Nonpeptidic delta ligands

NALTRINDOLE AS A LEAD FOR THE DEVELOPMENT OF NONPEPTIDE DELTA LIGANDS... 

Keywords 8 Agonists 8 Antagonists Diphenylmethylpiperazines Nonpeptidic delta ligands SNC 80... 

Benzhydrylpiperazines as Nonpeptidic Delta Opioid Receptor Ligands... 

Constant, P., Davodeau, F., Peyrat, M. A., Poquet, Y., Puzo, G., and Bonneville, M. et al. (1994). Stimulation of human gamma delta T cells by nonpeptidic mycobacterial ligands. Science 264(5156), 267-270. 

Calderon SN, Rice KC, Rothman RB et al (1997) Probes for narcotic receptor mediated phenomena. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(aR)-a-((2 S,5R)-4-allyl-2,5-dimethyl-l-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid receptor ligands. J Med Chem 40 695-704... 

JH. Discriminative stimulus effects of BW373U86 a nonpeptide ligand with selectivity for delta opioid receptors. J Pharmacol Exp Ther 1993 267 888-895. 

Due to their high selectivity, DER and DEL were the basis for an extensive structure activity relationship study aimed to understand the essential requisites of p. and 8 activity. More than 200 analogues of DER and DEL C were synthesized, and the role of each amino acid in binding to p and 8 receptors and bioactivity was defined [21-31]. New synthetic products were prepared such as oxymorphindole and related derivatives [32], and (+)-4-[(alfa R)-alfa-((2S,5R)-4-allyl-2.5-dimethyl-l-piperazin-yl)-3-methoxy-benzyl]-N, diethylbenzamide [33]. These products are under investigation for their clinical relevance and provide potential nonpeptide ligands for studies on delta-opioid-receptor. 

Shenderovich, M.D., Liao, S., Qian, X. and Hmby, V.J. (2000) A three-dimensional model of the delta-opioid pharmacophore comparative molecular modeling of peptide and nonpeptide ligands. Biopolym. 53 565-580. 

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