200940-22-3

200940-22-3 structure

Name: SB 243213
Chemical Name: 5-Methyl-N-{6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl}-6-(trifluo romethyl)-1-indolinecarboxamide
CAS Number: 200940-22-3
Molecular Formula: C₂₂H₁₉F₃N₄O₂
Molecular Weight: 428.40700
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2016-07-17 11:29:39
Modify Date: 2024-01-09 21:24:49
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-hydroxytryptamine (5-HT)2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1].

Name	5-Methyl-N-{6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl}-6-(trifluo romethyl)-1-indolinecarboxamide

Description	SB 243213 hydrochloride is an orally active, selective and high-affinity 5-hydroxytryptamine (5-HT)2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT2C Receptor:9.37 (pKi)
In Vitro	SB 243213 hydrochloride showed little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It showed weak affinity (pKi<6.5) for the cloned human 5-HT1D and D3 receptors and moderate affinity (pKi=6.7) for the cloned human D2 receptor[1].
In Vivo	SB 243213 hydrochloride (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box[1]. SB 243213 hydrochloride (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction[1]. Animal Model: Male Sprague-Dawley experimentally naive rats (220-300 g)[1] Dosage: 0.1, 0.3, 1, 3, 10 mg/kg Administration: PO; 1 hour pre-test Result: Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
References	[1]. Wood MD, et al. SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99.

Molecular Formula	C₂₂H₁₉F₃N₄O₂
Molecular Weight	428.40700
Exact Mass	428.14600
PSA	70.84000
LogP	5.57770

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