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

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
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
Publication status	Published - 23 Jan 1996
Externally published	Yes

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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.",

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AU - Derrick, Ian

AU - Moynihan, Humphrey A.

AU - Broadbear, Jillian

AU - Woods, James H.

AU - Lewis, John W.

PY - 1996/1/23

Y1 - 1996/1/23

N2 - 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.

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.

UR - https://www.scopus.com/pages/publications/0030058349

U2 - 10.1016/0960-894X(95)00583-F

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JF - Bioorganic and Medicinal Chemistry Letters

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ER -

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

Abstract

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