Cayman SB-204741

SB-204741 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT_2B.¹ It inhibits 5-HT-induced contraction of isolated rat stomach fundus, a tissue that endogenously expresses high levels of 5-HT_2B receptors (PA₂ = 7.95). SB-204741 is selective for 5-HT_2B receptors over 5-HT_1A, 5-HT_1D, 5-HT_1E, 5-HT_2A, 5-HT_2C, 5-H_T3, 5-H_T4, dopamine D_1-3, histamine H₁, α₁- and α₂-adrenergic, and GABA_A receptors (K_is = 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.² It also reduces blood pressure in DOCA-salt hypertensive rats.³

WARNING This product is not for human or veterinary use.