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2,2,6- and 2,3,5-Trimethylpiperazines as monocyclic analogues of the μ-opioid agonist 3,8-diazabicyclo[3.2.1]octanes: Synthesis, modeling, and activity

✍ Scribed by Manuela Ballabio; Daniela Barlocco; Giorgio Cignarella; Diego Colombo; Lucio Toma

Publisher
Elsevier Science
Year
1997
Tongue
French
Weight
478 KB
Volume
53
Category
Article
ISSN
0040-4020

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✦ Synopsis

A series of trimethyipiperazine derivatives, structurally related to the Ix-agonist 3-cinnamyl-8-propionyl-3,8-diazabicyclo[3.2.1]octane, have been synthesized and teswxl in binding studies, using 3H-DAMGO as Ix-selective ligand. Their different affinity towards Ix-opioid receptors has been interpreted on the basis of a molecular modeling study performed through molecular mechanics calculations and high field IH MNR spectroscopy.

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ChemInform Abstract: 2,2,6- and 2,3,5-Tr
ChemInform Abstract: 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 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 33 KB 👁 1 views

Trimethylpiperazines as Monocyclic Analogues of the . mu.-Opioid Agonist 3,8-Diazabicyclo(3.2.1)octanes: Synthesis, Modeling, and Activity. -The trimethylpiperazine derivatives (IV)-(VII) are tested in binding studies for µ-opioid receptors. Their different affinity towards . mu.-opioid receptors i