The search for the dopamine receptor: tribulations.
In an attempt to identify specific binding to dopamine receptors the binding of 3H-pimozide to preparations of brain and to an artificial cellulose membrane was examined. Binding occurred rapidly, was pH and temperature dependent, and was displaceable by other neuroleptics. Displaceable binding was saturable at 5 X 10(-8) M pimozide. A weak correlation between IC50's for displacement of binding by drugs and their clinical potencies was observed. Displaceable binding of 3H-pimozide in different brain areas did not correlate with dopamine levels. The similarity of binding properties to brain and to artificial membrane suggests that these effects are a function of the physical-chemical properties of these drugs, and that these properties may be related to their clinical effect.
D002746:Chlorpromazine / Q000494:pharmacology; D003956:Dialysis; D004298:Dopamine / Q000502:physiology*; D005476:Fluphenazine / Q000494:pharmacology; D006220:Haloperidol / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D008567:Membranes, Artificial; D010868:Pimozide / Q000494:pharmacology; D011398:Promethazine / Q000494:pharmacology; D011955:Receptors, Drug / Q000187:drug effects; D013696:Temperature; D013997:Time Factors
D008567:Membranes, Artificial; D011955:Receptors, Drug; D010868:Pimozide; D011398:Promethazine; D006220:Haloperidol; D005476:Fluphenazine; D002746:Chlorpromazine; D004298:Dopamine