SB-216641A

SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A blocks SKF-99101H from functioning in vivo[1][2].

Research Areas >> Neurological Disease

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

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

5-HT1B Receptor

5-HT1D Receptor

SB-216641A (0.6–20 mg/kg；腹腔注射；单剂量) 在豚鼠内以剂量依赖性方式阻碍 SKF-99101H 诱导的低体温[1]。 SB-216641A (559 nmol/kg；静脉注射；单剂量) 与 5-HT1B/D 受体拮抗剂 GR-127935 联用时改善了狗注射 800 nmol/kg 舒马曲坦 Sumatriptan (HY-B0121B) 后观察到的胃松弛[2]。 Animal Model: Guinea pigs[1]. Dosage: 0.6, 2.0, 6.0 and 20.0 mg/kg. Administration: Intraperitoneal injection; single dose. Result: Significantly blocked the effects of SKF-99101H. Animal Model: Dogs[2]. Dosage: 559 nmol/kg. Administration: Intravenous injection; single dose. Result: Improved the gastric relaxation.

[1]. Hagan JJ, et al. Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig. Eur J Pharmacol. 1997 Jul 23;331(2-3):169-74.  

[2]. De Ponti F, et al. Role of 5-HT1B/D receptors in canine gastric accommodation: effect of sumatriptan and 5-HT1B/D receptor antagonists. Am J Physiol Gastrointest Liver Physiol. 2003 Jul;285(1):G96-104.