Table 1.

Activity of MAGL and FAAH inhibitors tested for their analgesic effects.

Inhibitors	Compounds	IC50	Analgesic Effects and Targets	Ref
FAAH	OL135	5 nM	Attenuation of mechanical and cold allodynia	[112]
	PF3845	514 nM	Attenuation of mechanical and cold allodynia	[119,120,151]
	URB597	5 nM	Moderate thermal antinociception. Anti-allodynic effect in inflammatory pain. Decreased hyperalgesia in the TGVS	[115,116,122]
	URB937	26.8 nM	Inhibition of nocifensive behavior. Decreased peripheral nociception	[121,152]
MAGL	JZL184	262 nM	Behavioral analgesic effects. Reduction of NTG-induced hyperalgesia of spinal and TGVS origin	[130,131,135,136]
	URB602	280 nM	Reduction of NTG-induced hyperalgesia of spinal and TGVS origin	[129,131]
	KML29	43 nm	Behavioral analgesic effect	[45,132,133,134]
	MJN110	<100 nM	Attenuation of mechanical allodynia and thermal hyperalgesia	[138,139]
	JJKK-048	<0.4 nM	Not tested	[123]
Dual MAGL FAAH	JZL195	13 nM FAAH 19 nM MAGL	Reduction of peripheral and cephalic pain	[145]
	AKU-005	0.2–1.1 nM MAGL 63 nM FAAH	Not tested	[141]

Inhibitor potencies defined by IC₅₀ values in rat brain membranes (OL135, URB597, URB937, JZL184, URB602, KML29, MJN110, JZL195), Colo cell line (PF3845) and rat cerebellar membranes (JJKK-048, AKU-005).