Endogenous dopamine differently affects N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine and cocaine binding to the dopamine uptake complex.
1. [3H]N-[1-(2-Benzo(b)thiophenyl)cyclohexyl]piperidine ([3H]BTCP) labels in vivo the dopamine uptake complex in the mouse striatum. 2. In mice treated with gamma-butyrolactone (GBL, 400 mg/kg), [3H]BTCP specific binding was increased and ID50 values of BTCP and cocaine for the prevention of [3H]BTCP binding were significantly lowered. 3. In GBL-treated mice, cocaine (5 mg/kg, s.c.) had no effect on the BTCP ID50 value, whereas GBR 12783 (2 mg/kg, s.c.) increased it significantly. 4. Thus in vivo, endogenous dopamine and cocaine are competitive and non-competitive inhibitors, respectively, of the binding of [3H]BTCP.
Maurice
T
T
INSERM U 336, Ecole Nationale Supérieure de Chimie, Montpellier, France.
Barbanel
G
G
Vignon
J
J
D015107:4-Butyrolactone / Q000494:pharmacology; D000818:Animals; D003042:Cocaine / Q000493:pharmacokinetics*; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D004298:Dopamine / Q000494:pharmacology*; D018492:Dopamine Antagonists; D050483:Dopamine Plasma Membrane Transport Proteins; D066298:In Vitro Techniques; D008297:Male; D008565:Membrane Proteins / Q000378:metabolism*; D051379:Mice; D009419:Nerve Tissue Proteins / Q000378:metabolism*; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D010879:Piperazines / Q000494:pharmacology
D018492:Dopamine Antagonists; D050483:Dopamine Plasma Membrane Transport Proteins; D008565:Membrane Proteins; D009419:Nerve Tissue Proteins; D010879:Piperazines; C056415:1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine; C039737:1-(2-(diphenylmethoxy)ethyl)-4-(3-phenyl-2-propenyl)piperazine; D003042:Cocaine; D010622:Phencyclidine; D015107:4-Butyrolactone; D004298:Dopamine