1780372-25-9

1780372-25-9 structure

Name: SB 243213 dihydrochloride
Chemical Name: SB 243213 dihydrochloride
CAS Number: 1780372-25-9
Molecular Formula: C₂₂H₂₁Cl₂F₃N₄O₂
Molecular Weight: 501.33
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2020-04-14 15:41:54
Modify Date: 2024-01-13 14:05:49
SB 243213 dihydrochloride 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 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1].

Name	SB 243213 dihydrochloride

Description	SB 243213 dihydrochloride 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 dihydrochloride 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 dihydrochloride shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows 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 dihydrochloride (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 dihydrochloride (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: p.o.; 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	C₂₂H₂₁Cl₂F₃N₄O₂
Molecular Weight	501.33

1780372-25-9	200940-23-4
200940-22-3	1781882-72-1
1226917-67-4	607373-46-6
929016-98-8	181632-25-7
201038-58-6	1049747-87-6
1158522-08-7	940364-43-2
134104-43-1	131615-57-1
6906-52-1	930439-75-1
1018584-77-4	1375289-11-4
849349-65-1	127437-46-1