SB 243213 dihydrochloride

Modify Date: 2024-01-13 14:05:49

SB 243213 dihydrochloride Structure
SB 243213 dihydrochloride structure
Common Name SB 243213 dihydrochloride
CAS Number 1780372-25-9 Molecular Weight 501.33
Density N/A Boiling Point N/A
Molecular Formula C22H21Cl2F3N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of SB 243213 dihydrochloride


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].

 Names

Name SB 243213 dihydrochloride

 SB 243213 dihydrochloride Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C22H21Cl2F3N4O2
Molecular Weight 501.33