Differential desensitization of human delta-opioid receptors by peptide and alkaloid agonists.

Abstract	The efficacy of different opioid agonists to induce acute desensitization of the human delta-opioid receptor-mediated inhibition of cAMP accumulation was investigated in the neuroblastoma cell line SK-N-BE, which endogenously expresses these receptors. While etorphine, a non-selective alkaloid agonist, caused 50% desensitization after a 30-min incubation, the same treatment in the presence of the selective peptide agonists, DPDPE ([D-Pen2,D-Pen5]enkephalin) and deltorphin I (Tyr-D-Ala-Phe-Asp-Val-Val-Gly), almost totally desensitized the delta-opioid receptor-mediated inhibition of adenylyl cyclase. When SK-N-BE cells were prechallenged either with alkaloid or peptide agonist, we observed a cross-desensitization that was less marked when cells were pretreated with peptide agonists and then challenged with etorphine. Taken together, these results demonstrate that human delta-opioid receptors are differentially desensitized by alkaloid and peptide agonists.
Authors	S Allouche, M Roussel, N Marie, P Jauzac
Journal	European journal of pharmacology (Eur J Pharmacol) Vol. 371 Issue 2-3 Pg. 235-40 (Apr 29 1999) ISSN: 0014-2999 [Print] Netherlands
PMID	10357261 (Publication Type: Comparative Study, Journal Article)
Chemical References	Adenylyl Cyclase Inhibitors Alkaloids Analgesics Analgesics, Opioid Enkephalins Oligopeptides Peptides Receptors, Opioid, delta deltorphin I, Ala(2)- Naloxone Etorphine Enkephalin, D-Penicillamine (2,5)- Cyclic AMP
Topics	Adenylyl Cyclase Inhibitors Alkaloids (pharmacology) Analgesics (pharmacology) Analgesics, Opioid (pharmacology) Cyclic AMP (metabolism) Drug Interactions Enkephalin, D-Penicillamine (2,5)- Enkephalins (pharmacology) Etorphine (pharmacology) Humans Naloxone (pharmacology) Neuroblastoma (enzymology, genetics) Oligopeptides (pharmacology) Peptides (pharmacology) Receptors, Opioid, delta (drug effects) Tumor Cells, Cultured

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