Potentiation of transmitter release from NMB human neuroblastoma cells by kappa-opioids is mediated by N-type voltage-dependent calcium channels.
The selective kappa-opioid agonist trans-(+/-)-3, 4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl) cyclohexyl] benzenacetamidemethansulfonate (U50,488) potentiates both basal and depolarization-evoked [3H]dopamine release from NMB cells. The potentiation of dopamine release by U50,488 is mediated by N-type voltage-dependent calcium channels since it is blocked by omega-conotoxin, and is resistant to pertussis toxin (PTX)-treatment. When the stimulation of release by U50,488 is blocked by the N-channel antagonist omega-conotoxin, an inhibitory effect on dopamine release is revealed, suggesting that stimulatory and inhibitory effects of U50,488 are exerted in parallel.
Keren
O
O
Department of Physiology and Pharmacology, Sackler School of Medicine, Tel Aviv University, Tel Aviv, Israel. orak@post.tau.ac.il
Gafni
M
M
Sarne
Y
Y
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer / Q000494:pharmacology*; D000700:Analgesics / Q000494:pharmacology; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D020864:Calcium Channels, N-Type / Q000187:drug effects / Q000502:physiology*; D004298:Dopamine / Q000378:metabolism*; D020881:Enkephalin, D-Penicillamine (2,5)- / Q000494:pharmacology; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000494:pharmacology; D006801:Humans; D009447:Neuroblastoma; D037342:Pertussis Toxin; D011190:Potassium Cyanide / Q000494:pharmacology; D017473:Receptors, Opioid, kappa / Q000819:agonists*; D014407:Tumor Cells, Cultured; D010566:Virulence Factors, Bordetella / Q000494:pharmacology; D020960:omega-Conotoxins / Q000494:pharmacology
D000700:Analgesics; D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D017473:Receptors, Opioid, kappa; D010566:Virulence Factors, Bordetella; D020960:omega-Conotoxins; D004743:Enkephalin, Leucine; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; C034318:enkephalin, Ser(2), Leu(5), Thr(6)-; D020881:Enkephalin, D-Penicillamine (2,5)-; D037342:Pertussis Toxin; D011190:Potassium Cyanide; D004298:Dopamine