G2A (GPR132) Antagonist

NOX-6-18 (GPR132-B-160, Compound 25) is a GPR132 antagonist with an EC₅₀ value of 0.075 μM. NOX-6-18 has promote insulin secretion activity with an EC₅₀ value of 0.7 μM.

SB-583355 (Compound 56) is a potent G2A antagonist. SB-583355 can be prepared by a Suzuki reaction between 4-methoxyphenyl boronic acid and 3-bromo-4-hydroxybenzoic acid following the conditions followed by an amide coupling reaction. SB-583355 blocks the activation of G2A mediated either by 9-HOPE or T-10148 in human G2A expressing CHO-K1 cells. SB-583355 can be studied in research for inflammation, myeloid leukemia, and neuropathic pain.

NOX-6-18 (dihydrocholide) (GPR132-B-160, Compound 25) is a GPR132 antagonist with an EC₅₀ value of 0.075 μM. NOX-6-18 (dihydrocholide) has promote insulin secretion activity with an EC₅₀ value of 0.7 μM.

GPR132 antagonist-2 is a G2A (GPR132) antagonist with an IC₅₀ of 0.69 μM. GPR132 antagonist-2 exerts weak stabilizing effects on the bromodomain of BRD2 and exhibits selectivity for non-olfactory GPCRs. GPR132 antagonist-2 inhibits G2A activation, blocks downstream inositol monophosphate accumulation, reverses G2A-mediated TRPV1 sensitization, suppresses 9-HODE-mediated capsaicin-induced TRPV1 responses, and activates FPR3. GPR132 antagonist-2 can be used in studies related to neuropathic pain.