title: Human delta opioid receptor: a stable cell line for functional studies of opioids.
abstract: A human delta opioid receptor cDNA clone (pREP10/hDOR) was transfected into Chinese hamster ovary (CHO) cells. The stable cell line expressed a high density of delta opioid receptors (137,000 +/- 21,600 receptors/cell). DPDPE inhibited 90% of the forskolin-stimulated cAMP accumulation in these cells with high potency (EC50 = 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 delta 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 delta opioid receptor. The data support the use of the recombinant cell line for functional studies of opioid drugs.
authors.affiliation: Department of Pharmacology, University of Arizona, Tucson, USA.
authors.forename: E
authors.initials: E
authors.lastname: Malatynska
authors.forename: Y
authors.initials: Y
authors.lastname: Wang
authors.forename: R J
authors.initials: RJ
authors.lastname: Knapp
authors.forename: G
authors.initials: G
authors.lastname: Santoro
authors.forename: X
authors.initials: X
authors.lastname: Li
authors.forename: S
authors.initials: S
authors.lastname: Waite
authors.forename: W R
authors.initials: WR
authors.lastname: Roeske
authors.forename: H I
authors.initials: HI
authors.lastname: Yamamura
mesh_terms: D000818:Animals; D016466:CHO Cells; D005576:Colforsin / Q000037:antagonists & inhibitors; D006224:Cricetinae; D000242:Cyclic AMP / Q000378:metabolism; D020881:Enkephalin, D-Penicillamine (2,5)-; D004745:Enkephalins / Q000037:antagonists & inhibitors*; D006801:Humans; D009271:Naltrexone / Q000031:analogs & derivatives / Q000494:pharmacology; D011869:Radioligand Assay; D017465:Receptors, Opioid, delta / Q000037:antagonists & inhibitors / Q000187:drug effects*; D011994:Recombinant Proteins / Q000032:analysis
chemical_list: D004745:Enkephalins; D017465:Receptors, Opioid, delta; D011994:Recombinant Proteins; D005576:Colforsin; D009271:Naltrexone; D020881:Enkephalin, D-Penicillamine (2,5)-; D000242:Cyclic AMP; C055382:naltrindole