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*Compound via MeSH
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Hazardous Substances DB
*N,N'-BIS(2-METHYLPHENYL)GUANIDINE
*PENTAZOCINE

Vol. 286, Issue 1, 163-171, July 1998

Sigma Ligands Stimulate the Electrical Activity of Frog Pituitary Melanotrope Cells through a G-Protein-Dependent Inhibition of Potassium Conductances1

Olivier Soriani , Hubert Vaudry , Yan Ai Mei , François Roman and Lionel Cazin

European Institute for Peptide Research (IFRMP no. 23), Laboratory of Cellular and Molecular Neuroendocrinology, INSERM U413, UA CNRS, University of Rouen, 76821 Mont-Saint-Aignan (O.S., H.V., Y.A.M., L.C.) and Institut de Recherche Jouveinal, 3-9 rue de la Loge, 94260 Fresnes, France (O.S., H.V., Y.A.M., L.C., F.R.)

We have investigated the effects of sigma ligands [1,3-di(2-tolyl)guanidine (DTG) and (+)-pentazocine] on the electrical activity of cultured frog pituitary melanotrope cells by using the patch-clamp technique. DTG and (+)-pentazocine (10 µM each) induced a reversible depolarization associated with an increase in membrane resistance and action potential firing. In voltage-clamp experiments, DTG and (+)-pentazocine elicited inward currents whose intensity augmented with membrane depolarization. The currents vanished or reversed between -90 and -100 mV, at values close to the K+ equilibrium potential (EK+ = -102 mV). DTG (2-500 µM) and (+)-pentazocine (0.2-200 µM) reduced the outward delayed rectifier K+ current [IK (V)] in a dose-dependent manner with EC50 of 64 and 37 µM, respectively. In contrast, naloxone (50 µM) and pirenzepine (10 µM) did not affect the sigma ligand-induced inhibition of IK (V). Addition of guanosine-5'-O-(3-thiophosphate) in the pipette solution irreversibly sustained the DTG-induced current whereas guanosine-5'-O-(2-thiodiphosphate) virtually suppressed the response. Cholera toxin-pretreatment (1 µg/ml; 18 hr) abolished the inward current and the inhibition of IK (V) induced by sigma ligands. In contrast, pretreatment with pertussis toxin (1 µg/ml; 18 hr) had no effect. Taken together, these data indicate that DTG and (+)-pentazocine activate the electrical activity of cultured frog melanotrope cells by reducing both a tonic K+ current and a voltage-dependent [IK (V)] K+ conductance through the activation of a cholera toxin-sensitive G-protein.

0022-3565/98/2861-0163$03.00/0
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Copyright © 1998 by The American Society for Pharmacology and Experimental Therapeutics


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