EEDQ, a tool for ex vivo measurement of occupancy of D-1 and D-2 dopamine receptors

Eur J Pharmacol. 1988 Aug 24;153(2-3):309-11. doi: 10.1016/0014-2999(88)90621-8.

Abstract

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.

MeSH terms

  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine
  • Animals
  • Benzazepines / metabolism
  • Benzazepines / pharmacology
  • Corpus Striatum / metabolism
  • Ergolines / pharmacology
  • In Vitro Techniques
  • Male
  • Quinolines* / pharmacology
  • Quinpirole
  • Raclopride
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine / drug effects
  • Receptors, Dopamine / metabolism*
  • Salicylamides / pharmacology
  • Spiperone / metabolism

Substances

  • Benzazepines
  • Ergolines
  • Quinolines
  • Receptors, Dopamine
  • Salicylamides
  • Quinpirole
  • Raclopride
  • Spiperone
  • EEDQ
  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine