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

Resultado de la investigación: Article › revisión exhaustiva

12 Citas (Scopus)

Resumen

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.

Idioma original	English (US)
Páginas (desde-hasta)	167-172
Número de páginas	6
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	6
N.º	2
DOI	https://doi.org/10.1016/0960-894X(95)00583-F
Estado	Published - ene 23 1996
Publicado de forma externa	Sí

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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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.

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

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