EEDQ, a tool for ex vivo measurement of occupancy of D-1 and D-2 dopamine receptors.
EEDQ (N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline) inactivates dopamine (DA) D-1 and D-2 receptors, measured by ex vivo [3H]SCH 23390 and [3H]spiperone binding in striatal homogenates. SCH 23390 (D-1 antagonist) and SK&F 38393 (D-1 agonist) protect against inactivation of D-1 receptors (ED50 values 0.075 and 53 mumol/kg, respectively). Raclopride (D-2 antagonist) and quinpirole (D-2 agonist) protect against inactivation of D-2 receptors (ED50 values 0.48 and 7.1 mumol/kg, respectively). The potencies correspond closely to those obtained by in vivo binding experiments using radioligands.
D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; D000818:Animals; D001552:Benzazepines / Q000378:metabolism / Q000494:pharmacology; D003342:Corpus Striatum / Q000378:metabolism; D004873:Ergolines / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D011804:Quinolines / Q000494:pharmacology; D019257:Quinpirole; D020891:Raclopride; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism*; D012457:Salicylamides / Q000494:pharmacology; D013134:Spiperone / Q000378:metabolism
D001552:Benzazepines; D004873:Ergolines; D011804:Quinolines; D011954:Receptors, Dopamine; D012457:Salicylamides; D019257:Quinpirole; D020891:Raclopride; D013134:Spiperone; C000470:EEDQ; D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine