[Interaction of tetrahydroisoquinolines and 3-aminotetralines with opioid mu-receptors].
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.
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KN
Iarygin
O N
ON
Ankudinova
A M
AM
Kotin
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D015259:Dopamine Agents / Q000378:metabolism; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D004745:Enkephalins / Q000378:metabolism; D007546:Isoquinolines / Q000378:metabolism*; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism*; D017450:Receptors, Opioid, mu; D013696:Temperature; D044005:Tetrahydroisoquinolines; D013764:Tetrahydronaphthalenes / Q000378:metabolism
D015259:Dopamine Agents; D004745:Enkephalins; D007546:Isoquinolines; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; D044005:Tetrahydroisoquinolines; D013764:Tetrahydronaphthalenes; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; C006561:2-aminotetralin; C011639:ADTN; C014843:1,2,3,4-tetrahydroisoquinoline
Vzaimodeĭstvie tetragidroizokhinolinov i 3-aminotetralinov s opioidnymi mu-retseptorami.