". Journal ... Note that only active muscle α1-adrenergic receptors will be blocked. Resting muscle will not have its α1-adrenergic receptors ... In contrast to α2-adrenergic receptors, α1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more ... The α1-adrenergic receptor has several general functions in common with the α2-adrenergic receptor, but also has specific ...
Alfa-1D adrenergički receptor - Википедија, слободна енциклопедијаAlfa-1D adrenergički receptor - Википедија, слободна енциклопедија
1994). „Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c.". Biochem ... Kyprianou N, Benning CM (2000). „Suppression of human prostate cancer cell growth by alpha1-adrenoceptor antagonists doxazosin ... 1995). „Cloning of the human alpha 1d-adrenergic receptor and inducible expression of three human subtypes in SK-N-MC cells.". ... Cell surface expression of alpha1D-adrenergic receptors is controlled by heterodimerization with alpha1B-adrenergic receptors ...
Alfa-1 adrenergički receptor - Википедија, слободна енциклопедијаAlfa-1 adrenergički receptor - Википедија, слободна енциклопедија
Labetalol (koristi se za hipertenziju; it is a mixed alpha/beta adrenergic antagonist)[4] ... adrenergički receptor je G protein-spregnuti receptor koji vezuje Gq heterotrimerni G protein. Postoje tri visoko homologna ... Adrenergički receptor. Literatura[уреди]. *↑ Woodman OL, Vatner SF (1987). „Coronary vasoconstriction mediated by α1- and α2- ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
Alpha-1B adrenergic receptorAlpha-1B adrenergic receptor
Antagonists L-765,314 Risperidone Alpha-1B adrenergic receptor has been shown to interact with AP2M1. A role in regulation of ... 1994). "Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c". Biochem ... The alpha-1B adrenergic receptor (α1B adrenoreceptor), also known as ADRA1B, is an alpha-1 adrenergic receptor, and also ... 2003). "The adaptor complex 2 directly interacts with the alpha 1b-adrenergic receptor and plays a role in receptor endocytosis ...
Alpha blockerAlpha blocker
However, the most common type of alpha blocker is usually an α1 blocker. Non-selective α-adrenergic receptor antagonists ... are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha- ... "Alpha-Adrenoceptor Antagonists (Alpha-Blockers)" (PDF). British Hypertension Society. "CV Pharmacology , Alpha-Adrenoceptor ... and alpha 2-adrenergic receptors". The FASEB Journal. 6: 832-839. McKeage, Kate; Plosker, Greg L. (2002-03-01). "Alfuzosin". ...
Adrenergic antagonistAdrenergic antagonist
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 ...
Alpha-2A adrenergic receptorAlpha-2A adrenergic receptor
... seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists ... 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 ...
Beta-2 adrenergic receptorBeta-2 adrenergic receptor
... denotes selective antagonist to the receptor. Beta-2 adrenergic receptor has been shown to interact with: AKAP12, OPRD1, Grb2, ... Other adrenergic receptors Alpha-1 adrenergic receptor Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-3 adrenergic ... The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor ... "Insulin stimulates sequestration of beta-adrenergic receptors and enhanced association of beta-adrenergic receptors with Grb2 ...
Beta-3 adrenergic receptorBeta-3 adrenergic receptor
... 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 antagonists". The Journal of Pharmacology and Experimental Therapeutics. 290 (2): 649-55. PMID 10411574. ...
Adrenergic receptorAdrenergic receptor
ISBN 0-443-06911-5. Alpha receptors illustrated The Adrenergic Receptors "Adrenoceptors". IUPHAR Database of Receptors and Ion ... "Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes". Molecular ... Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 Cannon WB, Rosenbluth A (31 May 1933). "Studies On Conditions ... Basic Neurochemistry: α- and β-Adrenergic Receptors Brief overview of functions of the β3 receptor Theory of receptor ...
WB-4101WB-4101
... is a compound which acts as an antagonist at the α1B-adrenergic receptor. It was one of the first selective antagonists ... Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism? Farmaco. 1998 Apr;53(4):278-86. ... developed for this receptor and was invented in 1969, but is still commonly used in research into adrenergic receptors, ... 1969 Mar;12(2):326-9. PMID 5791620 Morrow AL, Creese I. Characterization of alpha 1-adrenergic receptor subtypes in rat brain: ...
Vascular smooth muscleVascular smooth muscle
See also receptor antagonist) α 2 {\displaystyle \alpha _{2}} receptors. Agonists of α 2 {\displaystyle \alpha _{2}} receptors ... The main endogenous agonist of these cell receptors is norepinephrine (NE). The adrenergic receptors exert opposite physiologic ... alpha _{2}} receptors in the vascular smooth muscle cells). Usage of β 2 {\displaystyle \beta _{2}} receptor agonists as ... However, in clinical practice drugs applied intravenously that are agonists of α 2 {\displaystyle \alpha _{2}} receptors ( ...
BronchospasmBronchospasm
... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ... Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ... Both of these medications activate alpha-1 adrenergic receptors that result in smooth muscle constriction. Non-selective beta ... Beta blockers bind into the β2 receptors and block the action of epinephrine and norepinephrine from binding to its receptors, ...
Pausinystalia johimbePausinystalia johimbe
ISBN 9789290814955 Doxey, JC; Lane AC; Roach AG; Virdee NK (Feb 1984). "Comparison of the alpha-adrenoceptor antagonist ... Among other alkaloids is corynanthine, an alpha-1 adrenergic receptor blocker and raubasine. Extracts from the bark of yohimbe ...
MonatepilMonatepil
... is a calcium channel blocker and α1-adrenergic receptor antagonist used as an antihypertensive. Sugimoto T, Hosoki K ... Karasawa T (July 1995). "Relative contribution of alpha 1-adrenoceptor blocking activity to the hypotensive effect of the novel ... calcium antagonist monatepil". Journal of Cardiovascular Pharmacology. 26 (1): 55-60. doi:10.1097/00005344-199507000-00009. ...
Alpha-1D adrenergic receptorAlpha-1D adrenergic receptor
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... 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 ... The alpha-1D adrenergic receptor (α1D adrenoreceptor), also known as ADRA1D, is an alpha-1 adrenergic receptor, and also ...
NiguldipineNiguldipine
... is a calcium channel blocker and a1-adrenergic receptor antagonist. Boer R, Grassegger A, Schudt C, Glossmann H ( ... Niguldipine binds with very high affinity to Ca2+ channels and to a subtype of alpha 1-adrenoceptors". European Journal of ...
Substance PSubstance P
Hesketh PJ (Jul 2001). "Potential role of the NK1 receptor antagonists in chemotherapy-induced nausea and vomiting". Supportive ... 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 ...
AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and Processes
Wakefulness-Promoting AgentsReceptors, Adrenergic, alpha-2Interleukin 1 Receptor Antagonist ProteinNeurokinin-1 Receptor AntagonistsPurinergic P1 Receptor AntagonistsDose-Response Relationship, DrugRats, Sprague-DawleyHistamine H2 AntagonistsSerotonin 5-HT3 Receptor AntagonistsPiperidinesExcitatory Amino Acid AntagonistsAngiotensin Receptor AntagonistsDopamine AntagonistsSerotonin 5-HT2 Receptor AntagonistsAdenosine A2 Receptor AntagonistsHormone AntagonistsAdenosine A1 Receptor AntagonistsPurinergic P2 Receptor AntagonistsRats, WistarNarcotic AntagonistsHistamine H1 AntagonistsReceptors, EndothelinMuscarinic AntagonistsGABA-A Receptor AntagonistsAdrenergic alpha-1 Receptor AntagonistsSerotonin AntagonistsGABA AntagonistsSialoglycoproteinsHistamine AntagonistsReceptors, Adrenergic, alphaalpha 1-AntitrypsinLeukotriene AntagonistsReceptor, Endothelin AReceptors, SerotoninReceptors, N-Methyl-D-AspartateSerotonin 5-HT1 Receptor AntagonistsNicotinic AntagonistsDizocilpine MaleateReceptors, Interleukin-1Adrenergic alpha-2 Receptor AntagonistsAdrenergic alpha-AntagonistsBiphenyl CompoundsBenzazepinesTetrazolesRadioligand AssayPyridinesXanthinesGuinea PigsSerotonin Receptor AgonistsPeptides, CyclicSulfonamidesDrug InteractionsIndolesHistamine H3 AntagonistsBinding, CompetitivePyrazolesHypoxia-Inducible Factor 1, alpha SubunitQuinoxalinesCells, CulturedAzepinesTime FactorsLosartanEndothelin-1GABA-B Receptor AntagonistsSubstance Palpha7 Nicotinic Acetylcholine ReceptorSerotoninReceptors, BradykininSignal TransductionNeuronsCimetidineReceptors, Neurokinin-1Adenosine A3 Receptor AntagonistsReceptor, Endothelin BPurinergic P2X Receptor AntagonistsPiperazinesBehavior, AnimalPyrrolidinesReceptors, Adrenergic, alpha-1Interleukin-1Receptors, CholecystokininDevazepideAdrenergic AntagonistsPrazosinReceptors, ThromboxaneReceptors, VasopressinKetanserin2-Amino-5-phosphonovalerateSerotonin 5-HT4 Receptor AntagonistsElectric StimulationDisease Models, AnimalReceptor, Cannabinoid, CB1BenzimidazolesMice, Inbred C57BLReceptors, Dopamine D2AdenosineNaltrexoneInjections, IntraventricularAdrenergic alpha-AgonistsFamotidineReceptors, Neurokinin-2CalciumBradykininCannabinoid Receptor AntagonistsNaloxoneQuinuclidinesBenzodiazepinonesHistamineAdrenergic beta-2 Receptor AntagonistsBicucullineReceptors, NicotinicImidazolesInterleukin-1alphaMineralocorticoid Receptor AntagonistsReceptors, Histamine H3Blood PressureYohimbineReceptors, Opioid
Lisinopril or Coreg CR® in Reducing Side Effects in Women With Breast Cancer Receiving Trastuzumab - Full Text View -...Lisinopril or Coreg CR® in Reducing Side Effects in Women With Breast Cancer Receiving Trastuzumab - Full Text View -...
Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Vasodilator Agents. Adrenergic alpha-1 Receptor Antagonists ... Current treatment with angiotensin converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs), such as losartan, ... Patients are stratified according to chemotherapy comprising an anthracycline (yes vs no). Patients are randomized to 1 of 3 ...
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Coreg CR, Blood Vessel Stiffness and Blood Vessel Function - Full Text View - ClinicalTrials.govCoreg CR, Blood Vessel Stiffness and Blood Vessel Function - Full Text View - ClinicalTrials.gov
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Adrenergic alpha-1 Receptor Antagonists. Adrenergic ... Coreg CR also blocks alpha-receptors, which may provide added blood pressure-lowering. In addition, Coreg CR may have anti- ... Although both drugs reduce blood pressure by blocking the action of noradrenaline on beta-receptors in the blood vessels, ... differs from an alpha/beta blocker (Coreg CR) in these effects. We will also examine the mechanism by which such differences ...
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LAAS (Losartan Anti-Atherosclerosis Study)(0954-330)(COMPLETED) - Full Text View - ClinicalTrials.govLAAS (Losartan Anti-Atherosclerosis Study)(0954-330)(COMPLETED) - Full Text View - ClinicalTrials.gov
Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Vasodilator Agents. Adrenergic alpha-1 Receptor Antagonists ... Angiotensin Receptor Antagonists. Molecular Mechanisms of Pharmacological Action. Diuretics. Natriuretic Agents. Physiological ... Experimental: 1 Losartan or Losartan/HCTZ. Drug: losartan potassium Once daily , Cozaar® (losartan) 50 mg, Cozaar® (losartan) ... when blood pressure is measured at Visit 1(week -2) and at Visit 2(week 0). ...
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BOAT: Beta Blocker Uptitration With OptiVol After Cardiac Resynchronization Therapy (CRT) - Full Text View - ClinicalTrials.govBOAT: Beta Blocker Uptitration With OptiVol After Cardiac Resynchronization Therapy (CRT) - Full Text View - ClinicalTrials.gov
Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of Pharmacological Action. Vasodilator ... Adrenergic beta-Antagonists. Anti-Arrhythmia Agents. Antihypertensive Agents. Sympatholytics. Autonomic Agents. Peripheral ... 2005 Apr 1;95(7):889-91. Effect of metoprolol CR/XL in chronic heart failure: Metoprolol CR/XL Randomised Intervention Trial in ... Active Comparator: 1 CRT and b-blocker uptitration to target dose. Drug: Beta blocker (carvedilol or metoprolol succinate) Both ...
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Glycemic Control Of Carvedilol Versus Metoprolol In Patients With Type II Diabetes Mellitus And Hypertension - Full Text View -...Glycemic Control Of Carvedilol Versus Metoprolol In Patients With Type II Diabetes Mellitus And Hypertension - Full Text View -...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Must be on stable regimen of ACE (angiotensin converting enzyme) / ARB (angiotensin receptor blocker) treatment alone or in ... Must have a history of mild to moderate hypertension (140-179 systolic; 90-1-9 diastolic). ...
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Repurposing alpha1 Noradrenergic Antagonists for Alcoholism Treatment - Full Text View - ClinicalTrials.govRepurposing alpha1 Noradrenergic Antagonists for Alcoholism Treatment - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Double-blind, placebo-controlled, cross-over design study examining the effects of a norepinephrine alpha1 receptor antagonist ... Repurposing alpha1 Noradrenergic Antagonists for Alcoholism Treatment. The safety and scientific validity of this study is the ... The first objective of the current study is to examine norepinephrine alpha1 (NE-alpha1) receptor involvement in reactivity to ...
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A Study Investigating the Bioequivalence of the Fixed Dose Combination of COREG CR to COREG CR and ZESTRIL. - Full Text View -...A Study Investigating the Bioequivalence of the Fixed Dose Combination of COREG CR to COREG CR and ZESTRIL. - Full Text View -...
Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Vasodilator Agents. Adrenergic alpha-1 Receptor Antagonists ... History of sensitivity to carvedilol, lisinopril, alpha-blockers, beta-blockers or ACE inhibitors. ... History of asthma, COPD and/or hypersensitivity to β-adrenergic blocking agents. ... History of regular alcohol consumption exceeding 7 drinks/week for women or 14 drinks/week for men (1 drink = 5 ounces of wine ...
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LAAS (Losartan Anti-Atherosclerosis Study)(0954-330)(COMPLETED) - Full Text View - ClinicalTrials.govLAAS (Losartan Anti-Atherosclerosis Study)(0954-330)(COMPLETED) - Full Text View - ClinicalTrials.gov
Angiotensin Receptor Antagonists. Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter ... Experimental: 1 Losartan or Losartan/HCTZ. Drug: losartan potassium Once daily , Cozaar® (losartan) 50 mg, Cozaar® (losartan) ... when blood pressure is measured at Visit 1(week -2) and at Visit 2(week 0). ...
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Impedance Cardiography to Decrease the Risk of Preeclampsia - Full Text View - ClinicalTrials.govImpedance Cardiography to Decrease the Risk of Preeclampsia - Full Text View - ClinicalTrials.gov
Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Sympathomimetics. Adrenergic alpha-1 Receptor Antagonists. ... Adrenergic beta-1 Receptor Antagonists. Adrenergic beta-Antagonists. ...
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Hydralazine Versus Labetalol for the Management of Hypertensive Disorders of Pregnancy - Full Text View - ClinicalTrials.govHydralazine Versus Labetalol for the Management of Hypertensive Disorders of Pregnancy - Full Text View - ClinicalTrials.gov
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
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Effects of the Use of Adjuvant Drugs After Extracorporeal Shockwave Lithotripsy (ESWL) in Renal Calculus - Full Text View -...Effects of the Use of Adjuvant Drugs After Extracorporeal Shockwave Lithotripsy (ESWL) in Renal Calculus - Full Text View -...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Some drugs, like alpha blockers and calcium channel blockers, can improve the success rates of this procedure. Our objective is ...
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Clinical Trial to Evaluate the Antihypertensive Effect of AGSCT101 in Patient With Hypertension - Full Text View -...Clinical Trial to Evaluate the Antihypertensive Effect of AGSCT101 in Patient With Hypertension - Full Text View -...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... The purpose of this study is to evaluate the antihypertensive effect of AGSCT101 tablet in patient with stage 1 to 2 essential ... Phase III Clinical Trial to Evaluate the Antihypertensive Effect of AGSCT101 Versus Carvedilol in Patient With Stage 1 to 2 ... active clinical trial to evaluate the efficacy and safety of AGSCT101 versus Carvedilol in patient with stage 1 to 2 essential ...
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Randomized Controlled Trial of Labetalol Versus Hydralazine for Severe Hypertension in Obstetric Patients. - Full Text View -...Randomized Controlled Trial of Labetalol Versus Hydralazine for Severe Hypertension in Obstetric Patients. - Full Text View -...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... OBJECTIVES:1) To compare efficacy and severe persistent hypertension after intravenous Labetalol versus Hydralazine, within ...
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PK Comparison of GL2701 With Finasteride and Tamsulosin in Combination - Full Text View - ClinicalTrials.govPK Comparison of GL2701 With Finasteride and Tamsulosin in Combination - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... 5-alpha Reductase Inhibitors. Steroid Synthesis Inhibitors. Enzyme Inhibitors. Hormone Antagonists. Hormones, Hormone ...
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Diesel Exhaust and Vascular Function - Full Text View - ClinicalTrials.govDiesel Exhaust and Vascular Function - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... To examine role of adrenergic system a trial of alpha-blocker terazosin is also used. Each participant completes four study ... sessions, separated by at least three weeks: 1) Diesel exhaust inhalation (DE, controlled at 300 micrograms/cubic meter for two ...
clinicaltrials.gov
Study of the Medication Prazosin for Alcohol Dependence - Full Text View - ClinicalTrials.govStudy of the Medication Prazosin for Alcohol Dependence - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Clinical Trial of the Adrenergic Alpha-1 Antagonist Prazosin for Alcohol Dependence. ... Recent advances in understanding the neurobiology of substance dependence and relapse support the notion that adrenergic ...
clinicaltrials.gov
Carvedilol Versus Verapamil in Chronic Heart Failure Secondary to Non-Ischemic Cardiomyopathy - Full Text View - ClinicalTrials...Carvedilol Versus Verapamil in Chronic Heart Failure Secondary to Non-Ischemic Cardiomyopathy - Full Text View - ClinicalTrials...
Adrenergic alpha-Antagonists. Anti-Arrhythmia Agents. Calcium Channel Blockers. Membrane Transport Modulators. ... Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Therefore, we hypothesize that improvement in microvascular function by calcium antagonist, verapamil may result in additional ... the improvement in endothelial function and diminishing of subendocardial ischemia with calcium antagonists may be promising in ...
clinicaltrials.gov
The Effects of Doxazosin on the Cardiovascular and Subjective Effects of Cocaine - Full Text View - ClinicalTrials.govThe Effects of Doxazosin on the Cardiovascular and Subjective Effects of Cocaine - Full Text View - ClinicalTrials.gov
Noradrenergic α₁ receptor antagonist treatment attenuates positive subjective effects of cocaine in humans: a randomized trial ... Adrenergic alpha-1 Receptor Antagonists. Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. ... Because this class of medication needs to be titrated upward due to the potential for hypotension, treatment will begin at 1 mg ... and increased by 1 mg increments every three days until 4 mg is reached on day 12. ...
clinicaltrials.gov
Treatment of Severe Hypertension During Pre-Eclampsia: A Preliminary Equivalence Study Between Urapidil and Nicardipine - Full...Treatment of Severe Hypertension During Pre-Eclampsia: A Preliminary Equivalence Study Between Urapidil and Nicardipine - Full...
Serotonin Receptor Agonists. Serotonin Agents. Neurotransmitter Agents. Physiological Effects of Drugs. Adrenergic alpha-1 ... Urapidil (Eupressyl*) :IV (PSE) 1 microg/kg/min° until reduction PAM 15 %. Reduction ¼ of the posology to obtain PAM between ...
clinicaltrials.gov
Control of Emergence Blood Pressure During Craniotomy for Tumor Surgery Between Labetolol and Diltiazem - Full Text View -...Control of Emergence Blood Pressure During Craniotomy for Tumor Surgery Between Labetolol and Diltiazem - Full Text View -...
Adrenergic beta-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Physiological Effects of Drugs ...
clinicaltrials.gov
Prazosin Vibrostimulation Autonomic Dysreflexia and Spinal Cord Injury Study - Full Text View - ClinicalTrials.govPrazosin Vibrostimulation Autonomic Dysreflexia and Spinal Cord Injury Study - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Prazosin is an alpha-adrenergic blocker and has a slower and less abrupt suppressive effect on blood pressure. We hypothesize ...
clinicaltrials.gov
Clinical Use of Andante SmartStep System in Gait Rehabilitation - Full Text View - ClinicalTrials.govClinical Use of Andante SmartStep System in Gait Rehabilitation - Full Text View - ClinicalTrials.gov
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
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Impact of Tamsulosin on Voiding Patterns Following Early Catheter Removal After Robot-assisted Laparoscopic Radical...Impact of Tamsulosin on Voiding Patterns Following Early Catheter Removal After Robot-assisted Laparoscopic Radical...
Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ... Patients must not have a history of treatment with alpha blockers within 4 weeks ... Patients must not have hypersensitivity to trial drug or other alpha-blockers ...
clinicaltrials.gov
Chronic Postconcussive Headache: A Placebo-Controlled Treatment Trial of Prazosin - Full Text View - ClinicalTrials.govChronic Postconcussive Headache: A Placebo-Controlled Treatment Trial of Prazosin - Full Text View - ClinicalTrials.gov
Adrenergic alpha-1 Receptor Antagonists. Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. ... and angiotensin receptor blockers; magnesium prescribed specifically for headache. ... Current use of prazosin at a dose of ,2 mg or other alpha-1 antagonist for any purpose ... Allergy or previous adverse reaction to prazosin or other alpha-1 antagonist ...
clinicaltrials.gov
Pharmacogenetics of Doxazosin for Cocaine Dependence - Full Text View - ClinicalTrials.govPharmacogenetics of Doxazosin for Cocaine Dependence - Full Text View - ClinicalTrials.gov
Adrenergic alpha-1 Receptor Antagonists. Adrenergic alpha-Antagonists. Adrenergic Antagonists. Adrenergic Agents. ... which inhibits the binding of norepinephrine to alpha receptors in the autonomic nervous system. ... Doxazosin, an alpha 1-adrenergic receptor antagonist, may play an important role in cocaine addiction in humans. This study ... The NE system, especially the alpha 1-adrenergic receptor, may play an important role in cocaine addiction in humans. The ...
clinicaltrials.gov
AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and Processes
Wakefulness-Promoting AgentsReceptors, Adrenergic, alpha-2Interleukin 1 Receptor Antagonist ProteinNeurokinin-1 Receptor AntagonistsPurinergic P1 Receptor AntagonistsDose-Response Relationship, DrugRats, Sprague-DawleyHistamine H2 AntagonistsSerotonin 5-HT3 Receptor AntagonistsPiperidinesExcitatory Amino Acid AntagonistsAngiotensin Receptor AntagonistsDopamine AntagonistsSerotonin 5-HT2 Receptor AntagonistsAdenosine A2 Receptor AntagonistsHormone AntagonistsAdenosine A1 Receptor AntagonistsPurinergic P2 Receptor AntagonistsRats, WistarNarcotic AntagonistsHistamine H1 AntagonistsReceptors, EndothelinMuscarinic AntagonistsGABA-A Receptor AntagonistsAdrenergic alpha-1 Receptor AntagonistsSerotonin AntagonistsGABA AntagonistsSialoglycoproteinsHistamine AntagonistsReceptors, Adrenergic, alphaalpha 1-AntitrypsinLeukotriene AntagonistsReceptor, Endothelin AReceptors, SerotoninReceptors, N-Methyl-D-AspartateSerotonin 5-HT1 Receptor AntagonistsNicotinic AntagonistsDizocilpine MaleateReceptors, Interleukin-1Adrenergic alpha-2 Receptor AntagonistsAdrenergic alpha-AntagonistsBiphenyl CompoundsBenzazepinesTetrazolesRadioligand AssayPyridinesXanthinesGuinea PigsSerotonin Receptor AgonistsPeptides, CyclicSulfonamidesDrug InteractionsIndolesHistamine H3 AntagonistsBinding, CompetitivePyrazolesHypoxia-Inducible Factor 1, alpha SubunitQuinoxalinesCells, CulturedAzepinesTime FactorsLosartanEndothelin-1GABA-B Receptor AntagonistsSubstance Palpha7 Nicotinic Acetylcholine ReceptorSerotoninReceptors, BradykininSignal TransductionNeuronsCimetidineReceptors, Neurokinin-1Adenosine A3 Receptor AntagonistsReceptor, Endothelin BPurinergic P2X Receptor AntagonistsPiperazinesBehavior, AnimalPyrrolidinesReceptors, Adrenergic, alpha-1Interleukin-1Receptors, CholecystokininDevazepideAdrenergic AntagonistsPrazosinReceptors, ThromboxaneReceptors, VasopressinKetanserin2-Amino-5-phosphonovalerateSerotonin 5-HT4 Receptor AntagonistsElectric StimulationDisease Models, AnimalReceptor, Cannabinoid, CB1BenzimidazolesMice, Inbred C57BLReceptors, Dopamine D2AdenosineNaltrexoneInjections, IntraventricularAdrenergic alpha-AgonistsFamotidineReceptors, Neurokinin-2CalciumBradykininCannabinoid Receptor AntagonistsNaloxoneQuinuclidinesBenzodiazepinonesHistamineAdrenergic beta-2 Receptor AntagonistsBicucullineReceptors, NicotinicImidazolesInterleukin-1alphaMineralocorticoid Receptor AntagonistsReceptors, Histamine H3Blood PressureYohimbineReceptors, Opioid
DopamineSubtypesAffinitySubtypePrazosinNorepinephrinePharmacologyLigandsStimulationVasoconstrictionBlockadeMuscarinicInhibitorsAdrenoceptorBlockerAdrenoreceptorPartial agonistNoradrenalineSelectivityBindsYohimbineEpinephrineAntagonismPhenylephrineInhibitionDoxazosinVasodilationMediateInverse agonistEndogenousIntracellularInhibitInhibitorVascular smoothPotent and selectiveInhibitsActs as a selectiveSelective alpha-1 adreneNMDATamsulosinAllostericBlood vesselsBenign Prostatic HLigandNeuronsProtein coupled receptorsHistamine ReceptorsGeneBlockersInhibitoryDopaminergicNeurotransmitterSerotonin 5-HT2A recBeta-receptorsCalciumPostsynapticSympathetic nervouPathwaysBlock alpha-receptorsAdenosineCompetitive antagonistAgonist activityClonidine
Dopamine33
Subtypes18
Affinity32
Subtype15
Prazosin25
Norepinephrine23
Pharmacology3
Ligands11
Stimulation23
Vasoconstriction11
Blockade14
Muscarinic14
Inhibitors13
Adrenoceptor12
Blocker32
Adrenoreceptor9
Partial agonist5
Noradrenaline6
Selectivity6
Binds10
Yohimbine3
Epinephrine5
  • 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)
Antagonism9
Phenylephrine4
Inhibition7
Doxazosin6
Vasodilation4
Mediate6
Inverse agonist1
Endogenous2
Intracellular13
Inhibit8
Inhibitor3
Vascular smooth7
Potent and selective3
Inhibits1
Acts as a selective1
Selective alpha-1 adrene2
NMDA13
  • 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)
  • 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)
  • 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)
  • 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)
Tamsulosin12
  • Randomization (1:1) of male patients, over age 50, undergoing elective spine surgery to tamsulosin versus a placebo. (clinicaltrials.gov)
  • Subjects will be randomized 1:1 to receive either oral tamsulosin 0.4 mg or placebo, taken once each evening, beginning 5 days prior to surgery and continuing through the first postoperative day. (clinicaltrials.gov)
  • At Screening (Visit 1), subjects will enter into a 4-week open label tamsulosin hydrochloride 0.4 mg QD run-in period prior to being randomized into the 12-week double-blind treatment period (Visit 2). (clinicaltrials.gov)
  • If subjects meet all entry criteria at the end of the tamsulosin hydrochloride run-in period, subjects will be randomized to 1 of 2 treatment groups (mirabegron or placebo) for 12 weeks of treatment in addition to the continuation of tamsulosin hydrochloride 0.4 mg QD. (clinicaltrials.gov)
  • Maximum urinary flow (Qmax) will be measured at Visit 1 (Screening/tamsulosin hydrochloride run-in) and Visit 5 (Week 12/End of Treatment). (clinicaltrials.gov)
  • Post-void residual volume (PVR) will be assessed at Screening/tamsulosin hydrochloride run-in (Visit 1), Baseline (Visit 2) and at Week 4 (Visit 3), Week 8 (Visit 4), and Week 12/End of Treatment (Visit 5). (clinicaltrials.gov)
  • If all entry criteria are met, subjects will be randomised (1:1) to receive Dutasteride plus tamsulosin with lifestyle advice or watchful waiting, with lifestyle advice, with a defined escalation to tamsulosin. (clinicaltrials.gov)
  • This is especially the case for Tamsulosin and other alpha-1-a blockers, since alpha-1-a receptors are present also in the iris dilator muscle, which allows unopposed action of the parasympathetically innervated iris constrictor muscle and loss of iris tone. (wikipedia.org)
  • 5: The method of claim 1, wherein the agents comprise bromocriptine, metoprolol, and tamsulosin. (patents.com)
  • Tamsulosin, and other medications in the class called alpha blockers, work by relaxing bladder neck muscles and muscle fibers in the prostate itself and make it easier to urinate. (wikipedia.org)
  • Selective action of tamsulosin in alpha 1A/D receptors is controversial and over three quarters of tamsulosin registered human studies are unpublished. (wikipedia.org)
  • It provides less symptomatic relief than alpha-1 blockers such as tamsulosin and symptomatic relief is slower in onset (six months or more of treatment with finasteride may be required to determine the therapeutic results of treatment). (wikipedia.org)
Allosteric2
Blood vessels6
Benign Prostatic H1
  • In patients with benign prostatic hyperplasia (BPH), administration of an alpha-1 receptor antagonist decreased lower urinary tract symptoms (LUTS) and reduced the urinary ATP/creatinine ratio, with improvement of LUTS being greater in patients who had a high baseline urinary ATP level. (scirp.org)
Ligand8
Neurons8
  • Double immunostaining showed that HIF-1α was upregulated in ischemic neurons but not in astrocytes andendothelial cells. (tripdatabase.com)
  • These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. (wikipedia.org)
  • for example, α2A receptors are localized on prefrontal cortical neurons where they regulate higher cognitive function. (wikipedia.org)
  • As a consequence of this, nicotinic receptors are often cited as the receptor on the postganglionic neurons at the ganglion. (wikipedia.org)
  • Another role for these receptors is at the junction of the innervated tissues and the postganglionic neurons in the parasympathetic division of the autonomic nervous system. (wikipedia.org)
  • A possible connection has been suggested between mGluRs and neuromodulators, as mGluR1 antagonists block adrenergic receptor activation in neurons. (wikipedia.org)
  • 1) It mediates hyperalgesia due to EP11 receptors located in the central nervous system but suppresses pain perception due to E1 located on dorsal root ganglia neurons in rats. (wikipedia.org)
  • Its receptor - the neurokinin type 1 - is distributed over cytoplasmic and nuclear membranes of many cell types (neurons, glia, endothelia of capillaries and lymphatics, fibroblasts, stem cells, white blood cells) in many tissues and organs. (wikipedia.org)
Protein coupled receptors5
Histamine Receptors1
  • Considering the range of its therapeutic concentrations (e.g., 63-271 nM at 90 mg/day), only the actions of iprindole on the 5-HT2 and histamine receptors might be anticipated to be of possible clinical significance. (wikipedia.org)
Gene15
Blockers21
Inhibitory3
Dopaminergic3
Neurotransmitter5
Serotonin 5-HT2A rec1
Beta-receptors3
Calcium14
  • Therefore, we hypothesize that improvement in microvascular function by calcium antagonist, verapamil may result in additional clinical benefit. (clinicaltrials.gov)
  • Accordingly, coronary endothelial dysfunction at the microvascular and epicardial level in patients with acute-onset idiopathic dilated cardiomyopathy and chronic congestive heart failure has been reported (3,4) Thus, taking all mentioned above into account, the improvement in endothelial function and diminishing of subendocardial ischemia with calcium antagonists may be promising in terms of using these drugs for therapy of patients with stable chronic heart failure. (clinicaltrials.gov)
  • Thus, taking all mentioned above into account, the improvement in endothelial function and diminishing of subendocardial ischemia with calcium antagonists may be promising in terms of using these drugs for therapy of patients with stable chronic heart failure. (clinicaltrials.gov)
  • Very little data exists about the pharmacological properties, metabolism, and toxicity of 2C-H. It exhibits agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with Galpha16 protein assessed as internal calcium mobilization. (wikipedia.org)
  • Role of the sympathetic nervous system in blood pressure maintenance and in the antihypertensive effects of calcium antagonists in spontaneously hypertensive rats. (ahajournals.org)
  • Specifically, α1 receptors are characterized as Gq GPCRs, signaling through Phospholipase C to increase IP3 and DAG, thus increasing the release of calcium. (wikipedia.org)
  • This receptor is directly associated with one of its ultimate effectors, the class C L-type calcium channel CaV1.2. (wikipedia.org)
  • The RYR2 ryanodine receptor isoform is the major cellular mediator of calcium-induced calcium release (CICR) in animal cells. (wikipedia.org)
  • In non-metazoan species, calcium-release channels with sequence homology to RyRs can be found, but they are shorter than the mammalian ones and may be closer to IP3 Receptors. (wikipedia.org)
  • In skeletal muscle, activation of ryanodine receptors occurs via a physical coupling to the dihydropyridine receptor (a voltage-dependent, L-type calcium channel), whereas, in cardiac muscle, the primary mechanism of activation is calcium-induced calcium release, which causes calcium outflow from the sarcoplasmic reticulum. (wikipedia.org)
  • It has been shown that calcium release from a number of ryanodine receptors in a ryanodine receptor cluster results in a spatiotemporally restricted rise in cytosolic calcium that can be visualised as a calcium spark. (wikipedia.org)
  • Ryanodine receptors are very close to mitochondria and calcium release from RyR has been shown to regulate ATP production in heart and pancreas cells. (wikipedia.org)
  • a small amount of Ca2+ in the cytosol near the receptor will cause it to release even more Ca2+ (calcium-induced calcium release/CICR). (wikipedia.org)
  • Alpha-1D subunits belong to the Cav1 family, which is characterised by L-type calcium currents. (wikipedia.org)
Postsynaptic3
Sympathetic nervou1
  • Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system. (wikipedia.org)
Pathways2
Block alpha-receptors2
Adenosine8
Competitive antagonist4
Agonist activity2
Clonidine2