SB 204741

Names

[ CAS No. ]:
152239-46-8

[ Name ]:
SB 204741

[Synonym ]:
Tocris-1372
N-(1-Methyl-1H-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea
Lopac-S-0693

Biological Activity

[Description]:

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

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

human 5-HT2B Receptor:7.1 (pKi)

[In Vitro]

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].

[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]. Animal Model: Rats[1] Dosage: 0.25~1.0 mg/kg Administration: I.p. Result: Induced myocardial remodeling.

[References]

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.38g/cm3

[ Boiling Point ]:
335.9ºC at 760 mmHg

[ Molecular Formula ]:
C₁₄H₁₄N₄OS

[ Molecular Weight ]:
286.35200

[ Flash Point ]:
157ºC

[ Exact Mass ]:
286.08900

[ PSA ]:
87.19000

[ LogP ]:
3.73320

[ Vapour Pressure ]:
0.000116mmHg at 25°C

[ Index of Refraction ]:
1.707

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ RIDADR ]:
NONH for all modes of transport

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