morphinans and 7-spiroindanyloxymorphone

morphinans has been researched along with 7-spiroindanyloxymorphone* in 1 studies

Other Studies

1 other study(ies) available for morphinans and 7-spiroindanyloxymorphone

Article	Year
Synthesis of 7-arylmorphinans. Probing the "address" requirements for selectivity at opioid delta receptors. Journal of medicinal chemistry, 1998, Jul-30, Volume: 41, Issue:16 Through arylation of 6-keto opiates with diaryliodonium iodide, a series of 7-aryl opiates (3-8) have been prepared in an effort to investigate the effect of conformational mobility of the delta "address" moiety on opioid agonist and antagonist potencies. Evaluation of the ligands in the mouse vas deferens and guinea pig ileum preparations revealed that they were less potent and less selective than the conformationally constrained ligands, naltrindole (1, NTI) and 7-(spiroindanyl)oxymorphone (2, SIOM), at delta opioid receptors. It is concluded that the coplanarity of the address moiety with the C ring of the morphinan structure enhances delta antagonist potency and selectivity. Topics: Animals; Electric Stimulation; Guinea Pigs; Ileum; In Vitro Techniques; Ligands; Male; Mice; Models, Molecular; Molecular Conformation; Morphinans; Muscle, Smooth; Naltrexone; Narcotic Antagonists; Oxymorphone; Pain Measurement; Receptors, Opioid, delta; Spiro Compounds; Vas Deferens	1998

Article

Year

Synthesis of 7-arylmorphinans. Probing the "address" requirements for selectivity at opioid delta receptors.

Journal of medicinal chemistry, 1998, Jul-30, Volume: 41, Issue:16

Through arylation of 6-keto opiates with diaryliodonium iodide, a series of 7-aryl opiates (3-8) have been prepared in an effort to investigate the effect of conformational mobility of the delta "address" moiety on opioid agonist and antagonist potencies. Evaluation of the ligands in the mouse vas deferens and guinea pig ileum preparations revealed that they were less potent and less selective than the conformationally constrained ligands, naltrindole (1, NTI) and 7-(spiroindanyl)oxymorphone (2, SIOM), at delta opioid receptors. It is concluded that the coplanarity of the address moiety with the C ring of the morphinan structure enhances delta antagonist potency and selectivity.

Topics: Animals; Electric Stimulation; Guinea Pigs; Ileum; In Vitro Techniques; Ligands; Male; Mice; Models, Molecular; Molecular Conformation; Morphinans; Muscle, Smooth; Naltrexone; Narcotic Antagonists; Oxymorphone; Pain Measurement; Receptors, Opioid, delta; Spiro Compounds; Vas Deferens

1998