Immuno-photoaffinity labeling of the D2-dopamine receptor.
Azido-haloperidol was synthesized and applied as a photoaffinity ligand for the D2-dopamine receptor. In bovine striatal membranes, azido-haloperidol bound reversibly to the receptor (KD = 15 nM), and when exposed to light, it bound to the receptor irreversibly. This irreversible inactivation was prevented by the dopaminergic agonist N-propylnorapomorphine or the dopaminergic antagonists haloperidol and (+)-butaclamol. The photoaffinity labeled D2-receptor was probed with anti-haloperidol antibodies following gel electrophoresis and transfer to nitrocellulose. A major polypeptide of 94 kDa reacted with the anti-haloperidol antibodies. This polypeptide band was not observed when the photoaffinity labeling was performed in the presence of (+)-butaclamol or spiperone.
Kanety
H
H
Department of Chemical Immunology, Weizmann Institute of Science, Rehovot, Israel.
Fuchs
S
S
D000345:Affinity Labels / Q000378:metabolism*; D000818:Animals; D001058:Apomorphine / Q000031:analogs & derivatives / Q000494:pharmacology; D001386:Azides / Q000378:metabolism; D002069:Butaclamol / Q000494:pharmacology; D002417:Cattle; D003342:Corpus Striatum / Q000378:metabolism; D006220:Haloperidol / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D007158:Immunologic Techniques; D007700:Kinetics; D008970:Molecular Weight; D010777:Photochemistry; D011954:Receptors, Dopamine / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism
D000345:Affinity Labels; D001386:Azides; D011954:Receptors, Dopamine; C057173:haloperidol 4-azidobenzoate; D013134:Spiperone; C009074:N-n-propylnorapomorphine; D002069:Butaclamol; D006220:Haloperidol; D001058:Apomorphine