Several monocyclic derivatives structurally related to the μ-opioid agonist 3-cinnamyl-8 propionyl-3,8-diazabicyclo[3.2. 1]octane have been synthesized and tested in binding studies using the μ-selective 3H-DAMGO as ligand. Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards μ-opioid receptors.
MONOCYCLIC ANALOGS OF THE MU-OPIOID AGONIST 3,8-DIAZABICYCLO-[3.2.1]OCTANES - SYNTHESIS, MODELING, AND ACTIVITY / D. BARLOCCO, S. VILLA, W. FRATTA, P. FADDA, D. COLOMBO, L. TOMA. - In: TETRAHEDRON. - ISSN 0040-4020. - 51:42(1995), pp. 11547-11556.
MONOCYCLIC ANALOGS OF THE MU-OPIOID AGONIST 3,8-DIAZABICYCLO-[3.2.1]OCTANES - SYNTHESIS, MODELING, AND ACTIVITY
D. BARLOCCOPrimo
;S. VILLASecondo
;D. COLOMBOPenultimo
;
1995
Abstract
Several monocyclic derivatives structurally related to the μ-opioid agonist 3-cinnamyl-8 propionyl-3,8-diazabicyclo[3.2. 1]octane have been synthesized and tested in binding studies using the μ-selective 3H-DAMGO as ligand. Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards μ-opioid receptors.
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