| Description |
SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively[1]. SB-215505 increases wakefulness and motor activity in rats[2].
|
| Related Catalog |
|
| Target |
5-HT2B Receptor:8.3 (pKi)
5-HT2A Receptor:6.77 (pKi)
5-HT2C Receptor:7.66 (pKi)
|
| In Vitro |
SB-215505 is 30 fold selective for the 5-HT2B over the 5-HT2A receptor, and only marginally selective over the 5-HT2C receptor[1].
|
| In Vivo |
SB-215505 (0.1-1.0 mg/kg; i.p.; two doses) dose-dependently increases wakefulness (W) and decreases IS, PS, SWS-2[2]. Animal Model: Male Sprague-Dawley rats weighing 230-260 g[2] Dosage: 0.1, 0.3 and 1.0 mg/kg Administration: IP; two doses (4 days between two doses) Result: Dose-dependently increased wakefulness (W) and decreased intermediate stage of sleep (IS), paradoxical sleep (PS), SWS-2.
|
| References |
[1]. C Reavill, et al. Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4. [2]. Sandor Kantor, et al. Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505. J Pharmacol. 2004 Aug;142(8):1332-42.
|
