产品说明书

	同义名 :	6-Iodopravodoline;6-Iodopravadoline;iodopravadoline.
	CAS号 :	164178-33-0
	货号 :	A889592
	分子式 :	C23H25IN2O3
	纯度 :	99+%
	分子量 :	504.361
	MDL号 :	MFCD01861183
	存储条件：	粉末 Sealed in dry,2-8°C 液体 -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

AM630 (iodopravadoline), a novel aminoalkylindole. AM630 behaved as a competitive antagonist of CP 55,940, WIN 55,212-2, anandamide and (R)-(+)-arachidonyl-1'-hydroxy-2'-propylamide (AM356), producing rightward shifts in the log concentration response curves of these cannabinoid receptor agonists. AM630 was markedly more potent as an antagonist of delta 9-THC and CP 55,940 (Kd = 14.0 and 17.3 nM respectively) than as an antagonist of WIN 55,212-2, AM356 or anandamide (Kd = 36.5, 85.9 and 278.8 nM respectively)[3]. AM630 is a protean ligand that can target a constitutively active form of the hCB(2) receptor (R*) with low affinity to produce agonism or neutral antagonism and a constitutively inactive form of this receptor (R) with much higher affinity to produce inverse agonism, and that the constitutive activity of whole cells is decreased less by pre-incubation with AM630 than with the higher-efficacy inverse agonist, SR144528[4]. AM251 and AM630 activated trigeminal (TG) sensory neurons in a concentration-dependent fashion (threshold 1 μM). AM630 (1-100 μM), but not AM251, was a significantly more potent agonist in cells co-expressing both TRPA1 and TRPV1 channels[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.98mL 0.40mL 0.20mL	9.91mL 1.98mL 0.99mL	19.83mL 3.97mL 1.98mL

参考文献

[1]Patil M, Patwardhan A, et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology. 2011 Sep;61(4):778-88. [2]Mukherjee S, Adams M, et al. Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors. Eur J Pharmacol. 2004 Nov 28;505(1-3):1-9. [3]Pertwee R, Griffin G, Fernando S, Li X, Hill A, Makriyannis A. AM630, a competitive cannabinoid receptor antagonist. Life Sci. 1995;56(23-24):1949-1955 [4]Bolognini D, Cascio MG, Parolaro D, Pertwee RG. AM630 behaves as a protean ligand at the human cannabinoid CB2 receptor. Br J Pharmacol. 2012;165(8):2561-2574 [5]Patil M, Patwardhan A, Salas MM, Hargreaves KM, Akopian AN. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology.2011;61(4):778-788