SB 221284

Modify Date: 2024-01-05 17:15:11

SB 221284 Structure
SB 221284 structure
Common Name SB 221284
CAS Number 196965-14-7 Molecular Weight 353.36200
Density 1.43g/cm3 Boiling Point 536.2ºC at 760 mmHg
Molecular Formula C16H14F3N3OS Melting Point N/A
MSDS N/A Flash Point 278.1ºC

 Use of SB 221284


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].

 Names

Name 5-methylsulfanyl-N-pyridin-3-yl-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
Synonym More Synonyms

 SB 221284 Biological Activity

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
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.

 Chemical & Physical Properties

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

 Synonyms

5-(Methylthio)-1-(3-pyridylcarbamoyl)-6-(trifluoromethyl)indoline
Tocris-1379
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