196965-14-7

196965-14-7 structure

Name: SB 221284
Chemical Name: 5-methylsulfanyl-N-pyridin-3-yl-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
CAS Number: 196965-14-7
Molecular Formula: C₁₆H₁₄F₃N₃OS
Molecular Weight: 353.36200
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2019-01-01 18:33:43
Modify Date: 2024-01-05 17:15:11
SB 221284 is a selective 5-HT2C/2B receptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. SB 221284 can be used for the research of neurological disease[1].

Name	5-methylsulfanyl-N-pyridin-3-yl-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
Synonyms	5-(Methylthio)-1-(3-pyridylcarbamoyl)-6-(trifluoromethyl)indoline Tocris-1379

Description	SB 221284 is a selective 5-HT2C/2B receptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. SB 221284 can be used for the research of neurological disease[1].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT2A Receptor:6.4 (pKi) 5-HT2B Receptor:7.9 (pKi) 5-HT2C Receptor:8.6 (pKi)
In Vivo	SB 221284 (0.1~1 mg/kg, i.p.) pre-treatment doses shows to block mCPP induced hypolocomotion, significantly enhances the hyperactivity induced by phencyclidine or MK-801[1]. SB 221284 (1 mg/kg, i.p.) significantly enhances the magnitude and duration of the increase induced by phencyclidine[1] Animal Model: Male Sprague Dawley rats (250–360 g)[1] Dosage: 0.1~1 mg/kg Administration: I.p. Result: Pre-treatment doses showed to block mCPP induced hypolocomotion, significantly enhanced the hyperactivity induced by phencyclidine or MK-801. Animal Model: Male Sprague Dawley rats (250–360 g)[1] Dosage: 1 mg/kg Administration: I.p. Result: Significantly enhanced the magnitude and duration of the increase induced by phencyclidine.
References	[1]. Hutson PH, et al. Activation of mesolimbic dopamine function by phencyclidine is enhanced by 5-HT(2C/2B) receptor antagonists: neurochemical and behavioural studies. Neuropharmacology. 2000;39(12):2318-2328. [2]. Bromidge SM, et al. Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines. J Med Chem. 1998;41(10):1598-1612.

Density	1.43g/cm3
Boiling Point	536.2ºC at 760 mmHg
Molecular Formula	C₁₆H₁₄F₃N₃OS
Molecular Weight	353.36200
Flash Point	278.1ºC
Exact Mass	353.08100
PSA	70.53000
LogP	4.55490
Vapour Pressure	1.43E-11mmHg at 25°C
Index of Refraction	1.621

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