同义名 :	CID 1261822
	CAS号 :	713121-80-3
	货号 :	A811582
	分子式 :	C28H25N5O4S
	纯度 :	99%+
	分子量 :	527.59
	MDL号 :	MFCD05999971
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

G protein-coupled receptor 55 (GPR55) belongs to the class A family of G-protein coupled receptor (GPCRs)[1]. GPR55 was activated by a range of plant, synthetic and endogenous cannabinoids and blocked by the non-psychoactive phytocannabinoid, cannabidiol. ML-193 is a potent and selective GPR55 antagonist( IC50 : 221 nM). It shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2, and can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats. Intra-striatal administration of ML193 increased time on the rotarod, decreased latency to remove the label and slip steps in 6-OHDA-lesioned rats mostly at the dose of 1 g/rat[2]. M184 significantly promoted neuronal differentiation in vitro while ML193 reduced differentiation rates as compared to vehicle treatment. Continuous administration of O-1602 into the hippocampus via a cannula connected to an osmotic pump resulted in increased Ki67+ cells within the dentate gyrus. O-1602 increased immature neuron generation, as assessed by DCX+ and BrdU+ cells, as compared to vehicle-treated animals. GPR55-/- animals displayed reduced rates of proliferation and neurogenesis within the hippocampus while O-1602 had no effect as compared to vehicle controls[3].

临床研究
NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01500278	-		Completed	-	-
NCT01500278	Rheumatoid Arthritis	Phase 4	Completed	-	-
NCT00552344	Crohn Disease	Phase 3	Completed	-	-

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.90mL 0.38mL 0.19mL	9.48mL 1.90mL 0.95mL	18.95mL 3.79mL 1.90mL

参考文献

[1] Bo Liu,et al. GPR55: from orphan to metabolic regulator? Pharmacol Ther. 2015 Jan;145:35-42. [2]Fatemi I, et, al. The effect of intra-striatal administration of GPR55 agonist (LPI) and antagonist (ML193) on sensorimotor and motor functions in a Parkinson's disease rat model. Acta Neuropsychiatr. 2021 Feb;33(1):15-21. [3]Hill JD, et, al. Activation of GPR55 increases neural stem cell proliferation and promotes early adult hippocampal neurogenesis. Br J Pharmacol. 2018 Aug;175(16):3407-3421.