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The experiment was conducted on transfected CHO-cell proteins that expressed sufficient numbers of human receptor subtypes with varying concentrations of [3H]-spiperone, a known antagonist for dopaminergic activity, to test for saturation concentrations. The antagonist activity for non-specific binding was conducted in the presence of (+)-butaclamol, a known antagonist as well with lower inhibition capabilities than [3H]-spiperone, while total binding activity was tested in the presence of the (-)-butaclamol isomer, that has even lesser affinity that its isomeric counterpart…
This may later prove valuable to drug development against disorders like schizophrenia that is caused by excessive dopaminergic activity.
The variations in physiologic actions of dopamine are mediated by at least five distinct G protein coupled receptor types (Missale, C., et al, 1998). Kebabian and Calne (1979) distinguished two dopamine receptor types - and - that can be differentiated 'pharmacologically, biologically, physiologically and by their anatomical distribution' (Civelli, O., 2000). Since the analysis is on receptors only they are being discussed here. Subsequent cloning of receptors revealed that they belonged to the supergene family of the G-protein coupled receptors (Civelli, O., 2000). The three subtypes belonging to the -like sub-family are the, and ones that inhibit adenylyl cyclase and activate channels (Missale, C., et al, 1998). The genetic structure of the and vary by tissue types and species' through alternative splicing. The subtype is highly polymorphic. ...
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