Interaction of tetrahydroisoquinolines and 3-aminotetralines with opioid mu-receptors
Iarygin, K.N.; Ankudinova, O.N.; Kotin, A.M.
Bioorganicheskaia Khimiia 17(9): 1172-1176
1991
ISSN/ISBN: 0132-3423 PMID: 1687237 Document Number: 379316
The interaction of the tetrahydroisoquinoline (THIQ) and 3-aminotetraline (3-AT derivatives with opioid .mu.-receptors has been studied. It is shown that THIQ and 3-AT derivatives bind to a site on the .mu.-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.