BW373U86, its enantiomers, and related compounds: Interactions of non-peptide delta agonists at multiple δcx binding sites in rat brain

X. Y. Cha, H. Xu, S. N. Calderon, L. E. Smith, K. C. Rice, Frank Porreca, R. B. Rothman

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Previous studies delineated two classes of δ binding sites: a δ binding site not associated with the opioid receptor complex, termed the δncx site, and a δ site associated with the opioid receptor complex, termed the δcx site (for review see (1)). More recent studies resolved two δcx binding sites in rat brain termed δcx-1 and δcx-2 (2). Pretreatment of membranes with the δ-selective acylating agent (+)-trans-SUPERFIT depletes membranes of the δncx binding site which permits selective labeling of the δcx binding sites with [3H]DADLE (3). Ligand-selectivity studies of the non-peptide δ agonist, BW373U86, its enantiomers and related compounds showed that these drugs have higher affinities for δ sites than μ sites (4,5). This study determined the selectivity of these compounds for the two δcx binding sites. The data indicate that (+)-4-[(αR)-α((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC80) and deltorphin-II are highly selective for δcx-2 binding site (2758-fold and 700-fold respectively). In contrast, morphine is selective for δcx-1 binding site (78-fold).

Original languageEnglish (US)
Pages (from-to)45-46
Number of pages2
JournalRegulatory Peptides
Volume54
Issue number1
DOIs
StatePublished - Nov 10 1994

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Enantiomers
Rats
Brain
Binding Sites
Opioid Receptors
Leucine-2-Alanine Enkephalin
Membranes
BW 373U86
Labeling
Morphine
Ligands
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Neuroscience(all)

Cite this

BW373U86, its enantiomers, and related compounds : Interactions of non-peptide delta agonists at multiple δcx binding sites in rat brain. / Cha, X. Y.; Xu, H.; Calderon, S. N.; Smith, L. E.; Rice, K. C.; Porreca, Frank; Rothman, R. B.

In: Regulatory Peptides, Vol. 54, No. 1, 10.11.1994, p. 45-46.

Research output: Contribution to journalArticle

Cha, X. Y. ; Xu, H. ; Calderon, S. N. ; Smith, L. E. ; Rice, K. C. ; Porreca, Frank ; Rothman, R. B. / BW373U86, its enantiomers, and related compounds : Interactions of non-peptide delta agonists at multiple δcx binding sites in rat brain. In: Regulatory Peptides. 1994 ; Vol. 54, No. 1. pp. 45-46.
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