Formulation: A solid
Formal Name: N-(1-methyl-1H-indol-5-yl)-N′-(3-methyl-5-isothiazolyl)-urea
Purity: ≥95%
Formula Markup: C14H14N4OS
Formula Weight: 286,4
Shelf life (days): 1460
CAS Number: 152239-46-8
Notes: SB-204741 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.{61368} 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, α1- and α2-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.{61369} It also reduces blood pressure in DOCA-salt hypertensive rats.{61370}