SB-204741

SB-204741 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B. It inhibits 5-HT-induced contraction of isolated rat stomach fundus, a tissue that endogenously expresses high levels of 5-HT2B receptors (pA2 = 7.95). SB-204741 is selective for 5-HT2B receptors over 5-HT1A, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, dopamine D1-3, histamine H1, alpha1- and alpha2-adrenergic, and GABAA receptors (Kis = 1-100 µM). In vivo, SB-204741 (1 mg/kg per day) prevents the development of pulmonary arterial hypertension (PAH) and reduces vascular stiffness in a Bmpr2 mutant mouse model of hereditary PAH. It also reduces blood pressure in DOCA-salt hypertensive rats.Formal Name: N-(1-methyl-1H-indol-5-yl)-N'-(3-methyl-5-isothiazolyl)-urea. CAS Number: 152239-46-8. Molecular Formula: C14H14N4OS. Formula Weight: 286.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 15 mg/ml. lambdamax: 231, 270 nm. SMILES: O=C(NC1=CC(C=CN2C)=C2C=C1)NC3=CC(C)=NS3. InChi Code: InChI=1S/C14H14N4OS/c1-9-7-13(20-17-9)16-14(19)15-11-3-4-12-10(8-11)5-6-18(12)2/h3-8H,1-2H3,(H2,15,16,19). InChi Key: USFUFHFQWXDVMH-UHFFFAOYSA-N.