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].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

5-HT2A Receptor:6.4 (pKi)

5-HT2B Receptor:7.9 (pKi)

5-HT2C Receptor:8.6 (pKi)

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.

[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.