N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, an irreversible receptor inactivator, as a tool for measurement of alpha 2-adrenoceptor occupancy in vivo.
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.
Pilc
A
A
Institute of Pharmacology, Polish Academy of Sciences, Smetna.
Nowak
G
G
Zak
J
J
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D003000:Clonidine / Q000378:metabolism; D008297:Male; D011804:Quinolines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism*; D015016:Yohimbine / Q000378:metabolism
D000317:Adrenergic alpha-Antagonists; D011804:Quinolines; D011942:Receptors, Adrenergic, alpha; D015016:Yohimbine; C000470:EEDQ; D003000:Clonidine