cyclomethyline

Cyclomethyline is a multifunctional small molecule ligand that acts as an $\alpha_{2C}$-adrenergic receptor agonist, an $\alpha_{2A}$-adrenergic receptor antagonist, and a 5-HT$_{1A}$ receptor agonist. Developed by researchers at the University of Camerino, cyclomethyline has been investigated preclinically for its potential in managing opioid use disorder, specifically by reducing morphine withdrawal symptoms and alleviating associated depressive symptoms. Unlike non-subtype-selective $\alpha_2$-adrenergic agonists like clonidine, cyclomethyline's $\alpha_{2A}$-adrenergic receptor antagonism avoids the sedative and hypotensive side effects typically associated with $\alpha_{2A}$ activation, while its $\alpha_{2C}$-adrenergic agonism and 5-HT$_{1A}$ agonism synergistically alleviate withdrawal and exert potent antidepressant-like effects.

Other names

(R)-(-)-2-[1-(2-(cyclopropylmethyl)phenoxy)ethyl]-4,5-dihydro-1H-imidazole(R)-(-)-cyclomethyline(S)-(+)-2-[1-(2-(cyclopropylmethyl)phenoxy)ethyl]-4,5-dihydro-1H-imidazole(S)-(+)-cyclomethyline(±)-cyclomethyline2-[1-(2-(cyclopropylmethyl)phenoxy)ethyl]-4,5-dihydro-1H-imidazole