Uses
SB 228357 is a SR-2C/SR-2B receptor antagonist. It is used in the treatment of irritable bowel syndrome (IBS).
Definition
ChEBI: SB 228357 is an indolyl carboxylic acid.
Biological Activity
5-HT 2C/2B receptor antagonist (pK i values are 7.0, 8.1 and 9.1 at 5-HT 2A , 2B and 2C receptors respectively). Displays inverse agonism in a 5-HT-stimulated PI hydrolysis model of 5-HT 2C receptor function. Orally active in vivo .
in vivo
SB228357 (0-10 mg/kg; oral administration; for 90 minutes; male Sprague Dawley rats) treatment significantly reverses Haloperidol-induced catalepsy[2].
| Animal Model: | Male Sprague Dawley rats (200-250g) injected with Haloperidol[2] |
| Dosage: | 0 mg/kg, 0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg |
| Administration: |
Oral administration; for 90 minutes |
| Result: | Significantly reversed Haloperidol-induced catalepsy.
|
IC 50
5-HT
2A Receptor: 6.9 (pKi); 5-HT
2C Receptor: 9 (pKi); 5-HT
2B Receptor: 8 (pKi)