Phenyl-substituted Normethadones: Synthesis and Pharmacology-Reference-Cited by-同舟云学术

Phenyl-substituted Normethadones: Synthesis and Pharmacology

Published:1995-03 Issue:3 Volume:47 Page:237-242
ISSN:2042-7158
Container-title:Journal of Pharmacy and Pharmacology
language:en
Short-container-title:

Author:

Mbela T K N¹,Poupaert J H²¹,Cumps J²¹,Moussebois C²¹,Haemers A³¹,Borloo M³¹,Dumont P²¹

Affiliation:

1. Department of Pharmaceutics and Drug Analysis, Laboratory of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Kinshasa, PO Box 212, Kinshasa 11, Zaire

2. Department of Pharmaceutical Sciences, Laboratory of Medicinal Chemistry, School of Pharmacy, Catholic University of Louvain (UCL), 73, Av. E. Mournér 7340, B-1200 Brussels, Belgium

3. Department of Pharmaceutical Chemistry, University of Antwerp (UIA) Universiteitsplein 1, B-2610 Antwerpen, Belgium

Abstract

Abstract Phenyl-substituted normethadone derivatives were synthesized and their affinity (IC50) for opioid receptors was determined by displacement of the specific binding sites of [3H]sufentanyl on rat brain preparations. Substitution resulted in a decrease of affinity in-vitro. These results suggest that normethadone-like compounds may interact with the P subsite of the μ-opioid receptor and that the P subsite has a well-defined cavity shape of stringent dimensions.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Link

http://academic.oup.com/jpp/article-pdf/47/3/237/36998385/j.2042-7158.1995.tb05786.x.pdf

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