SC 51089 free base

SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity[1][2][3].

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

Research Areas >> Neurological Disease

EP1:1.3 μM (Ki)

TP:11.2 μM (Ki)

EP3:17.5 μM (Ki)

FP:61.1 μM (Ki)

SC 51089 free base (5 μM; 24 h) 减弱前列腺素 E2 (PGE2) 诱导的暴露于 t-BuOOH 的神经元细胞死亡[2]。

SC 51089 free base (40 μg/kg; infused i.p. for 28 d) 改善 HD 小鼠运动协调和平衡功能障碍，并挽救长期记忆缺陷[3]。 Animal Model: R6/1 mouse model of Huntington's disease (HD), from 13 to 18 weeks of age[3] Dosage: 40 μg/kg/day Administration: Infused i.p. at a rate of 0.11 μL/h during 28 days by osmotic mini-pump system Result: Ameliorated motor coordination and balance dysfunction. Rescued long-term memory deficit. Improved the expression of specific synaptic markers. Reduced the number of huntingtin nuclear inclusions in the striatum and hippocampus.

[1]. Abramovitz M, et, al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93.  

[2]. Saleem S, et, al. Effects of EP1 receptor on cerebral blood flow in the middle cerebral artery occlusion model of stroke in mice. J Neurosci Res. 2007 Aug 15;85(11):2433-40.  

[3]. Anglada-Huguet M, et, al. Prostaglandin E2 EP1 receptor antagonist improves motor deficits and rescues memory decline in R6/1 mouse model of Huntington's disease. Mol Neurobiol. 2014 Apr;49(2):784-95.