... is a histamine H3 receptor antagonist. It has neuroprotective effects via stimulation of GABA release in brain ... Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z (2007). "The histamine H3 receptor antagonist clobenpropit ... Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P (2007). "The human histamine H3 receptor couples to GIRK channels in ...
It is a histamine 3 (H3) receptor antagonist/inverse agonist. It represents the first commercially available medication in its ... Schwartz JC (2011). "The histamine H3 receptor: from discovery to clinical trials with pitolisant". Br. J. Pharmacol. 163 (4): ... It was the first H3 receptor inverse agonist to be tested in humans or introduced for clinical use. It was designed and ... Pitolisant was developed by Jean-Charles Schwartz, Walter Schunack, and colleagues after the former discovered the H3 receptor ...
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Chlorprothixene is an antagonist of the following receptors: 5-HT2, 5-HT6, 5-HT7: antipsychotic effects, sedation/anxiolysis, ...
H3 receptor antagonist "Thioperamide". IUPHAR/BPS Guide to Pharmacology. Schwartz JC (June 2011). "The histamine H3 receptor: ... Thioperamide was found to be an antagonist of histamine autoreceptors, which negatively regulate the release of histamine, and ... Thioperamide is a potent HRH4 antagonist and selective HRH3 antagonist capable of crossing the blood-brain barrier. It was used ... Its action on H3 is thought to promote wakefulness and improve memory consolidation. ...
... is a histamine antagonist selective for the H3 subtype. McLeod RL, Rizzo CA, West RE Jr, Aslanian R, McCormick K, ... Pharmacological characterization of the novel histamine H3-receptor antagonist N-(3,5-dichlorophenyl)-N'-[[4-(1H-imidazol-4- ...
... is a histamine antagonist selective for the H3 subtype. It has anorectic effects in animal studies and is being ... December 2005). "Influence of a selective histamine H3 receptor antagonist on hypothalamic neural activity, food intake and ... "Increase of neuronal histamine in obese rats is associated with decreases in body weight and plasma triglycerides". Obesity ( ...
"Characterization of histamine H3 receptors in mouse brain using the H3 antagonist 125Iiodophenpropit". Naunyn-Schmiedeberg's ... Iodophenpropit is a histamine antagonist which binds selectively to the H3 subtype. Its 125I radiolabelled form has been used ... "Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, 125I-iodophenpropit, to ... for mapping the distribution of H3 receptors in animal studies. Jansen, FP; Wu, TS; Voss, HP; Steinbusch, HW; Vollinga, RC; ...
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R (February 2012). "Interactions of recombinant human histamine H1, H2 ... Ghoneim OM, Legere JA, Golbraikh A, Tropsha A, Booth RG (2006). "Novel ligands for the human histamine H1 receptor: synthesis, ... Proudman RG, Pupo AS, Baker JG (August 2020). "The affinity and selectivity of α-adrenoceptor antagonists, antidepressants, and ...
... is an extremely potent histamine H3 inverse agonist/antagonist. The histamine H3 receptor is an inhibitory ... Pillot C, Ortiz J, Héron A, Ridray S, Schwartz JC, Arrang JM (August 2002). "Ciproxifan, a histamine H3-receptor antagonist/ ... Witkin JM, Nelson DL (July 2004). "Selective histamine H3 receptor antagonists for treatment of cognitive deficiencies and ... a potent histamine H3-receptor antagonist". J. Pharmacol. Exp. Ther. 287 (2): 658-66. PMID 9808693. ...
von Coburg Y, Kottke T, Weizel L, Ligneau X, Stark H (2009). "Potential utility of histamine H3 receptor antagonist ... It is also a strong antagonist of the H1 receptor, a moderate antagonist of the 5-HT2 and α1-adrenergic receptors, and a weak ... Appl H, Holzammer T, Dove S, Haen E, Strasser A, Seifert R (2012). "Interactions of recombinant human histamine H₁R, H₂R, H₃R, ... Maprotiline has also more recently been identified as a potent antagonist of the 5-HT7 receptor, with this action potentially ...
"Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H- ... Impentamine is a histamine antagonist selective for the H3 subtype. Vollinga, RC; Menge, WM; Leurs, R; Timmerman, H (1995). " ... Van Der Goot, H; Timmerman, H (2000). "Selective ligands as tools to study histamine receptors". European Journal of Medicinal ...
... is an antagonist at the H2 and H3 histamine receptors. It is largely inactive as an H2 antagonist at physiological ... ISBN 978-0-19-850346-0. "Tagamet: Discovery of Histamine H2-receptor Antagonists". National Historic Chemical Landmarks. ... in their intent to develop a histamine antagonist for the treatment of peptic ulcers. The discovery of burimamide ultimately ... pH, but its H3 affinity is 100x higher. It is a thiourea derivative. Burimamide was first developed by scientists at Smith, ...
... is a histamine antagonist selective for the H3 subtype. It has stimulant and nootropic effects in animal studies, ... Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD (July 2008). "The histamine H3 receptor: an attractive ... November 2004). "Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist". Br. J. Pharmacol. 143 (5 ... "Effects of histamine H(3) antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in ...
Histamine H3 receptor. Agonists: alpha-Methylhistamine • Cipralisant • هیستامین • ایمتیت • ایمپیپ • ایمتریدین • متیمپیپ • ... Antagonists: Asenapine • Latrepirdine • Metitepine • Ritanserin • SB-699,551. * Note that the 5-HT5B گیرنده is not functional ... Antagonists: A-۳۴۹٬۸۲۱ • A-۴۲۳٬۵۷۹ • ABT-۲۳۹ • بتاهیستین • بوریم‌آمید • Ciproxifan • Clobenpropit • Conessine • GSK-۱۸۹٬۲۵۴ • ... Histamine N-methyltransferase inhibitors. آمودیاکین • BW-۳۰۱U • دیفن هیدرامین • هارمالین • Metoprine • کیناکرین • SKF-۹۱٬۴۸۸ • ...
Subdivisions of histamine antagonists include H1 receptor antagonists, H2 receptor antagonists, and H3 receptor antagonists. ... Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). ... Histaminergic means "working on the histamine system", and histaminic means "related to histamine". A histaminergic agent (or ... drug) is a chemical which functions to directly modulate the histamine system in the body or brain. ...
Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells. BMC Pharmacology. 2008 ... to antagonist, to inverse agonist in different tissues, depending on the level of constitutive activity of the histamine H3 ... Protean agonism at histamine H3 receptors in vitro and in vivo. Proceedings of the National Academy of Sciences USA. 2003 Sep ... Proxyfan is a histamine H3 receptor ligand which is a "protean agonist", producing different effects ranging from full agonist ...
A-349,821 is a potent and selective histamine H3 receptor antagonist (or possibly an inverse agonist). It has nootropic effects ... April 2003). "Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists". ... a selective and potent human histamine H3 receptor antagonist". Biochemical Pharmacology. 68 (5): 933-45. doi:10.1016/j.bcp. ... H3 receptor antagonist Faghih R, Dwight W, Pan JB, Fox GB, Krueger KM, Esbenshade TA, et al. ( ...
... is a potent and selective histamine antagonist which binds selectively to the H3 subtype. However while VUF-5681 ... Baker JG (June 2008). "Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells". ... "Constitutive activity of H3 autoreceptors modulates histamine synthesis in rat brain through the cAMP/PKA pathway". ... blocks the activity of more potent H3 agonists, recent studies suggest that it may have some weak partial agonist activity when ...
"Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics". Bioorganic & Medicinal Chemistry ... Its mechanism of action is not entirely clear but believed to be related to its ability as a dopamine antagonist. It also has ... Histamine receptors (H1 receptors, accounting for sedation, antiemetic effect, vertigo, and weight gain) α1- and α2-adrenergic ... Furthermore, the brain has a higher density of histamine H1 receptors than any body organ examined which may account for why ...
Potent and selective histamine H3 receptor antagonist with drug-like properties". J. Pharmacol. Exp. Ther. 313 (1): 165-75. doi ... analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists". Biochemical Pharmacology. 71 (8): 1103-13. ... and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist". J. ... but is still widely used in animal research into H3 antagonists / inverse agonists. Esbenshade TA, Fox GB, Krueger KM, Miller ...
This history has led to contemporary research into drugs which are H3 receptor antagonist and which affect the Histamine H4 ... March 2008). "Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its ... a potent histamine H3-receptor antagonist". The Journal of Pharmacology and Experimental Therapeutics. 287 (2): 658-66. PMID ... a selective and potent human histamine H3 receptor antagonist". Biochemical Pharmacology. 68 (5): 933-45. doi:10.1016/j.bcp. ...
It acts as a histamine antagonist, selective for the H3 subtype (with an affinity of pKi = 8.27; Ki = ~5 nM). It was also found ... "A new family of H3 receptor antagonists based on the natural product Conessine". Bioorganic & Medicinal Chemistry Letters. 18 ( ... "The Alkaloid Conessine and Analogues as Potent Histamine H3Receptor Antagonists". Journal of Medicinal Chemistry. 51 (17): 5423 ...
Pitolisant, a selective histamine 3 (H3) receptor antagonist/inverse agonist, was approved by FDA during August 2019. It works ... There is ongoing research into the efficacy of gamma aminobutyric acid A (GABAA) receptor antagonists for the treatment of ... Flumazenil, a GABAA receptor antagonist is approved by the FDA for use in anesthesia reversal and benzodiazepine overdose. ... Suvorexant, a hypocretin receptor antagonist, has been developed to limit the natural effects of hypocretin in patients with ...
A-423,579 is one of a range of histamine antagonists developed by Abbott Laboratories which are selective for the H3 subtype, ... "Antiobesity evaluation of histamine H3 receptor (H3R) antagonist analogs of A-331440 with improved safety and efficacy". ... radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists". Basic ...
He is co-inventor of pitolisant, the first histamine H3-receptor antagonist/inverse agonist Wakix, for treating narcolepsy. ... 1, 2001, 13-vii-13-viii "Charon Robin Ganellin", EHRS Tagamet: Discovery of Histamine H2-receptor Antagonists from American ... collaborating with Sir James Black researching histamine H2-receptor antagonists. This research eventually led to the discovery ... This discovery was crucial to their research, providing the impetus to search for a suitable H2-receptor antagonist to affect ...
... is a strong antagonist of the histamine H3 receptor and a weak agonist of the histamine H1 receptor. Betahistine ... The study authors suggest that hypersensitivity reactions may be a direct result of betahistine's role in increasing histamine ... More importantly, betahistine has a powerful antagonistic effects at H3 receptors, thereby increasing the levels of ... Its chemical structure closely resembles those of phenethylamine and histamine.[citation needed] Betahistine is marketed under ...
GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves ... Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat ... Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and ... The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. British Journal of Pharmacology. 2008 ...
June 1998). "High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models". ... An Efficient Multigram Synthesis of the Potent Histamine H3 Antagonist GT-2331 and the Reassessment of the Absolute ... Cipralisant (GT-2331, tentative trade name Perceptin) is an extremely potent histamine H3 receptor ligand originally developed ... Cipralisant was initially classified as a selective H3 antagonist, but newer research (2005) suggests also agonist properties, ...
June 2007). "GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and ... August 2008). "Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and ... April 2007). "Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory ... It has subnanomolar affinity for the H3 receptor (Ki = 0.2nM) and selectivity of over 10,000x for H3 over other histamine ...
... may also act on histamine H3 receptors, thereby producing adverse effects.[citation needed] Astemizole does also act ... Astemizole is a histamine H1-receptor antagonist. It has anticholinergic and antipruritic effects. Astemizole is rapidly ... This suppresses the formation of edema and pruritus (caused by histamine). Despite some earlier reports that astemizole does ... absorbed from the gastrointestinal tract and competitively binds to histamine H1 receptor sites in the gastrointestinal tract, ...
GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves ... Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat ... Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and ... The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. British Journal of Pharmacology. 2008 ...
Glutamate receptor antagonist(英語:Excitatory amino acid antagonist) (NMDA(英語:NMDA receptor antagonist)) ... 組織胺受體激動劑(英語:Histamine agonist) ... 血清素受體拮抗劑(英語:Serotonin antagonist) (5-HT3(英語:5-HT3 antagonist)) ... Cannabinoid receptor antagonist(英語:Cannabinoid receptor antagonist). *Endocannabinoid enhancer(英語:Endocannabinoid enhancer) ( ... 多巴胺受體拮抗劑(英語:Dopamine
"Purification and molecular cloning of a secreted, Frizzled-related antagonist of Wnt action". Proc. Natl. Acad. Sci. U.S.A. 94 ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
InChI=1S/C19H24N4O2/c20-18(21)14-4-8-16(9-5-14)24-12-2-1-3-13-25-17-10-6-15(7-11-17)19(22)23/h4-11H,1-3,12-13H2,(H3,20,21)(H3, ... Indirect/downstream NO modulators: ACE inhibitors/AT-II receptor antagonists (e.g., captopril, losartan) ... the solution should be slowly infused to minimize the release of histamine.[19] ... Pentamidine is also identified as a potential small molecule antagonist that disrupts this interaction between S100P and RAGE ...
Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z. The histamine H3 receptor antagonist clobenpropit enhances ... Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P (2007). "The human histamine H3 receptor couples to GIRK channels in ... InChI=1S/C14H17ClN4S/c15-12-5-3-11(4-6-12)8-18-14(16)20-7-1-2-13-9-17-10-19-13/h3-6,9-10H,1-2,7-8H2,(H2,16,18)(H,17,19) Y. Key ... Klobenpropit je histaminski antagonist H3 receptora.[5] On ima neuroprotektivno dejstvo, koje ostvaruje putem stimulacije ...
Agonists and antagonists[edit]. Specific antagonists include istradefylline (KW-6002) and SCH-58261, while specific agonists ... Specific antagonists include MRS1191, MRS1523 and MRE3008F20, while specific agonists include Cl-IB-MECA and MRS3558.[19] ... Adenosine antagonists are widely used in neonatal medicine; A reduction in A1 expression appears to prevent hypoxia-induced ... Xanthine derivatives such as caffeine and theophylline act as non-selective antagonists at A1 and A2A receptors in both heart ...
乙酰胆碱 (M1, M2, M3, M4, M5) · 多巴胺(英语:Dopamine receptor) (D1, D2, D3, D4, D5) · 组织胺(英语:Histamine receptor) (H1, H2, H3, H4) · 褪黑素( ... GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor. British Journal of Pharmacology. January 1994 ...
Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ...
D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
... drugs which are selective receptor antagonists of CysLTR1 but not CysLTR2.[20][21][22][23] Models of allergic reactions in ... a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma". Journal of Medicinal Chemistry. 58 (15): 6093-113. doi: ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... and development asthma and that drugs targeting CYSLTR2 may work in a manner that differs from those of CYSLTR1 antagonists.[9] ...
CCL18 has been identified as an endogenous antagonist of the GPER.[16] ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... "In vivo effects of a GPR30 antagonist". Nat. Chem. Biol. 5 (6): 421-7. doi:10.1038/nchembio.168. PMC 2864230. PMID 19430488 ...
Quartara L, Altamura M (Aug 2006). "Tachykinin receptors antagonists: from research to clinic". Current Drug Targets. 7 (8): ... SB-222,200 - potent and selective antagonist, Ki = 4.4 nM, 3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide, ... Advenier C, Lagente V, Boichot E (Aug 1997). "The role of tachykinin receptor antagonists in the prevention of bronchial ... NK3 receptor antagonists are being investigated as treatments for various indications.[7] ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... Antagonists: Agomelatine. *Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, ... Antagonists: Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, clorotepine, clozapine, ...
Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ...
Orthosteric (competitive) Antagonist bicuculline,[59] gabazine,[69] thujone,[70] flumazenil[71] Uncompetitive antagonist (e.g. ... Kuriyama K, Sze PY (January 1971). "Blood-brain barrier to H3-γ-aminobutyric acid in normal and amino oxyacetic acid-treated ...
response to histamine. • behavioral fear response. • dopamine receptor signaling pathway. • G-protein coupled receptor ... Apomorphine - D4 selective but also D2 and D3 agonist, α-adrenergic and serotonergic weak antagonist ... Lanig H, Utz W, Gmeiner P (April 2001). "Comparative molecular field analysis of dopamine D4 receptor antagonists including 3-[ ... an antagonist with high affinity and selectivity for the human dopamine D4 receptor". Journal of Medicinal Chemistry. 39 (10): ...
Category:Dopamine antagonists. References[edit]. *^ Girault JA, Greengard P (2004). "The neurobiology of dopamine signaling". ... antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine ... unless blocked by a receptor antagonist or a synthetic partial agonist.[8] ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
Ramatroban, vidupiprant, and Bay U3405 are non-selective (i.e. known to influence other receptors) antagonists of DP2.[9] ... PDP2 receptor antagonists have been shown to allergic reactions induced in the airways mice and sheep as well as the airways ... The following compounds are selective receptor antagonists of and thereby inhibit the activation of DP2: fevipiprant, ... Setipiprant (ACT-129968), a selective, orally active antagonist of the (DP2) receptor, proved to be well-tolerated and ...
The potency of second generation histamine antagonists is (from strongest to weakest) desloratadine (Ki 0.4 nM) , ... InChI=1S/C22H23ClN2O2/c1-2-27-22(26)25-12-9-15(10-13-25)20-19-8-7-18(23)14-17(19)6-5-16-4-3-11-24-21(16)20/h3-4,7-8,11,14H,2,5- ... Loratadine is a tricyclic antihistamine, which acts as a selective inverse agonist of peripheral histamine H1 receptors.[11][16 ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... InChI=1S/C21H26N2OS2/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(26(2)24)15-19(21)23/h3-4,8-11,15-16H,5-7,12- ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... Antagonists: Agomelatine. *Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, ...
InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) Y ... Histamine. *HTMT. *UR-AK49. *Antagonists: First-generation: 4- ... InChI=1/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8) ...
Antagonists: AR-A000002. *Beta blockers (e.g., alprenolol, carteolol, isamoltane, oxprenolol, penbutolol, propranolol, ... InChI=1S/C11H15NO2/c1-8(12-2)5-9-3-4-10-11(6-9)14-7-13-10/h3-4,6,8,12H,5,7H2,1-2H3 Y ... Antagonists: ABT-354. *Atypical antipsychotics (e.g., aripiprazole, asenapine, clorotepine, clozapine, fluperlapine, ... Antagonists: Agomelatine. *Atypical antipsychotics (e.g., amisulpride, aripiprazole, asenapine, brexpiprazole, cariprazine, ...
InChI=1S/C17H21NO/c1-18(2)12-13-19-17-11-7-6-10-16(17)14-15-8-4-3-5-9-15/h3-11H,12-14H2,1-2H3 Y ... Histamine. *HTMT. *L-Histidine. *UR-AK49. *Antagonists: First-generation: 4-Methyldiphenhydramine. *Alimemazine ...
InChI=1S/C16H14N2O4/c1-7(2)8-3-4-12-9(5-8)13(19)10-6-11(16(20)21)14(17)18-15(10)22-12/h3-7H,1-2H3,(H2,17,18)(H,20,21) Y ... Its mechanism of action is not well-determined, but it might inhibit inflammation by inhibiting the release of histamine and ... muscarinic antagonist. *Aclidinium bromide. *Glycopyrronium bromide. *Ipratropium bromide#. *Oxitropium bromide. *Tiotropium ...
"Effects of a novel corticotropin-releasing-hormone receptor type I antagonist on human adrenal function". Molecular Psychiatry ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ... D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ...
MEN-10376 - potent and selective antagonist, 7-amino acid polypeptide chain. CAS# 135306-85-3 ... one small-molecule antagonist Saredutant is currently in clinical trials as an anxiolytic and antidepressant. ... "Tachykinin antagonists inhibit nerve-mediated contractions in the circular muscle of the human ileum. Involvement of neurokinin ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
On the other hand, GHS-R antagonists have anorectic effects and are likely to be useful for the treatment of obesity. ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
Antagonists[edit]. *Agouti signalling peptide - nonselective peptide antagonist. In other organisms[edit]. ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
... and administration of mixed GHB/GABAB receptor agonists along with a selective GABAB antagonist or selective agonists for the ... Histamine *H1. *H2. *H3. *H4. *Melatonin (1A. *1B. *1C). *TAAR (1. *2 ...
Cleary L, Murad K, Bexis S, Docherty JR (2005). "The alpha (1D)-adrenoceptor antagonist BMY 7378 is also an alpha (2C)- ... Kyprianou N, Benning CM (2000). "Suppression of human prostate cancer cell growth by alpha1-adrenoceptor antagonists doxazosin ... adrenoceptor antagonist". Auton Autacoid Pharmacol. 25 (4): 135-41. doi:10.1111/j.1474-8673.2005.00342.x. PMID 16176444.. ... adrenoceptor antagonist with minimal dopamine D(2) and 5-HT(1A) receptor affinity". Eur. J. Pharmacol. 433 (1): 123-7. doi: ...