A series of trimethylpiperazine derivatives, struturally related to the μ-agonist 3-cinnamyl-8-propionyl-3,8-diazabicyclo[3.2.1]octane have been synthesized and rested in binding studies, using 3H-DAMGO as μ-selective ligand. Their different affinity towards μ-opioid receptors has been interpreted on the basis of a molecular modeling study performed through molecular mechanics calculations and high field 1H MNR spectroscopy.
2,2,6- and 2,3,5-trimethylpiperazines as monocyclic analogues of the mu-opioid agonist 3,8-diazabicyclo[3.2.1]octanes: Synthesis, modeling, and activity / M. Ballabio, D. Barlocco, G. Cignarella, D. Colombo, L. Toma. - In: TETRAHEDRON. - ISSN 0040-4020. - 53:4(1997), pp. 1481-1490.
2,2,6- and 2,3,5-trimethylpiperazines as monocyclic analogues of the mu-opioid agonist 3,8-diazabicyclo[3.2.1]octanes: Synthesis, modeling, and activity
M. BallabioPrimo
;D. BarloccoSecondo
;G. Cignarella;D. ColomboPenultimo
;
1997
Abstract
A series of trimethylpiperazine derivatives, struturally related to the μ-agonist 3-cinnamyl-8-propionyl-3,8-diazabicyclo[3.2.1]octane have been synthesized and rested in binding studies, using 3H-DAMGO as μ-selective ligand. Their different affinity towards μ-opioid receptors has been interpreted on the basis of a molecular modeling study performed through molecular mechanics calculations and high field 1H MNR spectroscopy.Pubblicazioni consigliate
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