Binding characteristics of the dopamine agonist/antagonist [3H]terguride (transdihydrolisuride) in the rat striatum.
The binding properties of [3H]terguride were studied in various regions of the rat brain. The highest density of [3H]terguride binding sites was found in the striatum and tuberculum olfactorium. In the striatum, the binding was saturable, stereoselective and of a high affinity. There was a good correlation between the inhibition of [3H]terguride and [3H]spiperone bindings by various dopaminergic agents. Drugs with affinity to another type of receptors did not displace [3H]terguride binding in the striatum; only SCH 23390 was effective. The experiments indicate a certain affinity of the ligand to D-1 receptors. Nevertheless, [3H]terguride appears to have an affinity to D-2 receptors in the striatum and, thanks to its dopamine agonistic/antagonistic profile, would be useful in the further study of dopamine receptors.
Valchár
M
M
Vrsecká
M
M
Krejcí
I
I
Dlabac
A
A
D000818:Animals; D001552:Benzazepines / Q000494:pharmacology; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism*; D004873:Ergolines / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D008090:Lisuride / Q000031:analogs & derivatives / Q000378:metabolism*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects*; D013134:Spiperone / Q000378:metabolism
D001552:Benzazepines; D004873:Ergolines; D011954:Receptors, Dopamine; C006208:dironyl; D013134:Spiperone; D008090:Lisuride