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*  5-HT2B receptor
Lin Z, Walther D, Yu XY, Drgon T, Uhl GR (Dec 2004). "The human serotonin receptor 2B: coding region polymorphisms and ... receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide)". The Journal ... also known as serotonin receptor 2B is a protein that in humans is encoded by the HTR2B gene. 5-HT2B is a member of the 5-HT2 ... serotonin) receptor 2B". Schmuck K, Ullmer C, Engels P, Lübbert H (Mar 1994). "Cloning and functional characterization of the ...
*  5-HT receptor
Smriga M, Torii K (2003). "L-Lysine acts like a partial serotonin receptor 4 antagonist and inhibits serotonin-mediated ... The 7 general serotonin receptor classes include a total of 14 known serotonin receptors. The specific types have been ... The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin ... The genes coding for serotonin receptors are expressed across the mammalian brain. Genes coding for different receptors types ...
*  5-HT2C receptor agonist
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 ...
*  Pirenperone
... (INN, USAN, BAN; developmental code names R-47456, R-50656) is a serotonin receptor antagonist described as an ... It is a relatively selective antagonist of the serotonin 5-HT2 receptors and has been used in scientific research to study the ... serotonin system. In the 1980s, the drug was found to block the effects of the lysergic acid diethylamide (LSD) in animals, and ... led to the elucidation of the 5-HT2A receptor as the biological mediator of the effects of serotonergic psychedelics. J. Elks ( ...
*  Quinupramine
... 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 3-527-31058-4. Sakamoto H, Yokoyama N, Kohno S, Ohata K (December 1984). "Receptor binding profile of quinupramine, a new ... It has negligible affinity for the α1-adrenergic, α2-adrenergic, β-adrenergic, or D2 receptor. Clinically, quinupramine is ...
*  Serotonin-dopamine reuptake inhibitor
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 ... CS1 maint: Multiple names: authors list (link) Media related to Serotonin-dopamine reuptake inhibitors at Wikimedia Commons. ... This in turn leads to increased extracellular concentrations of serotonin and dopamine, and, therefore, an increase in ...
*  Cyproheptadine
Of the serotonin receptors, it is an especially potent antagonist of the 5-HT2 receptors, and this underlies its effectiveness ... in the treatment of serotonin syndrome. Cyproheptadine is known to be an antagonist or inverse agonist of all of the receptors ... Cyproheptadine is a very potent antihistamine or antagonist of the H1 receptor. At higher concentrations, it also has ... such as selective serotonin reuptake inhibitors and monoamine oxidase inhibitors), and in cases of high levels of serotonin in ...
*  Iprindole
Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal ... Tsai BS, Yellin TO (1984). "Differences in the interaction of histamine H2 receptor antagonists and tricyclic antidepressants ... Kanba S, Richelson E (1983). "Antidepressants are weak competitive antagonists of histamine H2 receptors in dissociated brain ... "Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor". Psychopharmacology. 126 (3): 234- ...
*  Aptazapine
It is a potent α2-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been ... while having no significant effects on the reuptake of serotonin or norepinephrine. Based on its pharmacological profile, ... January 1983). "CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist". Life Sciences. 32 (4): 355-63. doi:10.1016 ... shown to act as a 5-HT2 receptor antagonist and H1 receptor inverse agonist, ...
*  Sarpogrelate
... serotonin receptor important for sarpogrelate binding. Journal of Pharmacological Sciences. 2007 Jul;104(3):274-7. PMID ... 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 Thérapie. 1996 Mar-Apr; ... a specific 5HT2-receptor antagonist, improves the coronary microcirculation in coronary artery disease. Clinical Cardiology. ...
*  Cinanserin
"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 preparation is effective ...
*  Glemanserin
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 ...
*  Chlorphenamine
In addition to being a histamine H1 receptor antagonist, chlorphenamine has been found to act as a potent serotonin reuptake ... a preferred ligand for in vitro and in vivo characterization of serotonin receptors". J. Neurochem. 48 (1): 115-24. doi:10.1111 ... "Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole". FEBS ... has been reported to possess Kd values of 15 nM for the H1 receptor and 1,300 nM for the muscarinic acetylcholine receptors in ...
*  Tricyclic antidepressant
With the exception of the sigma receptors, the TCAs act as antagonists or inverse agonists of the receptors and as inhibitors ... "Interactions of selective serotonin reuptake inhibitors with subtypes of sigma receptors in rat brain". European Journal of ... 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 ...
*  LY-215,840
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 ...
*  Oxaprotiline
... 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 ...
*  Problem gambling
The opioid antagonist drug nalmefene has also been trialled quite successfully for the treatment of compulsive gambling. Other ... Deficiencies in serotonin might also contribute to compulsive behavior, including a gambling addiction. There are three ... The DSM-5 has re-classified the condition as an addictive disorder, with sufferers exhibiting many similarities to those who ... In the DSM-5, the term addiction is synonymous with the classification of severe substance-use disorder. Ministerial Council on ...
*  Nefazodone
It has been described as a serotonin antagonist and reuptake inhibitor (SARI) due to its combined actions as a potent serotonin ... It also has high affinity for the α1-adrenergic receptor and serotonin 5-HT1A receptor, and relatively lower affinity for the ... Nefazodone acts primarily as a potent antagonist of the serotonin 5-HT2A receptor and to a lesser extent of the serotonin 5- ... α2-adrenergic receptor and dopamine D2 receptor. Nefazodone has low but significant affinity for the serotonin, norepinephrine ...
*  Butriptyline
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 ... The chemical name of butriptyline is 3-(10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-yl)-N,N,2-trimethylpropan-1-amine and its ...
*  International nonproprietary name
Examples are: -anib for angiogenesis inhibitors (e.g. pazopanib) -anserin for serotonin receptor antagonists, especially 5-HT2 ... sartan for angiotensin II receptor antagonists (e.g. losartan) -tinib for tyrosine kinase inhibitors (e.g. imatinib) -vastatin ... antagonists (e.g. ritanserin and mianserin) -arit for antiarthritic agents (e.g. lobenzarit) -ase for enzymes (e.g. alteplase ...
*  Head-twitch response
... atropine and cannabinoid receptor antagonists. As well, compounds such as 5-HTP, fenfluramine and 1-Methylpsilocin can also ... The head-twitch response (HTR) is a rapid side-to-side head movement that occurs in mice and rats after the serotonin 5-HT2A ... produce head twitch and do stimulate serotonin receptors, but are not hallucinogenic in humans. This means that while the head ... Also, the effect can be non-specific, with head twitch responses also produced by some drugs that do not act through 5-HT2 ...
*  5-HT1A receptor
... by NK1 receptor inhibition. Consequently, novel NK1 receptor antagonists are now in use for the treatment of nausea and emesis ... The serotonin 1A receptor is encoded by the HTR1A gene. The 5-HT1A receptor is the most widespread of all the 5-HT receptors. ... The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor (5-HT receptor) that binds the ... Parks CL, Shenk T (1996). "The serotonin 1a receptor gene contains a TATA-less promoter that responds to MAZ and Sp1". J. Biol ...
*  Setiptiline
... acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, ... 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] ...
*  TGBA01AD
... (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 ... doi:10.1007/s40290-013-0007-5. ISSN 1178-2595. AdisInsight: TGBA01AD PubChem Substance FKB01MD (TGBA01AD) - AdisInsight. ...
*  Dosulepin
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 ... Dosulepin is a transporter blocker of the serotonin transporter (SERT) and the norepinephrine transporter (NET), thereby acting ...
*  List of investigational anxiolytics
... and α1-adrenergic receptor antagonist [12] Midomafetamine (MDMA; "ecstasy") - serotonin-norepinephrine-dopamine releasing agent ... atypical μ-opioid receptor agonist [14] Verucerfont (GSK-561679, NBI-77860) - CRF1 receptor antagonist [15] 4-Androstadienol ( ... vasopressin V1A receptor antagonist [25] List of investigational drugs Garakani, Amir; Murrough, James W.; Iosifescu, Dan V. ( ... and H1 receptor antagonist [10] Cyclobenzaprine (TNX-102) - undefined mechanism of action [11] Iloperidone (HP-873, ILO-522; ...
*  Chlorprothixene
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Wander TJ, Nelson A, Okazaki H, Richelson E (1987). "Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of ... Chlorprothixene is an antagonist of the following receptors: 5-HT2: antipsychotic effects, anxiolysis, weight gain D1, D2, D3: ... I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes". Methods Find ...