Correspondency between different affinity states and target size of the bovine striatal D2 dopamine receptor.
Target size analysis of the D2 dopamine receptor in the bovine striatum revealed the presence of two populations of this receptor, in terms of apparent molecular size. The size of large target was approximately 150 X 10(4) daltons, while that of small target was 11 X 10(4) daltons. The antagonist [3H]spiperone labeled both large and small sized D2 receptors, while agonist [3H]n-propylapomorphine (NPA) labeled only the former. In addition, the apparent molecular size of a functional unit for the GTP effect was calculated to be 150 X 10(4) daltons, such appearing to be identical to that of large target sized D2 dopamine receptors. Therefore, the large sized D2 receptor, probably an oligomeric complex consisting of D2 receptor recognition protein and guanine nucleotide regulatory protein, has a high affinity for both agonist and antagonist, while the small sized receptor, probably a monomeric or dimeric receptor recognition protein, has a high affinity for only the antagonist.
D000110:Acetylcholinesterase / Q000378:metabolism; D000818:Animals; D001058:Apomorphine / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D002069:Butaclamol / Q000494:pharmacology; D002417:Cattle; D002462:Cell Membrane / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism*; D004298:Dopamine / Q000494:pharmacology; D006160:Guanosine Triphosphate / Q000494:pharmacology; D007700:Kinetics; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism* / Q000528:radiation effects; D017448:Receptors, Dopamine D2; D013134:Spiperone / Q000378:metabolism; D013469:Sulpiride / Q000494:pharmacology
D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D013134:Spiperone; C009074:N-n-propylnorapomorphine; D013469:Sulpiride; D006160:Guanosine Triphosphate; D002069:Butaclamol; D000110:Acetylcholinesterase; D001058:Apomorphine; D004298:Dopamine