Interaction of tetrahydroisoquinolines and 3-aminotetralines with opioid μ-receptors

K. N. Yarygin, O. N. Ankudinova, A. M. Kotin

Institute of Experimental Cardiology, Cardiology Research Centre of the USSR, Academy of Medical Sciences, Moscow, Institute of Experimental Medicine, Academy of Medical Sciences of the USSR, Leningrad

Abstract: The interaction of the tetrahydroisoquinoline (THIQ) and 3-aminotetraline (3-AT derivatives with opioid μ-receptors has been studied. It is shown that THIQ and 3-AT derivatives bind to a site on the μ-receptor which these compounds are likely to share with “classical” opiates, whose structure also includes the 3-AT group. The binding site-for nonpeptide substances is in a strong allosteric interaction with the binding site for enkephalins. Some biological effects of THIQ and 3-AT derivatives can be explained in terms of their interaction with opioid receptors. One may speculate that the evolution of the endogenous opioid receptor ligands proceeded from simple 3-AT derivatives towards morphinans and, probably, benzomorphans.

Russian Journal of Bioorganic Chemistry 1991, 17 (9):1172-1176

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