SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1.
IC50&Target
human 5-HT2B Receptor
7.1 (pKi)
体外研究
The most selective 5-HT2B receptor ligand to be tested is SB 204741 with approximately 20 fold selectivity for the human 5-HT2B receptor as compared to the human 5-HT2C receptor.
体内研究
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.
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.
Animal Model:
Rats
Dosage:
0.25~1.0 mg/kg
Administration:
I.p.
Result:
Induced myocardial remodeling.
分子式
C14H14N4Os
分子量
286.35
CAS号
152239-46-8
运输条件
Room temperature in continental US; may vary elsewhere.