CIM0216

CIM0216 is a synthetic, small-molecule, cell-permeable isoxazolyl-phenylacetamide-based compound that acts as a potent, selective, and reversible agonist (superagonist) of the transient receptor potential melastatin 3 (TRPM3) ion channel. It has an EC50 of approximately 770 nM in HEK293-TRPM3 cells, greatly exceeding the potency of the canonical TRPM3 agonist pregnenolone sulfate. CIM0216 activates both the central calcium-conducting pore and an alternative cation permeation pathway of TRPM3, showing high selectivity over other TRP channels such as TRPM1, TRPM2, TRPM4-8, and TRPV1. While primarily utilized as a research tool to study TRPM3 physiology, neurogenic inflammation, nociception, and vascular biology, it has been investigated in in vitro pharmacology studies by Erasmus MC and Universitair Medisch Centrum Rotterdam to evaluate TRPM3-mediated vasodilation in human dermal arteries from normotensive and preeclamptic pregnancies.

Other names

3,4-dihydro-N-(5-methyl-3-isoxazolyl)-α-phenyl-1(2H)-quinolineacetamide2-(3,4-dihydroquinolin-1(2H)-yl)-N-(5-methylisoxazol-3-yl)-2-phenylacetamide