N-cyclohexylethyl-N-noroxymorphindole: A μ-opioid preferring analogue of naltrindole

Andrew Coop; Arthur E. Jacobson; Mario D. Aceto; Louis S. Harris; John R. Traynor; James H. Woods; Kenner C. Rice

doi:10.1016/S0960-894X(00)00479-0

N-cyclohexylethyl-N-noroxymorphindole: A μ-opioid preferring analogue of naltrindole

Andrew Coop, Arthur E. Jacobson, Mario D. Aceto, Louis S. Harris, John R. Traynor, James H. Woods, Kenner C. Rice

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

8 Scopus citations

Abstract

The position of the indole in the indolomorphinans, which includes the δ opioid antagonist naltrindole, is considered to be responsible for the δ opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be μ preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands. (C) 2000 Elsevier Science Ltd.

Original language	English (US)
Pages (from-to)	2449-2451
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	10
Issue number	21
DOIs	https://doi.org/10.1016/S0960-894X(00)00479-0
State	Published - Nov 6 2000
Externally published	Yes

ASJC Scopus subject areas

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

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title = "N-cyclohexylethyl-N-noroxymorphindole: A μ-opioid preferring analogue of naltrindole",

abstract = "The position of the indole in the indolomorphinans, which includes the δ opioid antagonist naltrindole, is considered to be responsible for the δ opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be μ preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands. (C) 2000 Elsevier Science Ltd.",

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AU - Jacobson, Arthur E.

AU - Aceto, Mario D.

AU - Harris, Louis S.

AU - Traynor, John R.

AU - Woods, James H.

AU - Rice, Kenner C.

PY - 2000/11/6

Y1 - 2000/11/6

N2 - The position of the indole in the indolomorphinans, which includes the δ opioid antagonist naltrindole, is considered to be responsible for the δ opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be μ preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands. (C) 2000 Elsevier Science Ltd.

AB - The position of the indole in the indolomorphinans, which includes the δ opioid antagonist naltrindole, is considered to be responsible for the δ opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be μ preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands. (C) 2000 Elsevier Science Ltd.

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