Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors

…, G Ronsisvalle, SW Tam, AE Takemori

Index: Portoghese; Larson; Sayre; Yim; Ronsisvalle; Tam; Takemori Journal of Medicinal Chemistry, 1986 , vol. 29, # 10 p. 1855 - 1861

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Citation Number: 102

Abstract

Bivalent ligands containing the oxymorphamine or naltrexamine pharmacophores connected to spacers of varying length were synthesized and evaluated for their selectivity at 1.1, K, and 6 opioid receptors. The oxymorphamine bivalent ligands (1-8) behaved as p agonists on the electrically stimulated guinea pig ileum longitudinal muscle preparation (GPI). The spacer that conferred peak agonist activity in these series contains a total of ...