SB 204741

SB 204741 is a selective and high affinity 5-HT_2B antagonist with a pK_i value of 7.1^[1]. IC50 & Target: pKi: 7.1 (5-HT_2B)^[1] In Vitro: The most selective 5-HT_2B receptor ligand to be tested is SB 204741 with approximately 20 fold selectivity for the human 5-HT_2B receptor as compared to the human 5-HT_2C receptor^[1]. In Vivo: SB-204741 (0.25~1.0 mg/kg; i.p.) induces myocardial remodeling and dose dependently improves hemodynamic and ventricular functions following isoproterenol-induced myocardial injury^[1].
SB-204741 bolsters endogenous anti-oxidant enzymes activities, improves cardiac injury markers, NO level and lipid peroxidation level and attenuates TNFα level in isoproterenol-induced myocardial remodeling in rats. SB-204741 (0.5 and 1.0 mg/kg/day) pre-treatment for 28 days significantly amplifies NO level and GSH and SOD activities and attenuates TBARS level following isoproterenol-induced myocardial remodeling. SB-204741 inhibits inflammatory protein expression, upregulates autophagy and HSPs protein expressions in isoproterenol-induced myocardial remodeling in rats. SB-204741 improves myocardial architecture in isoproterenol-induced myocardial remodeling in rats^[1].