Determination of δ-opioid receptors in NG108-15 cells

• Published in: European journal of pharmacology Vol. 319; no. 1; pp. 109 - 114
• Main Authors: Ho, Begonia Y., Holmes, Blythe B., Zhao, Jinchuan, Fujimoto, James
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 01.01.1997; Elsevier
• Subjects: Biological and medical sciences; BNTX (7-benzylidenenaltrexone); Cell receptors; Cell structures and functions; DPDPE ([ d-Pen 2, d-Pen 5]enkephalin); DSLET ([ d-Ser 2,Leu 5,Thr 6]enkephalin); Fundamental and applied biological sciences. Psychology; Molecular and cellular biology; Naltriben; Neuropeptide receptors; NG108-15 cell; δ-Opioid receptor; BNTX (7-benzylidenenaltrexone); δ-Opioid receptor; NG108-15 cell; DPDPE ([ d-Pen 2, d-Pen 5]enkephalin); DSLET ([ d-Ser 2,Leu 5,Thr 6]enkephalin); Naltriben; Molecular structure; Opiate receptor δ; Rodentia; Cyclic AMP; Functional analysis; Identification; In vitro; Vertebrata; Biological fixation; Mammalia; Structure activity relation; Mouse; Animal; Established cell line; Affinity
• ISSN: 0014-2999; 1879-0712
• DOI: 10.1016/S0014-2999(96)00827-8

The δ-opioid receptors in mouse neuroblastoma X rat glioma hybridoma NG108-15 cells were characterized by receptor binding and cAMP assays. Saturation binding assays using [ 3H]naltrindole, [ 3H][ d-Pen 2, d-Pen 5]enkephalin (DPDPE) or [ 3H][ d-Ser 2,Leu 5,Thr 6]enkephalin (DSLET) gave similar binding capacities ( B max). Competition binding assays showed that DPDPE and DSLET have similar affinity for the [ 3H]DPDPE or [ 3H]DSLET binding sites. The rank order of potency of competition with [ 3H]DPDPE and [ 3H]DSLET was similar: naltriben ∼ DSLET ≥ DPDPE > 7-benzylidenenaltrexone (BNTX). Both DPDPE and DSLET were found to decrease cAMP formation. The action of DSLET was antagonized by naltriben but not BNTX, while the action of DPDPE was reversed by both antagonists. Therefore, the δ-opioid receptor in NG108-15 cells has similar affinity for the agonists DPDPE and DSLET, and a higher affinity for the antagonist naltriben than BNTX.