Autoradiographic evaluation of [11C]vinpocetine binding in the human postmortem brain.
The main objective ofthe study was to evaluate with autoradiographic technique whether or not [11C]vinpocetine, a compound widely used in the prevention and treatment of cerebrovascular diseases (Cavinton, Gedeon Richter Ltd., Budapest), binds to specific sites in the human brain in post mortem human brain sections. Binding was assessed under four conditions: the incubation was performed using Tris-HCl buffer with or without the addition of salts (0.1% (weight/vol) ascorbic acid, 120 mM NaCl, 5 mM KCl, 2 mM CaCl2 and 1 mM MgCl2), with or without the addition of excess (10 microM) unlabelled vinpocetine. Measurements on digitized autoradiograms indicated that [11C]vinpocetine labelled all grey matter areas in the human brain to a similar extent and no significantly heterogeneous binding could be demonstrated among cortical or subcortical regions. The addition of excess unlabelled vinpocetine lowered the binding slightly in all regions. Although these results indicate that [11C]vinpocetine does not bind to human brain transmitter receptors or transporters with a high affinity (Ki < 10 nM), it cannot be ruled out that the compound binds to receptors and/or transporters with lower affinity.
Hall
H
H
Karolinska Institutet, Department of Clinical Neuroscience, Karolinska Hospital, Stockholm, Sweden.
Varnäs
K
K
Sandell
J
J
Halldin
C
C
Farde
L
L
Vas
A
A
Kárpáti
E
E
Gulyás
B
B
D001345:Autoradiography; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D002250:Carbon Radioisotopes; D006801:Humans; D066298:In Vitro Techniques; D011180:Postmortem Changes; D011956:Receptors, Cell Surface / Q000378:metabolism; D014018:Tissue Distribution; D014748:Vinca Alkaloids / Q000378:metabolism*
D002250:Carbon Radioisotopes; D011956:Receptors, Cell Surface; D014748:Vinca Alkaloids; C013983:vinpocetine