naltriben

Naltriben is a benzofuran-substituted derivative of naltrexone that functions as a potent pharmacological tool. It was originally identified and widely used as a highly selective antagonist for the delta-2 (δ2) opioid receptor, distinguishing it from the delta-1 subtype. More recently, naltriben has gained prominence in ion channel research as a potent activator of the Transient Receptor Potential Melastatin 7 (TRPM7) channel, a bifunctional chanzyme that regulates magnesium (Mg2+) homeostasis and possesses an intrinsic kinase domain. In experimental models, naltriben is employed to investigate the role of TRPM7 in cardiovascular protection, where its activation has been shown to ameliorate vascular dysfunction, inflammation, and fibrosis induced by magnesium deficiency. It is primarily utilized as a research reagent and is not currently approved for clinical use.

Other names

Naltriben mesylate