. Author manuscript; available in PMC: 2010 Mar 1.

Published in final edited form as: Prostaglandins Other Lipid Mediat. 2009 Jul 15;89(3-4):105–111. doi: 10.1016/j.prostaglandins.2009.07.001

Table 2.

Pharmacological profile of compounds tested as GPR119 ligands.

Compound	Cell type	Measured response	Effect, EC₅₀ value	[Reference]
Cannabinoids
Anandamide	hGPR119-yeast	Fluorimetric assay	very weak	[57]
OEA	hGPR55-HEK293	↑cAMP	EC₅₀2.9 µM	[57]
	hGPR55-yeast	Fluorimetric assay	EC₅₀3.2 µM	[57]
	mGPR55-yeast	Fluorimetric assay	EC₅₀2.9 µM	[57]
PEA	hGPR55-yeast	Fluorimetric assay	EC₅₀3.2 µM, low efficacy	[57]
2-AG	hGPR55-yeast	Fluorimetric assay	no effect	[57]
CP5594	hGPR55-yeast	Fluorimetric assay	no effect	[57]
WIN55212-2	hGPR55-yeast	Fluorimetric assay	no effect	[57]
JWH133	hGPR55-yeast	Fluorimetric assay	no effect	[57]
Lysophospholipids
Oleoyl LPC	hGPR119-RH7777	↑cAMP	EC₅₀1.5 µM	[58]
	hGPR55-yeast	Fluorimetric assay	EC₅₀ >30 µM	[57]
	mGPR55-yeast	Fluorimetric assay	EC₅₀ >30 µM	[57]
Palmitoyl LPC	hGPR119-RH7777	↑cAMP	EC₅₀1.6 µM	[58]
Stearoyl LPC	hGPR119-RH7777	↑cAMP	EC₅₀3.3 µM	[58]
LP-ethanolamine	hGPR119-RH7777	↑cAMP	EC₅₀5.7 µM	[58]
LPI	hGPR119-RH7777	↑cAMP	EC₅₀5.7 µM	[58]
Synthetic ligands
PSN632408	hGPR55-HEK293	↑cAMP	EC₅₀1.9 µM	[57]
	hGPR55-yeast	Fluorimetric assay	EC₅₀5.6 µM	[57]
	mGPR55-yeast	Fluorimetric assay	EC₅₀7.9 µM	[57]
AR231453	hGPR55-HEK293	↑cAMP	EC₅₀5.7 nM	[59]
	HIT-T15	↑cAMP	EC₅₀4.7 nM	[59]
	HIT-T15	insulin release	EC₅₀3.5 nM	[59]
	GLUtag	↑cAMP	EC₅₀4.3 nM	[59]
	GLUtag	GLP-1 release	EC₅₀56 nM	[59]