Nonspecific effects of the selective kappa-opioid receptor agonist U-50,488H on dopamine uptake and release in PC12 cells.
kappa-Opioid receptor agonists decrease the levels of extracellular dopamine in vivo and in vitro. However, the mechanism(s) underlying these actions are unclear. The objective of this study was to distinguish between an effect of the selective kappa-opioid receptor agonist U-50,488H ((trans-(+/-)-3,4-dichloro-N-methyl-N-(2-[1-pyrrolidinyl]cyclohexyl)benzeneacetamide methanesulfonate) on secretion and reuptake of dopamine by PC12 cells. The data show that U-50,488H has both a modest effect to increase dopamine release and a more pronounced effect to inhibit dopamine uptake. Neither effect was sensitive to nor-binaltorphimine or naloxone, suggesting that they are not mediated through an opioid receptor.
Chudapongse
Nuannoi
N
Department of Pharmacology and Toxicology, University of Mississippi Medical Center, Jackson, MS 39216-4505, USA.
Kim
Seong-Youl
SY
Kramer
Robert E
RE
Ho
Ing K
IK
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer / Q000494:pharmacology*; D000818:Animals; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism*; D016716:PC12 Cells; D051381:Rats; D017473:Receptors, Opioid, kappa / Q000819:agonists* / Q000378:metabolism
D017473:Receptors, Opioid, kappa; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D004298:Dopamine