A novel analogue of clonidine with opiate-receptor agonist activity

Daphna Atlas*, Steven L. Sabol

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

A new analogue of the α2-adrenergic receptor ligand clonidine, N-(4-hydroxphenacetyl)-4-aminoclonidine, was synthesized. The analogue possesses opiate-receptor agonist activity in addition to α-adrenergic partial agonist activity. The analogue elicits inhibition of adenylate cyclase of NG108-15 neuroblastoma × glioma hybrid cells; most of the inhibition is reversed by the opiate-receptor antagonist naloxone. The analogue also inhibits the binding of [3H]D-Ala2-Met5-enkephalinamide and [3H]dihydromorphine to rat brain opiate receptors. The structure of the analogue suggests common elements in the ligand binding sites of α- and opiate receptors and may lead to a new class of opiate analgesics.

Original languageEnglish
Pages (from-to)924-931
Number of pages8
JournalBiochemical and Biophysical Research Communications
Volume94
Issue number3
DOIs
StatePublished - 16 Jun 1980
Externally publishedYes

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