| 词条 | RS-127445 |
| 释义 |
| verifiedrevid = 407718195 | IUPAC_name = 4-(4-fluoro-1-naphthyl)-6-isopropylpyrimidin-2-amine | image = RS-127,445_structure.png | width = 220 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 199864-87-4 | ATC_prefix = | ATC_suffix = | PubChem = 196968 | IUPHAR_ligand = 188 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID = 170590 | ChEMBL = 473186 | UNII = 0JAU3P8OBM | C=17 | H=16 | F=1 | N=3 | molecular_weight = 281.327 g/mol | smiles = Nc3nc(C(C)C)cc(n3)-c(cc2)c1ccccc1c2F | StdInChI = 1S/C17H16FN3/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13/h3-10H,1-2H3,(H2,19,20,21) | StdInChIKey = ZZZQXCUPAJFVBN-UHFFFAOYSA-N | synonyms = RS-127,445 }}RS-127445 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x selectivity over the closely related 5-HT2A and 5-HT2C receptors.[1] The role of the 5-HT2B receptor in the body is still poorly understood, and RS-127445 has been a useful tool in unravelling the function of the various systems in which this receptor is expressed.[2][3][4] References1. ^Bonhaus DW, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, Chang LK, Pulido-Rios T, Webber A, Leung E, Eglen RM, Martin GR. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. British Journal of Pharmacology. 1999 Jul;127(5):1075-82. {{DOI|10.1038/sj.bjp.0702632}} {{PMID|10455251}} {{Serotonergics}}{{nervous-system-drug-stub}}2. ^Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L. Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension. Nature Medicine. 2002 Oct;8(10):1129-35. {{DOI|10.1038/nm764}} {{PMID|12244304}} 3. ^Kelly CR, Sharif NA. Pharmacological evidence for a functional serotonin-2B receptor in a human uterine smooth muscle cell line. Journal of Pharmacology and Experimental Therapeutics. 2006 Jun;317(3):1254-61. {{PMID|16517693}} 4. ^Mbaki Y, Ramage AG. Investigation of the role of 5-HT2 receptor subtypes in the control of the bladder and the urethra in the anaesthetized female rat. British Journal of Pharmacology. 2008 Oct;155(3):343-56. {{PMID|18604238}} 5 : 5-HT2B antagonists|Pyrimidines|Naphthalenes|Fluoroarenes|Isopropyl compounds |
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