Me. Abood et Q. Tao, CHARACTERIZATION OF A DELTA-OPIOID RECEPTOR IN RAT PHEOCHROMOCYTOMA CELLS, The Journal of pharmacology and experimental therapeutics, 274(3), 1995, pp. 1566-1573
In one subclone of PC12 pheochromocytoma cells, PC12h, the levels of d
elta opioid receptors markedly increase in response to nerve growth fa
ctor (NGF). This increase, as assessed by [H-3]diprenorphine binding,
is found only under specific culture conditions. NGF treatment of PC12
h cells also results in the induction of delta opioid receptor (DOR-I)
mRNA. The time course for NGF induction of mRNA and protein is simila
r, although the levels of mRNA increase approximately 5-fold, whereas
the levels of receptor increase only 2-fold. Competition studies with
selective delta ([D-Pen(2,5)]-enkephalin, DPDPE), mu ([D-Ala(2),N-Me-P
he(4),Gly-ol(5)]-enkephalin, DAMGO) and kappa -N-[2-(1-pyrrolidinyl)-c
yclohexyl]-benzenacetamide methansulfonate salt, U50,488) opioid agoni
sts to displace [H-3]diprenorphine confirm that the delta subtype of o
pioid receptor is present on PC12h cells. The delta opioid receptor is
coupled functionally, as indicated by agonist inhibition of forskolin
-stimulated cAMP accumulation in a naloxone-reversible manner. Finally
, the delta opioid receptor was cloned from PC12h cells. The sequence
was identical with that described previously for the rat clone. The PC
12h cell line thus provides a model system in which to study regulatio
n of delta opioid receptors.