*  Amitriptyline - Wikipedia
... and as an agonist of the sigma σ1 receptor. It has also been shown to be a relatively weak NMDA receptor antagonist via the ... "Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor". Psychopharmacology. 126 (3): 234- ... the α1-adrenergic receptor, the histamine H1 and H2 receptors, and the muscarinic acetylcholine receptors, ... Amitriptyline additionally acts as an antagonist or inverse agonist of the serotonin 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, and 5-HT7 ...
  https://en.wikipedia.org/wiki/Amitriptyline
*  Central nervous control of energy and glucose balance: focus on the central melanocortin system
Serotonin 2C receptor agonists improve type 2 diabetes via melanocortin-4 receptor signaling pathways. Cell Metab. 2007;6:398- ... Selective loss of leptin receptors in the ventromedial hypothalamic nucleus results in increased adiposity and a metabolic ... AgRP is the endogenous antagonist of the melanocortin receptors.1-3 POMC and NPY/AgRP populations have been long believed to be ... 138 At least 14 serotonin receptors have been cloned, and many of these receptors have been implicated in the regulation of ...
  http://pubmedcentralcanada.ca/pmcc/articles/PMC3467098/
*  5-HT receptor - Wikipedia
... receptors, agonists and antagonists By Flavio Guzmán, M.D. on 9/08/09 "BRINTELLIX™ (vortioxetine) tablets for oral use. Full ... Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, Fujimiya M, Inui A (2009). "Selective serotonin reuptake ... The 7 general serotonin receptor classes include a total of 14 known serotonin receptors. The specific types have been ... Smriga M, Torii K (2003). "L-Lysine acts like a partial serotonin receptor 4 antagonist and inhibits serotonin-mediated ...
  https://en.wikipedia.org/wiki/5-HT_receptor
*  Pruvanserin - Wikipedia
... a selective serotonin 2A receptor antagonist on anxiety induced by predator stress in rats". European Journal of Pharmacology. ... inverse-agonists for the treatment of insomnia". Current Topics in Medicinal Chemistry. 8 (11): 969-76. doi:10.2174/ ... Terry AV, Buccafusco JJ, Bartoszyk GD (June 2005). "Selective serotonin 5-HT2A receptor antagonist EMD 281014 improves delayed ... a new selective serotonin 5-HT2A receptor antagonist". European Journal of Pharmacology. 473 (2-3): 229-30. doi:10.1016/S0014- ...
  https://en.wikipedia.org/wiki/Pruvanserin
*  China White Powder Factory Supply Agomelatine CAS: 138112-76-2 - China Agomelatine, Pharmaceutica Intermediates
Agomelatine is a melatoninergic agonist and selective antagonist of 5-HT2C receptors, and has been shown to be active in ... Agomelatine (S20098) displayed pKi values of 6.4 and 6.2 at native (porcine) and cloned, human (h)5-hydroxytryptamine (5-HT)2C ... It is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. Activation of 5 ... HT2C receptors by serotonin inhibits dopamine and norepinephrine release. ...
  http://simeiquan.en.made-in-china.com/product/zKixwDkYEdhl/China-White-Powder-Factory-Supply-Agomelatine-CAS-138112-76-2.html
*  5-HT2C receptor agonist - Wikipedia
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 ... Serotonin is an endogenous non-selective agonist for the 5-HT2C receptor with a binding constant of Ki = 16.0 nM. When ...
  https://en.wikipedia.org/wiki/5-HT2C_receptor_agonist
*  List of antidepressants - Wikipedia
... non-selective serotonin receptor agonist, SNDRA, and weak RIMA Indeloxazine (Elen, Noin) - serotonin releasing agent (SRA), NRI ... also a non-competitive antagonist of nicotinic acetylcholine receptors Amineptine (Survector, Maneon) and nomifensine (Merital ... non-selective serotonin receptor agonist, serotonin-norepinephrine-dopamine releasing agent (SNDRA), and weak RIMA Etryptamine ... and NMDA receptor antagonist Medifoxamine (Clédial, Gerdaxyl) - weak serotonin-dopamine reuptake inhibitor (SDRI) and 5-HT2A ...
  https://en.wikipedia.org/wiki/List_of_antidepressants
*  BW-723C86 - Wikipedia
"A Novel Role of Serotonin Receptor 2B Agonist as an Anti-Melanogenesis Agent". International Journal of Molecular Sciences. 17 ... it is around only 3 times as selective for 2B compared to 2C and so is much less selective than most research ligands, but no ... Highly selective 5-HT2C antagonists are available however, and so a combination of BW-723C86 with a selective 5-HT2C antagonist ... It has anxiolytic effects in animal studies, and is also used for investigating the function of the 5-HT2B receptor in a range ...
  https://en.wikipedia.org/wiki/BW-723C86
*  5-HT(2C) antagonism blocks blood oxygen level-dependent pharmacological-challenge magnetic resonance imaging signal in rat...
... receptor antagonists, SB 224289 (2.5 mg/kg) and SB 242084 (2 mg/kg), respectively. Subcutaneous injection of mCPP (3 mg/kg) ... agonist m-chlorophenylpiperazine (mCPP) challenge with pre-treatment with the selective 5-HT(1B) and 5-HT(2C) ... pharmacological-challenge magnetic resonance imaging was used to further characterize the central action of serotonin on ... receptor antagonist but was partially reversed by the 5-HT(2C) receptor antagonist. mCPP alone induced both positive and ...
  https://www.ndcn.ox.ac.uk/publications/106546
*  Pimavanserin - Wikipedia
... pimanvaserin is not a dopamine receptor antagonist, and instead acts as a highly selective antagonist of the serotonin 5-HT2A ... receptor. Pimavanserin acts as an inverse agonist and antagonist at serotonin 5-HT2A receptors with high binding affinity (Ki ... Pimavanserin shows low binding to σ1 receptors (Ki 120 nM) and has no appreciable affinity (Ki >300 nM) to serotonin 5-HT2B, ... behaving as a selective inverse agonist of the serotonin 5-HT2A receptor, with 40-fold selectivity for this site over the 5- ...
  https://en.wikipedia.org/wiki/Pimavanserin
*  SuperBiHelix method for predicting the pleiotropic ensemble of G-protein-coupled receptor conformations | PNAS
... it was found that all four selective agonists preferred the 15th WT conformation, whereas the four selective antagonists all ... and other adenosine receptors (22), serotonin 5-HT2B and 5-HT2C receptor (25), the histamine H3 receptor (26), the CCR5 ... 2011) Predicted structures of agonist and antagonist bound complexes of adenosine A3 receptor. Proteins 79(6):1878-1897. ... 16) found for the A3 adenosine receptor that the optimum conformation for binding four selective agonists was the 15th in the ...
  http://www.pnas.org/content/111/1/E72
*  5-HT2A receptor - Wikipedia
Design and Synthesis of Selective Serotonin Receptor Agonists for Positron Emission Tomography Imaging of the Brain. University ... as well as an antagonist on other serotonin receptors. Mirtazapine is a 5-HT2A, 5-HT2C, and 5-HT3 antagonist. Mirtazapine also ... Serotonin): Receptor Agonists and Antagonists". In Brunton LL, Lazo JS, Parker K. Goodman & Gilman's the Pharmacological Basis ... a selective serotonin 2A receptor inverse agonist". The Journal of Pharmacology and Experimental Therapeutics. 310 (3): 943-51 ...
  https://en.wikipedia.org/wiki/5-HT2A_receptor
*  Serotonin and the 5-HT2B Receptor in the Development of Enteric Neurons | Journal of Neuroscience
1996) Potent, selective, tetrahydro-β-corboline antagonists of the 5-HT2B (5-HT2B) contractile receptor in the rat stomach ... receptors are expressed in the fetal mouse gut. Receptor expression in fetal and adult bowel was analyzed by RT-PCR. The size ... and the effects of both agonists are blocked by SB206553. (2) mRNA encoding the 5-HT2B receptor was detected by RT-PCR in ... 1989) Ectopic expression of the serotonin 1c receptor and the triggering of malignant transformation. Science 244:1057-1062. ...
  http://www.jneurosci.org/content/20/1/294
*  Buspirone - Wikipedia
In addition to binding to serotonin receptors, buspirone is an antagonist of the dopamine D2 receptor with weak affinity. It ... However, buspirone has been reported to have shown "significant and selective intrinsic efficacy" at the α1-adrenergic receptor ... it is not a GABA receptor agonist), and so buspirone does not carry the risk of physical dependence and withdrawal symptoms for ... Plassat JL, Amlaiky N, Hen R (1993). "Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase". ...
  https://en.wikipedia.org/wiki/Buspirone
*  Functional selectivity - Wikipedia
... antagonist or more recently an inverse agonist through a specific receptor subtype, and that this characteristic will be ... is a functionally selective agonist at this receptor, activating phospholipase C (which leads to inositol triphosphate ... A number of biased agonists, such as those at opioid receptors that mediate pain, show potential at various receptor families ... Serotonin, the main endogenous ligand of 5-HT receptors, ... "Agonist-Receptor Efficacy. II. Agonist Trafficking of Receptor ...
  https://en.wikipedia.org/wiki/Functional_selectivity
*  PRX-08066 - Wikipedia
Patent US 7,030,240 B2], which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with a 5-HT2B ... receptor plays a key regulatory role in both neuroendocrine tumor cell proliferation and the modulation of the fibroblast ... PRX-08066 and other selective 5-HT2B antagonists are being researched for the treatment of pulmonary arterial hypertension, ... Svejda B, Kidd M, Giovinazzo F, Eltawil K, Gustafsson BI, Pfragner R, Modlin IM (June 2010). "The 5-HT(2B) ...
  https://en.wikipedia.org/wiki/PRX-08066
*  Serotonin receptor antagonist - Wikipedia
Please note, that although some non-selective serotonin antagonists may have an particular affinity for a specific 5-HT ... and many other organs and has been used in hypertension and psychosis Serotonin receptor agonist Lindley, C.; Blower, P. (2000 ... dopamine receptors D1 and D2, histamine receptor H1, and A1 adrenoreceptors. Ketanserin Antihypertensive. Blocks 5-HT2A, 5-HT2C ... A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action at serotonin (5-HT) receptors. ...
  https://en.wikipedia.org/wiki/Serotonin_receptor_antagonist
*  Mirtazapine - Wikipedia
It is specifically a potent antagonist or inverse agonist of the α2A-, α2B-, and α2C-adrenergic receptors, the serotonin 5-HT2A ... Antagonism of the H1 receptor is by far the strongest activity of mirtazapine, with the drug acting as a selective H1 receptor ... This is in accordance with the fact that it is not a serotonin reuptake inhibitor or MAOI, nor a serotonin receptor agonist. ... The drug acts as an antagonist of certain adrenergic and serotonin receptors, and is also a strong antihistamine. It is ...
  https://en.wikipedia.org/wiki/Mirtazapine
*  Serotonin antagonist and reuptake inhibitor - Wikipedia
... and H1 receptors, as partial agonists of the 5-HT1A receptor, and as inhibitors of the transporters. mCPP is an antagonist of ... Selective Serotonin Reuptake Inhibitor (SSRI) Gainsborough N, Nelson ML, Maskrey V, Swift CG, Jackson SH (1994). "The ... Serotonin antagonist and reuptake inhibitors (SARIs) are a class of drugs used mainly as antidepressants, but also as ... They act by antagonizing serotonin receptors such as 5-HT2A and inhibiting the reuptake of serotonin, norepinephrine, and/or ...
  https://en.wikipedia.org/wiki/Serotonin_antagonist_and_reuptake_inhibitor
*  Naproxen | CNS Diseases
Specific Migraine-Preventive Agents: Serotonin Antagonists The antiserotonin, migraine-preventive drugs are potent 5-HT2B- and ... General Action and Information Opioids bind to opiate receptors in the CNS, where they act as agonists of endogenously ... Barbital Nortriptyline Anticonvulsants Venlafaxine Carbamazepine Aripiprazole Anafranil Escitalopram Selective Serotonin ... Alpha Antagonists The U.S. Headache Consortium Guidelines and the AHCPR Technical Review included 17 controlled trials of a2 ...
  http://cnsdiseases.com/tag/naproxen
*  S32212 - Wikipedia
March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential ... It behaves as a selective, combined 5-HT2C receptor inverse agonist and α2-adrenergic receptor antagonist (at all three ... or mACh receptors. This profile of activity is compatible with the definition of a noradrenergic and specific serotonergic ... March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential ...
  https://en.wikipedia.org/wiki/S32212
*  Aripiprazole - Wikipedia
... may act essentially as a selective D2 receptor partial agonist without significantly affecting most of the serotonin receptors ... For the purpose of D2 blockage, aripiprazole, a partial agonist on D2 receptor site, should not be used with a full antagonist ... Wood M, Reavill C (2007). "Aripiprazole acts as a selective dopamine D2 receptor partial agonist". Expert Opin Investig Drugs. ... It appears to show predominantly antagonist activity on postsynaptic D2 receptors and partial agonist activity on presynaptic ...
  https://en.wikipedia.org/wiki/Aripiprazole
*  Agonist and Antagonist Binding to Rabbit Cortical 5-HT Receptors
Unexpectedly, Mg++ decreases the binding of the putative neutral antagonists ketanserin and MDL 100,907, suggesting that these ... compounds may actually be inverse agonists at the 5-HT 2A receptor. ... Mg++ shifts the 5HT 2A receptor toward the agonist high affinity state as demonstrated by the increased affinity of the agonist ... 5HT 2A receptor toward the agonist high affinity state as demonstrated by the increased affinity of the agonist, DOI. ...
  http://www.mgwater.com/rabbit.shtml
*  5-HT2B receptor - Wikipedia
Selective BW-723C86: fair functional subtype selectivity; almost full agonist. Anxiolytic in vivo. Ro60-0175 functionally ... receptors in the serotonin syndrome". Neuropharmacology. 61 (3): 495-502. doi:10.1016/j.neuropharm.2011.01.025. PMID 21277875. ... 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 ... Lin Z, Walther D, Yu XY, Drgon T, Uhl GR (Dec 2004). "The human serotonin receptor 2B: coding region polymorphisms and ...
  https://en.wikipedia.org/wiki/5-HT2B_receptor
*  Meta-Chlorophenylpiperazine - Wikipedia
It behaves as an agonist at most serotonin receptors. mCPP has been shown to act not only as a serotonin reuptake inhibitor but ... receptor agonists". Bioorg. Med. Chem. Lett. 14 (9): 2367-70. doi:10.1016/j.bmcl.2003.05.001. PMID 15081042. Silverstone PH, ... Thomas DR, Gager TL, Holland V, Brown AM, Wood MD (1996). "m-Chlorophenylpiperazine (mCPP) is an antagonist at the cloned human ... It has potent anorectic effects and has encouraged the development of selective 5-HT2C receptor agonists for the treatment of ...
  https://en.wikipedia.org/wiki/Meta-Chlorophenylpiperazine