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Covariation of alpha 2-adrenoceptor density and function following irreversible antagonism with EEDQ.

Abstract
1. Administration of the irreversible antagonist, N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, (EEDQ, 2 mg kg-1, i.p.) to mice reduced binding of [3H]-RX 821002 (2-methoxy-idazoxan) to alpha 2-adrenoceptors in whole mouse brain by 75% 24 h later. The receptor binding returned over time only being reduced by 25% by 16 days post administration; the time taken for binding to return to 50% of control levels was estimated to be 5.25 days. 2. EEDQ administration also resulted in the loss of the sedative effect of the alpha 2-adrenoceptor agonist, medetomidine, measured by the holeboard test of directed exploration and locomotor activity. Agonist-induced sedation returned to control values by 8 days post EEDQ administration. 3. EEDQ administration also resulted in the loss of the hypothermic response to medetomidine (0.1 mg kg-1, i.p.). Medetomidine-induced hypothermia returned to control values by 12 days post EEDQ administration. 4. Pretreatment with the selective alpha 2-adrenoceptor antagonist, RX 821002 (0.1-3.0 mg kg-1, i.p.) 45 min before EEDQ prevented the loss of alpha 2-adrenoceptors as well as the blockade of medetomide-induced sedation and hypothermia by EEDQ. 5. The results of these experiments indicate that there is significant receptor reserve for alpha 2-adrenoceptor-mediated behavioural and physiological responses.
AuthorsM J Durcan, P F Morgan, M L Van Etten, M Linnoila
JournalBritish journal of pharmacology (Br J Pharmacol) Vol. 112 Issue 3 Pg. 855-60 (Jul 1994) ISSN: 0007-1188 [Print] England
PMID7921612 (Publication Type: Journal Article)
Chemical References
  • Adrenergic alpha-2 Receptor Antagonists
  • Adrenergic alpha-Agonists
  • Adrenergic alpha-Antagonists
  • Dioxanes
  • Hypnotics and Sedatives
  • Imidazoles
  • Quinolines
  • Receptors, Adrenergic, alpha-2
  • EEDQ
  • 2-methoxyidazoxan
  • Medetomidine
  • Idazoxan
Topics
  • Adrenergic alpha-2 Receptor Antagonists
  • Adrenergic alpha-Agonists (pharmacology)
  • Adrenergic alpha-Antagonists (pharmacology)
  • Animals
  • Body Temperature (drug effects)
  • Dioxanes (pharmacokinetics)
  • Drug Interactions
  • Exploratory Behavior (drug effects)
  • Hypnotics and Sedatives (pharmacology)
  • Idazoxan (analogs & derivatives)
  • Imidazoles (pharmacology)
  • Male
  • Medetomidine
  • Mice
  • Motor Activity (drug effects)
  • Quinolines (pharmacology)
  • Radioligand Assay
  • Receptors, Adrenergic, alpha-2 (metabolism)

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