Chronic administration of the selective dopamine uptake inhibitor GBR 12909, but not cocaine, produces marked decreases in dopamine transporter density

1997 ◽  
Vol 356 (5) ◽  
pp. 562-569 ◽  
Author(s):  
Paul M. Kunko ◽  
Richard J. Loeloff ◽  
S. Izenwasser
Keyword(s):  
Dopamine Transporter ◽  
Chronic Administration ◽  
Dopamine Uptake ◽  
Gbr 12909 ◽  
Uptake Inhibitor ◽  
Selective Dopamine

A Tolerance Study of Single and Multiple Dosing of the Selective Dopamine Uptake Inhibitor GBR 12909 in Healthy Subjects

1990 ◽  
Vol 5 (4) ◽  
pp. 237-252 ◽  
Author(s):  
U. SØGAARD ◽  
J. MICHALOW ◽  
B. BUTLER ◽  
A. LUND LAURSEN ◽  
S. H. INGERSEN ◽  
...  
Keyword(s):  
Healthy Subjects ◽  
Dopamine Uptake ◽  
Gbr 12909 ◽  
Multiple Dosing ◽  
Uptake Inhibitor ◽  
Tolerance Study ◽  
Selective Dopamine

Phencyclidine and related compounds evoke [3H]dopamine release from rat mesencephalic cell cultures by a mechanism independent of the phencyclidine receptor, sigma binding site, or dopamine uptake site

1990 ◽  
Vol 68 (9) ◽  
pp. 1200-1206 ◽  
Author(s):  
Howard Mount ◽  
Patricia Boksa ◽  
Isabelle Chaudieu ◽  
Rémi Quirion
Keyword(s):  
Binding Site ◽  
Cell Cultures ◽  
Dopamine Release ◽  
Channel Blocker ◽  
Dopamine Uptake ◽  
Gbr 12909 ◽  
Related Compounds ◽  
Sigma Ligand ◽  
Selective Dopamine ◽  
Mesencephalic Cells

At concentrations ≥100 μM, phencyclidine (PCP), N-(1-(2-thienyl)-cyclohexyl)piperidine (TCP), and MK-801 induced [3H]dopamine release from dissociated cell cultures of rat mesencephalon. This release was Ca2+ independent and tetrodotoxin insensitive. Tetrodotoxin (2 μM) itself had no effect on spontaneous release of [3H]dopamine. [3H]Dopamine release was induced by 1,3-di(2-tolyl)guanidine, a sigma ligand, and by 4-aminopyridine (1–3 mM), a K+ channel blocker. No stereoselectivity was observed for [3H]dopamine release evoked by the dioxadrol enantiomers, dexoxadrol, and levoxadrol, or by enantiomers of N-allylnormetazocine (SKF 10,047). The selective dopamine uptake inhibitor 1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (GBR 12909) did not affect spontaneous or TCP-evoked [3H]dopamine release. Together, these data suggest that the dopamine-releasing effects of PCP-like compounds on the mesencephalic cells were not mediated by actions at the PCP receptor or sigma binding site, Ca2+, or Na+ channels, or at the high affinity dopamine uptake site. It remains conceivable that blocking actions of PCP-like compounds at voltage-regulated K+ channels may at least partly explain the response. These results are discussed in comparison with findings in intact brain.Key words: dopamine, phencyclidine, cell culture, mesencephalon.

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