Publication | Closed Access
Human δ opioid receptor
27
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References
1995
Year
Cellular PharmacologyPharmacotherapyExperimental PharmacologyCellular PhysiologyMolecular PharmacologyHuman δAddiction MedicineHealth SciencesDpdpe ActivityMolecular PhysiologyReceptor (Biochemistry)NeuropharmacologyPharmacologyCell BiologySignal TransductionAddictionδ Receptor AntagonismPhysiologyNeuropeptide ReceptorCellular BiochemistryMedicineOpioid Use Disorder
A HUMAN δ opioid receptor cDNA clone (pREP10/hDOR) was transfected into Chinese hamster ovary (CHO) cells. The stable cell line expressed a high density of δ opioid receptors (137 000 × 21 600 receptors/cell). DPDPE inhibited 90% of the forskolin-stimulated cAMP accumulation in these cells with high potency (EC5C = 1.3 nM). This effect of DPDPE was antagonized by naltrindole. The pseudo-pA2 value (Ke) of 155 pM for naltrindole is consistent with that measured for δ receptor antagonism in the mouse vas deferens. This is the first detailed characterization of DPDPE activity on forskolin-stimulated cAMP accumulation mediated through a human δ opioid receptor. The data support the use of the recombinant cell line for functional studies of opioid drugs.