The alpha 2-adrenoceptor antagonist, (+)-efaroxan, enhances acetylcholine release in the rat cortex in vivo.
Noradrenergic modulation of the cortical cholinergic system in vivo was studied by examining the effect of the selective alpha 2-adrenoceptor antagonist (+)-efaroxan on cortical acetylcholine outflow in the conscious rat, using the microdialysis technique. (+)-Efaroxan produced a dose-dependent increase in acetylcholine outflow (up to 300% at 0.63 mg/kg) which persisted for up to 3 h and which was stereospecific. The results demonstrate that rat cortical acetylcholine release can be augmented by (+)-efaroxan and that alpha 2-adrenoceptors may be involved. (+)-Efaroxan may have therapeutic potential in disorders in which cortical acetylcholine release is deficient.
Tellez
S
S
Division Neurobiologie I, Centre de Recherche Pierre Fabre, Castres, France.
Colpaert
F
F
Marien
M
M
D000109:Acetylcholine / Q000378:metabolism*; D000317:Adrenergic alpha-Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D001572:Benzofurans / Q000008:administration & dosage / Q000494:pharmacology*; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D007093:Imidazoles / Q000008:administration & dosage / Q000494:pharmacology*; D008297:Male; D017551:Microdialysis; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism
D000317:Adrenergic alpha-Antagonists; D001572:Benzofurans; D007093:Imidazoles; C062597:efaroxan; D000109:Acetylcholine