Species variation in dopamine receptor binding.
Binding of 3H-spiroperidol, 3H-apomorphine and 3H-ADTN (2-amino-6,7-dihydroxytetrahydronaphthalene) associated with dopamine receptors has been evaluated in corpus striatal membranes of calf, rat and human brains. Substantial species differences are apparent for numberous agonists and antagonists in competing for receptor binding. In general, dopamine receptor antagonists are more potent in rat and agonists more potent in calf. In competing for 3H-spiroperidol binding sulpiride, molindone and metaclopramide show the most pronounced species differences, being 3--10 times more potent in rat and human than in calf. In all three species agonists compete for 3H-spiroperidol binding with Hill coefficients less than one while antagonists inhibit 3H-spiroperidol binding with Hill coefficients of about 1.0. Conversely, 3H-apomorphine and 3H-ADTN binding in all three species is inhibited by antagonists with Hill coefficients less than 1.0 while agonists display Hill coefficients of about 1.0. In general agonists are more potent in competing for binding of 3H-apomorphine and 3H-ADTN than 3H-spiroperidol. However, a small component of dopamine, apomorphine and ADTN inhibition of 3H-spiroperidol binding displays very high affinity (IC50 about 1 nM). In human amygdala 3H-spiroperidol appears to label serotonin receptors predominantly.
D000818:Animals; D001058:Apomorphine / Q000378:metabolism; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D002417:Cattle; D002421:Caudate Nucleus / Q000378:metabolism; D005476:Fluphenazine / Q000378:metabolism; D006220:Haloperidol / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D011954:Receptors, Dopamine / Q000378:metabolism*; D013045:Species Specificity; D013134:Spiperone / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000378:metabolism
D011954:Receptors, Dopamine; D013764:Tetrahydronaphthalenes; D013134:Spiperone; D006220:Haloperidol; D001058:Apomorphine; D005476:Fluphenazine