N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, an irreversible receptor inactivator, as a tool for measurement of alpha 2-adrenoceptor occupancy in vivo

A Pilc; G Nowak; J Zak

doi:10.1016/0014-2999(92)90081-e

N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, an irreversible receptor inactivator, as a tool for measurement of alpha 2-adrenoceptor occupancy in vivo

Eur J Pharmacol. 1992 Feb 25;212(1):109-11. doi: 10.1016/0014-2999(92)90081-e.

Authors

A Pilc¹, G Nowak, J Zak

Affiliation

¹ Institute of Pharmacology, Polish Academy of Sciences, Smetna.

PMID: 1348228
DOI: 10.1016/0014-2999(92)90081-e

Abstract

In rats treatment with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) induces a dose-dependent decrease in the number of alpha 2-adrenoceptors. Prior injection of alpha-adrenergic agents such as yohimbine and clonidine protect alpha 2-adrenoceptors against the effects of EEDQ. The ED50 values for yohimbine and clonidine were 10.27 and 5.83 mumol/kg, respectively.

MeSH terms

Adrenergic alpha-Antagonists / pharmacology*
Animals
Cerebral Cortex / drug effects*
Cerebral Cortex / metabolism
Clonidine / metabolism
Male
Quinolines / pharmacology*
Rats
Rats, Inbred Strains
Receptors, Adrenergic, alpha / drug effects
Receptors, Adrenergic, alpha / metabolism*
Yohimbine / metabolism

Substances

Adrenergic alpha-Antagonists
Quinolines
Receptors, Adrenergic, alpha
Yohimbine
EEDQ
Clonidine