RS-127445

RS-127445
Clinical data
Other names	RS-127,445
Identifiers
	IUPAC name 4-(4-fluoro-1-naphthyl)-6-isopropylpyrimidin-2-amine;
CAS Number	199864-87-4;
PubChem CID	196968;
IUPHAR/BPS	188;
ChemSpider	170590;
UNII	0JAU3P8OBM;
ChEMBL	ChEMBL473186;
CompTox Dashboard (EPA)	DTXSID60941960 ;
Chemical and physical data
Formula	C17H16FN3
Molar mass	281.327 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Nc3nc(C(C)C)cc(n3)-c(cc2)c1ccccc1c2F;
	InChI InChI=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); Key:ZZZQXCUPAJFVBN-UHFFFAOYSA-N;
	(verify)

RS-127445 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT_2B receptor, with around 1000x selectivity over the closely related 5-HT_2A and 5-HT_2C receptors.^[1] The role of the 5-HT_2B 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]

References

^ 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
^ 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
^ 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
^ 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

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[1] 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

[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

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