SB 204741

• CAT Number: I009306
• CAS Number: 152239-46-8
• Molecular Formula: C14H14N4OS
• Molecular Weight: 286.35
• Purity: ≥95%
• Synonyms: 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea
• InChI: 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)
• InChIKey: USFUFHFQWXDVMH-UHFFFAOYSA-N
• SMILES: CC1=NSC(=C1)NC(=O)NC2=CC3=C(C=C2)N(C=C3)C

SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1].
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[1].
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].

Reference

[1]. Bonhaus DW, et al. The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors. Br J Pharmacol. 1995;115(4):622-628.
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[2]. Bharti S, et al. 5-HT2B receptor blockade attenuates β-adrenergic receptor-stimulated myocardial remodeling in rats via inhibiting apoptosis: role of MAPKs and HSPs. Apoptosis. 2015;20(4):455-465.
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