Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists

Stephen M. Husbands; John W. Lewis

doi:10.1016/0960-894X(95)00522-1

Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists

Stephen M. Husbands
, John W. Lewis

University of Bristol

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

Abstract

A series of morphinan derivatives which are cyclic imines and pyrrolidines containing a constrained phenyl group has been synthesised and tested for their opioid receptor binding affinity. In opioid binding assays the ligands displayed very high affinity particularly for μ receptors and some showed substantial μ selectivity.

Original language	English
Pages (from-to)	2969-2974
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	5
Issue number	24
DOIs	https://doi.org/10.1016/0960-894X(95)00522-1
Publication status	Published - 21 Dec 1995

Funding

Acknowledgement: The attthors acknowledge the National Institute for Drug Abuse for the funding to carry out this work (NIDA Grant no. DAO-7315) and also for the binding work carried out under grant no. N01DA-4-8307 at the Stanford Research Institute.

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)00522-1

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title = "Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists",

abstract = "A series of morphinan derivatives which are cyclic imines and pyrrolidines containing a constrained phenyl group has been synthesised and tested for their opioid receptor binding affinity. In opioid binding assays the ligands displayed very high affinity particularly for μ receptors and some showed substantial μ selectivity.",

author = "Husbands, \{Stephen M.\} and Lewis, \{John W.\}",

year = "1995",

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T1 - Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group

T2 - High affinity opioid agonists

AU - Husbands, Stephen M.

AU - Lewis, John W.

PY - 1995/12/21

Y1 - 1995/12/21

N2 - A series of morphinan derivatives which are cyclic imines and pyrrolidines containing a constrained phenyl group has been synthesised and tested for their opioid receptor binding affinity. In opioid binding assays the ligands displayed very high affinity particularly for μ receptors and some showed substantial μ selectivity.

AB - A series of morphinan derivatives which are cyclic imines and pyrrolidines containing a constrained phenyl group has been synthesised and tested for their opioid receptor binding affinity. In opioid binding assays the ligands displayed very high affinity particularly for μ receptors and some showed substantial μ selectivity.

UR - https://www.scopus.com/pages/publications/0028846956

U2 - 10.1016/0960-894X(95)00522-1

DO - 10.1016/0960-894X(95)00522-1

M3 - Article

AN - SCOPUS:0028846956

SN - 0960-894X

VL - 5

SP - 2969

EP - 2974

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 24

ER -

Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists

Abstract

Funding

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