6N-cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions

Ian Derrick; Humphrey A. Moynihan; Jillian Broadbear; James H. Woods; John W. Lewis

doi:10.1016/0960-894X(95)00583-F

6N-cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions

Ian Derrick, Humphrey A. Moynihan, Jillian Broadbear, James H. Woods, John W. Lewis

Research output: Contribution to journal › Article › peer-review

12 Scopus citations

Abstract

6N-cinnamoyl-β-naltrexamine and its p-nitro derivative (7 and 8) are κ-opioid agonists of high potency and exceptional efficacy and are only weakly effective μ opioid antagonists. This contrasts with the p-methyl analogue which has only low efficacy κ-agonism but is a selective irreversible μ-antagonist like β-FNA.

Original language	English (US)
Pages (from-to)	167-172
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	6
Issue number	2
DOIs	https://doi.org/10.1016/0960-894X(95)00583-F
State	Published - Jan 23 1996
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/0960-894X(95)00583-F

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AU - Derrick, Ian

AU - Moynihan, Humphrey A.

AU - Broadbear, Jillian

AU - Woods, James H.

AU - Lewis, John W.

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Y1 - 1996/1/23

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AB - 6N-cinnamoyl-β-naltrexamine and its p-nitro derivative (7 and 8) are κ-opioid agonists of high potency and exceptional efficacy and are only weakly effective μ opioid antagonists. This contrasts with the p-methyl analogue which has only low efficacy κ-agonism but is a selective irreversible μ-antagonist like β-FNA.

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6N-cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions

Abstract

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