Determination of δ-opioid receptors in NG108-15 cells

Autor:	Jinchuan Zhao, Blythe B. Holmes, Begonia Y. Ho, James M. Fujimoto
Rok vydání:	1997
Předmět:	Pharmacology medicine.medical_specialty Enkephalin Antagonist Biology Naltrexone chemistry.chemical_compound Endocrinology Opioid chemistry Naltriben Internal medicine Benzylidene compounds medicine Binding site Receptor medicine.drug
Zdroj:	European Journal of Pharmacology. 319:109-114
ISSN:	0014-2999
Popis:	The delta-opioid receptors in mouse neuroblastoma x rat glioma NG108-15 cells were characterized by receptor binding and cAMP assays. Saturation binding assays using [3H][D-Pen5]enkephalin (DPDPE) or [3H][D-Ser2, Leu5, Thr6]enkephalin (DSLET) gave similar binding capacities (Bmax). Competition binding assays showed that DPDPE and DSLET have similar affinity for the [3H]DPDPE or 3[H]DSLET binding sites. The rank order of potency of competition with [3H]DPDPE and [3H]DSLET was similar: naltriben approximately DSLET > or = 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 delta-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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::daa3dfb772b1098cad0feb35abc49063 https://doi.org/10.1016/s0014-2999(96)00827-8 Zobrazit plný text záznamu Full Text from ScienceDirect