Date published: 2025-10-21

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GPR18 Inhibitors

Chemical inhibitors of GPR18 can exert their inhibitory effects through various mechanisms that involve competition with endogenous ligands, alteration of receptor conformation, and blockade of receptor signaling pathways. SR144528 is a selective CB2 receptor antagonist that can inhibit GPR18 by competing for the same binding sites or cellular pathways utilized by endogenous cannabinoids, which are natural ligands for GPR18. In a similar vein, AM251, which is primarily recognized for its antagonistic effect on CB1 receptors, also demonstrates the capacity to inhibit GPR18 by blocking the action of endogenous agonists, thereby preventing their potential to activate GPR18 signaling. O-1918, another selective antagonist, targets the abnormal cannabidiol receptor, which may encompass GPR18, and functions by preventing activation by compounds similar to abnormal cannabidiol that would otherwise engage GPR18. Further inhibition strategies involve the use of JTE-907, a CB2 receptor inverse agonist, which may promote an inactive conformation of GPR18, thereby reducing the receptor's responsiveness to activation signals. PSB-SB-1202, a selective GPR55 antagonist, could also inhibit GPR18 by competing with GPR18 for ligands or interfering with shared signaling pathways. Synthetic derivatives of cannabidiol, specifically designed to antagonize GPR18, function by occupying the receptor's active site, thus preventing the binding and activation of GPR18 by its natural ligands. Rimonabant and LY320135, both antagonists of the CB1 receptor, extend their inhibitory influence to GPR18 by occupying binding sites on GPR18 that are crucial for its activation.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

O-1918

536697-79-7sc-202746
sc-202746A
1 mg
5 mg
$60.00
$230.00
(0)

O-1918 is known to be a selective antagonist of the abnormal cannabidiol (abn-CBD) receptor, which may include GPR18, and can inhibit GPR18 function by preventing activation by abn-CBD-like compounds.

JTE 907

282089-49-0sc-203616
sc-203616A
10 mg
50 mg
$283.00
$1100.00
(0)

JTE-907 is a selective CB2 receptor inverse agonist, which may inhibit GPR18 by promoting an inactive state of the receptor due to its ability to induce conformational changes that prevent receptor activation.

PSB-SB1202

1399049-60-5sc-476366
2.5 mg
$380.00
(0)

PSB-SB-1202 is a selective GPR55 antagonist that may also inhibit GPR18 by competing for overlapping ligand-binding sites or signaling pathways, thereby reducing GPR18's activity.

Rimonabant

168273-06-1sc-205491
sc-205491A
5 mg
10 mg
$72.00
$160.00
15
(1)

Rimonabant is a CB1 receptor antagonist that can also inhibit GPR18 by occupying its binding sites, thereby preventing the receptor's normal activation by cannabinoid-like compounds.