Of the serotonin receptors, it is an especially potent antagonist of the 5-HT2 receptors. This is thought to underlie its ... a potent in vivo serotonin antagonist". The American Journal of Psychiatry. 154 (6): 884a-884. doi:10.1176/ajp.154.6.884a. PMID ... such as selective serotonin reuptake inhibitors (and monoamine oxidase inhibitors), and in cases of high levels of serotonin in ... Dopamine antagonists, Local anesthetics, Muscarinic antagonists, Piperidines, 5-HT2 antagonists, Serotonin receptor antagonists ...

H1 receptor antagonists, Local anesthetics, Muscarinic antagonists, 2-Pyridyl compounds, Serotonin reuptake inhibitors, Sigma ... In addition to acting as an inverse agonist at the H1 receptor, chlorphenamine has been found to act as a serotonin reuptake ... a preferred ligand for in vitro and in vivo characterization of serotonin receptors". Journal of Neurochemistry. 48 (1): 115- ... "Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole". FEBS ...

"Serotonin (5-HT2) receptor mediated enhancement of cortical unit activity". Canadian Journal of Physiology and Pharmacology. 70 ... Cinanserin (INN) is a 5-HT2A and 5-HT2C receptor antagonist which was discovered in the 1960s. The molecule is an inhibitor of ... 5-HT2A antagonists, 5-HT2C antagonists, Thioethers, Anilides, Abandoned drugs, All stub articles, Nervous system drug stubs). ...

A closely related type of drug is a serotonin-dopamine releasing agent (SDRA). Relative to serotonin-norepinephrine-dopamine ... A serotonin-dopamine reuptake inhibitor (SDRI) is a type of drug which acts as a reuptake inhibitor of the monoamine ... This in turn leads to increased extracellular concentrations of serotonin and dopamine, and, therefore, an increase in ... Rothman RB, Blough BE, Baumann MH (2007). "Dual dopamine/serotonin releasers as potential medications for stimulant and alcohol ...

... is a serotonin receptor antagonist described as an antipsychotic and tranquilizer which was never marketed. It is a relatively ... selective antagonist of the serotonin 5-HT2 receptors and has been used in scientific research to study the serotonin system. ... led to the elucidation of the 5-HT2A receptor as the biological mediator of the effects of serotonergic psychedelics. ... 5-HT2 antagonists, Antipsychotics, Anxiolytics, Fluoroarenes, Ketones, Piperidines, Pyridopyrimidines, All stub articles, ...

January 1988). "Preclinical pharmacology of a new serotonergic receptor antagonist, LY281067". The Journal of Pharmacology and ... is an ergoline derivative which acts as a selective antagonist of the serotonin 5-HT2 receptors. It has been used for various ... synergistic interaction between serotonin and low density lipoproteins". Journal of the American College of Cardiology. 34 (5 ... Cohen ML, Parli CJ, Fuller RW (December 1989). "5-Hydroxytryptamine2 receptor antagonist activity of the acid metabolite (1- ...

Berend Olivier (10 July 1997). Serotonin Receptors and Their Ligands. Elsevier. p. 167. ISBN 978-0-444-82041-9. Retrieved 6 May ... 1988). "Pharmacological effects of MDL 11,939: A selective, centrally acting antagonist of 5-HT2 receptors". Drug Development ... Sramek JJ, Robinson RE, Suri A, Cutler NR (February 1995). "Efficacy trial of the 5-HT2 antagonist MDL 11,939 in patients with ... The first truly selective 5-HT2A ligand to be discovered, glemanserin resulted in the development of the widely used and even ...

... as well as a very weak α1-adrenergic receptor antagonist. It has negligible affinity for the serotonin transporter, dopamine ... or D2 receptors like its relative maprotiline is unclear. Levoprotiline acts as a selective H1 receptor antagonist, with no ... Dextroprotiline acts as a potent norepinephrine reuptake inhibitor and H1 receptor antagonist, ... or serotonin receptors, or any of the monoamine transporters. Oxaprotiline is a racemic compound composed of two isomers, R ...

In the late 1960s, non-selective serotonin receptor antagonists demonstrated a relationship between serotonin receptors and ... Later, animal studies showed that serotonin receptor agonists might act as a mediator of satiety. Serotonin has been implicated ... "The structure of human serotonin 2c G-protein-coupled receptor bound to agonists and antagonists". Journal of Molecular ... When serotonin binds to the receptors, the most important contacts are in TM helixes 3, 5 and 6 (Figure 3), while the other ...

... serotonin receptor important for sarpogrelate binding". Journal of Pharmacological Sciences. 104 (3): 274-7. doi:10.1254/jphs. ... a specific 5HT2-receptor antagonist, improves the coronary microcirculation in coronary artery disease". Clinical Cardiology. ... "The effect of a 5HT2 receptor antagonist sarpogrelate (MCI-9042) treatment on platelet function in Buerger's disease". ... and its metabolite for serotonin receptor subtypes". Archives Internationales de Pharmacodynamie et de Therapie. 331 (2): 189- ...

... (developmental code name CGS-15040A) is a serotonin 5-HT2 receptor antagonist that was investigated as a potential ... 1 July 1993). "Serotonergic (5-HT2) mediation of anxiety-therapeutic effects of serazepine in generalized anxiety disorder". ... 5-HT2 antagonists, Abandoned drugs, Anxiolytics, Heterocyclic compounds with 5 rings, Nitrogen heterocycles, Methyl esters). ...

Articles with short description, Short description matches Wikidata, Serotonin receptors). ... Serotonin)". Pharmacol. Rev. 46 (2): 157-203. PMID 7938165. Eison AS, Mullins UL (1996). "Regulation of central 5-HT2A ... "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine ( ... receptors: a review of in vivo studies". Behavioural Brain Research. 73 (1-2): 177-81. doi:10.1016/0166-4328(96)00092-7. PMID ...

2 receptor antagonist, blocks vascular and platelet 5-HT2 receptors and delays occlusion in a rabbit model of thrombosis". The ... which acts as a potent and selective antagonist at the serotonin 5-HT2 and 5-HT7 receptors. It has anti-hypertensive and muscle ... "Activation of Erk mitogen-activated protein kinase proteins by vascular serotonin receptors". Journal of Cardiovascular ... receptor in rat glomerulosa cells is associated with an increase in adenylyl cyclase activity and calcium influx through T-type ...

The opioid antagonist drug nalmefene has also been trialled quite successfully for the treatment of compulsive gambling. Group ... Deficiencies in serotonin might also contribute to compulsive behavior, including a gambling addiction. There are three ... There is some evidence to suggest that opioid antagonists, for example, naltrexone or nalmefene, and atypical antipsychotics ... and opioid antagonists, however the best approach for treatment, treatment regime including dosage and timing is not clear. ...

H1 receptor antagonists, Muscarinic antagonists, Serotonin receptor antagonists, Tricyclic antidepressants). ... Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal ... These actions appear to confer a profile similar to that of iprindole and trimipramine with serotonin-blocking effects as the ... 114-. ISBN 978-3-7186-5027-9. Richelson E, Nelson A (1984). "Antagonism by antidepressants of neurotransmitter receptors of ...

... quinupramine acts in vitro as a strong muscarinic acetylcholine receptor antagonist (anticholinergic) and H1 receptor ... It can be inferred that its in vivo metabolites may have stronger effects on the reuptake of norepinephrine and/or serotonin ... ISBN 978-3-527-31058-6. Sakamoto H, Yokoyama N, Kohno S, Ohata K (December 1984). "Receptor binding profile of quinupramine, a ... It has negligible affinity for the α1-adrenergic, α2-adrenergic, β-adrenergic, or D2 receptor. Clinically, quinupramine is ...

Examples are: -anib for angiogenesis inhibitors (e.g. pazopanib) -anserin for serotonin receptor antagonists, especially 5-HT2 ... for cannabinoid receptor agonists (e.g. cannabidiol,[citation needed] dronabinol) -nabant for cannabinoid receptor antagonists ... antagonists (e.g. ritanserin and mianserin) -ant for various receptors antagonists (e.g. aticaprant and rimonabant) -arit for ... sartan for angiotensin II receptor antagonists (e.g. losartan) -tinib for tyrosine kinase inhibitors (e.g. imatinib) -vastatin ...

H1 receptor antagonists, Noradrenergic and specific serotonergic antidepressants, Serotonin receptor antagonists, Tetracyclic ... It is a potent α2-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been ... January 1983). "CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist". Life Sciences. 32 (4): 355-63. doi:10.1016 ... while having no significant effects on the reuptake of serotonin or norepinephrine. Based on its pharmacological profile, ...

Wander TJ, Nelson A, Okazaki H, Richelson E (December 1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of ... Tsai BS, Yellin TO (November 1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic ... Kanba S, Richelson E (October 1983). "Antidepressants are weak competitive antagonists of histamine H2 receptors in dissociated ... H1 receptor antagonists, Indoles, Tricyclic antidepressants, Heterocyclic compounds with 3 rings). ...

With the exception of the sigma receptors, the TCAs act as antagonists or inverse agonists of the receptors and as inhibitors ... through interfering with the reuptake of serotonin and acting as antagonists to SHAM (serotonin, histamine, alpha, muscarinic) ... Tsai BS, Yellin TO (November 1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic ... and NMDA receptors, and as agonists at the sigma receptors (σ1 and σ2), some of which may contribute to their therapeutic ...

Agonist and antagonist properties at subtypes of dopamine D2-like receptor and α1/α2-adrenoceptor". The Journal of Pharmacology ... Agonist and antagonist properties at serotonin, 5-HT1 and 5-HT2, receptor subtypes". The Journal of Pharmacology and ... D1-receptor agonists, D2-receptor agonists, D3 receptor agonists, D4 receptor agonists, D5 receptor agonists, Erectile ... Dopamine antagonists, by their nature of competing for sites at dopamine receptors, reduce the effectiveness of the agonistic ...

... acts primarily as a potent antagonist of the serotonin 5-HT2A receptor and to a lesser extent of the serotonin 5- ... HT2C receptor. It also has high affinity for the α1-adrenergic receptor and serotonin 5-HT1A receptor, and relatively lower ... It has been described as a serotonin antagonist and reuptake inhibitor (SARI) due to its combined actions as a potent ... affinity for the α2-adrenergic receptor and dopamine D2 receptor. Nefazodone has low but significant affinity for the serotonin ...

Serotonin receptor agonists, Tryptamines, Indole ethers at the benzene ring, All stub articles, Nervous system drug stubs). ... and an antagonist of TRPM8. 5-Benzyloxytryptamine is illegal in Singapore. 5-Carboxamidotryptamine 5-Methoxytryptamine BW- ... 5-Benzyloxytryptamine (5-BT), is a tryptamine derivative which acts as an agonist at the 5-HT1D, 5-HT2 and 5-HT6 serotonin ... 36 (4-5): 713-720. doi:10.1016/S0028-3908(97)00019-1. PMID 9225298. S2CID 41813873. DeFalco J, Steiger D, Dourado M, Emerling D ...

... (also known as FKB01MD) is a serotonin reuptake inhibitor, 5-HT1A and 5-HT1D receptor agonist, and 5-HT2 receptor ... antagonist which is under development by Fabre-Kramer for the treatment of major depressive disorder. It has been in phase II ... Serotonin reuptake inhibitors, All stub articles, Nervous system drug stubs). ... doi:10.1007/s40290-013-0007-5. ISSN 1178-2595. S2CID 16286323. "TGBA01AD". AdisInsight. Springer Nature Switzerland AG. v t e ( ...

"Serotonin receptors in the human brain--IV. Autoradiographic mapping of serotonin-2 receptors". Neuroscience. 21 (1): 123-139. ... D1 antagonists, D2 antagonists, Fluoroarenes, H1 receptor antagonists, Imides, Janssen Pharmaceutica, Ketones, Piperidines, ... 23-. ISBN 978-0-12-801083-9. Olivier B, van Wijngaarden I, Soudijn W (10 July 1997). Serotonin Receptors and their Ligands. ... in receptor binding assays and autoradiography. This radio-labeling has enabled the study of serotonin 5-HT2A receptor ...

Are Potent Antagonists of Human Serotonin Receptor 2a (5HT2a), Histamine Receptor H-1 and á-Adrenergic Receptors: Mechanistic ... The sedative effects of cyclobenzaprine are likely due to its antagonistic effect on histamine, serotonin, and muscarinic ... Keegan MT, Brown DR, Rabinstein AA (December 2006). "Serotonin syndrome from the interaction of cyclobenzaprine with other ... At least one study also found increased risk of serotonin syndrome when cyclobenzaprine was taken with the serotonergic drugs ...

... by NK1 receptor inhibition. Consequently, novel NK1 receptor antagonists are now in use for the treatment of nausea and emesis ... In humans, the serotonin 1A receptor is encoded by the HTR1A gene. The 5-HT1A receptor is the most widespread of all the 5-HT ... The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin, ... de Almeida J, Mengod G (October 2008). "Serotonin 1A receptors in human and monkey prefrontal cortex are mainly expressed in ...

... atropine and cannabinoid receptor antagonists. As well, compounds such as 5-HTP, fenfluramine, 1-Methylpsilocin, Ergometrine, ... can also produce head twitch and do stimulate serotonin receptors, but are not hallucinogenic in humans. This means that while ... The head-twitch response (HTR) is a rapid side-to-side head movement that occurs in mice and rats after the serotonin 5-HT2A ... Also, the effect can be non-specific, with head twitch responses also produced by some drugs that do not act through 5-HT2 ...

... acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, ... H1 receptor antagonists, Noradrenergic and specific serotonergic antidepressants, Piperidines, Serotonin receptor antagonists, ... as well as an H1 receptor inverse agonist/antihistamine.[additional citation(s) needed] Setiptiline has a tetracyclic structure ... likely at the 5-HT2 subtypes,[citation needed] ...

Muscarinic antagonists, Serotonin receptor antagonists, Serotonin-norepinephrine reuptake inhibitors, Sodium channel blockers, ... It is also an antagonist of the histamine H1 receptor, α1-adrenergic receptor, serotonin 5-HT2 receptors, and muscarinic ... Richelson E, Nelson A (1984). "Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro". J. ... Cusack B, Nelson A, Richelson E (1994). "Binding of antidepressants to human brain receptors: focus on newer generation ...