Selective nonpeptide ligands as probes to explore δ opioid receptor architecture
Pharmacochemistry Library, ISSN: 0165-7208, Vol: 24, Issue: C, Page: 303-312
1996
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Article Description
This chapter discusses the selective non peptide ligands as probes to explore δ opioid receptor architecture. The relatively recent molecular cloning and sequencing of opioid receptors have confirmed the numerous pharmacologic and structure-activity relationship studies that have suggested the existence of multiple opioid receptors. Numerous ligands have been developed as potential opioid receptor probes in an effort to distinguish between different types of opioid receptors. These include peptide and nonpeptide agonists and antagonists. The chapter discusses the design and structure-activity relationship studies of δ-selective nonpeptide ligands and the role of conformation of the “address” moiety in conferring selectivity to the δ 1 and δ 2 subtypes of opioid receptors. Structure-activity relationship studies have suggested that agonist and antagonist ligands bind to separate or overlap recognition sites on δ opioid receptors. These sites exhibit different conformational requirements for the address component. In this regard, nonpeptide agonists require the plane of the aromatic group to be approximately orthogonal to the plane of ring C in the opiate. On the other hand, there are no specific conformational requirements for antagonists because the aromatic group that comprises the address may be coplanar to ring C or oriented orthogonally.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0165720896800249; http://dx.doi.org/10.1016/s0165-7208(96)80024-9; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77957090771&origin=inward; http://linkinghub.elsevier.com/retrieve/pii/S0165720896800249; https://linkinghub.elsevier.com/retrieve/pii/S0165720896800249; http://dx.doi.org/10.1016/s0165-7208%2896%2980024-9; https://dx.doi.org/10.1016/s0165-7208%2896%2980024-9
Elsevier BV
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