[3H]GBR 12935 labels mainly the piperazine acceptor site in the rat prefrontal cortex.
The binding characteristics of [3H]GBR 12935, a ligand for the dopamine (DA) transporter, have been extensively investigated in the striatum. The present study was designed to characterize [3H]GBR 12935-binding to prefrontal cortex (PFC) in rats. This region receives a dense DA input from the ventral tegmental area and is suspected to play a major role in higher associative functions. We demonstrated high-affinity, saturable, mazindol-sensitive [3H]GBR 12935-binding in the rat PFC; however, in contrast to the striatum, such binding was inhibited by increasing concentrations of Na+. This fact, together with the irregular pattern of the association kinetics and the marked sensitivity of [3H]GBR 12935-binding to piperazine derivatives, indicates the possible presence of more than one [3H]GBR 12935-binding site in the PFC. Furthermore, it appears that [3H] 12935 in the rat PFC labels mainly 'the piperazine acceptor site' and not the DA transporter.
Gordon
I
I
Department of Physiology and Pharmacology, Sackler Faculty of Medicine, Tel Aviv University, Isreal.
Weizman
R
R
Rehavi
M
M
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002352:Carrier Proteins / Q000378:metabolism; D018492:Dopamine Antagonists / Q000494:pharmacology*; D050483:Dopamine Plasma Membrane Transport Proteins; D005475:Flupenthixol / Q000494:pharmacology; D007700:Kinetics; D008024:Ligands; D008297:Male; D008454:Mazindol / Q000494:pharmacology; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D017072:Neostriatum / Q000187:drug effects / Q000378:metabolism; D009419:Nerve Tissue Proteins / Q000378:metabolism; D010879:Piperazines / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D017397:Prefrontal Cortex / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D012964:Sodium / Q000502:physiology
D002352:Carrier Proteins; D018492:Dopamine Antagonists; D050483:Dopamine Plasma Membrane Transport Proteins; D008024:Ligands; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D010879:Piperazines; C044630:1-(2 (diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine; D012964:Sodium; D008454:Mazindol; D005475:Flupenthixol