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ET Piros, PL Prather, PY Law, CJ Evans and TG Hales
Department of Psychiatry, University of California Los Angeles, School of Medicine 90024, USA.
To study cloned opioid receptor binding and modulation of both adenylyl cyclase and ion channel activity, we stably expressed mu- and delta- opioid receptors in the rodent pituitary-derived GH3 cell line. GH3 cells express G proteins and voltage-activated Ca2+ channels (predominantly of the L-type). Activation of cloned rat mu-opioid receptors expressed in GH3 cells (termed GH3MOR cells) inhibits L-type Ca2+ channel activity. GH3MOR cells, further transfected with mouse delta receptor cDNA (termed GH3MORDOR cells), bound both [D-Ala2,N- MePhe4,Gly-ol5]enkephalin (DAMGO) and [D-Pen2,D-Pen5]enkephalin (DPDPE). These opioid ligands inhibited adenylyl cyclase activity (IC50 = 174 and 0.53 nM, respectively). This action of DAMGO and DPDPE was attenuated selectively by mu- and delta-opioid receptor-specific antagonists. Activation of both opioid receptors also led to inhibition of Ca2+ channel activity, measured with Ba2+ as the charge carrier using the whole-cell patch-clamp technique. Both DAMGO (1 microM) and DPDPE (1 microM) reversibly inhibited Ba2+ currents (by 17.0 +/- 1.4% and 20.7 +/- 1.3%, respectively) in GH3MORDOR cells. The inhibitory action of DPDPE was dose dependent (IC50 = 1.6 nM) and was attenuated by pretreatment with pertussis toxin (200 ng/ml) or by the inclusion of guanosine-5'-O-(2-thio)diphosphate (2 mM) in the recording electrode. Ba2+ current inhibitions by both DAMGO and DPDPE were completely reversed by depolarizing (to > 50 mV) prepulses in GH3MORDOR cells. In summary, cloned mu- and delta-opioid receptors expressed in GH3 cells voltage-dependently couple through Gi/G(o) proteins to L-type Ca2+ channels.
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