Uses
SB 221284 is a potent, selective SR-2C/SR-2B antagonist.
Definition
ChEBI: SB 221284 is an indolyl carboxylic acid.
Biological Activity
Potent, selective 5-HT 2C/2B receptor antagonist. pK i values are 6.4, 7.9 and 8.6 for 5-HT 2A , 2B and 2C receptors respectively. Centrally active upon systemic administration in vivo .
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.
|
IC 50
5-HT
2A Receptor: 6.4 (pKi); 5-HT
2B Receptor: 7.9 (pKi); 5-HT
2C Receptor: 8.6 (pKi)
