A single dose of FG 7142 causes long-term increases in mouse cortical beta-adrenoceptors.
There is evidence that central monoamines are involved in the actions of benzodiazepines. We have investigated the effects of a single dose of the benzodiazepine partial inverse agonist, FG 7142, on radioligand binding to alpha 2- and beta-adrenoceptors in mouse cerebral cortex. We found that seven days after a single injection of FG 7142 there was a large increase in the density of beta-adrenoceptors. This rise was not detectable either 15-30 min, or 24 h after the injection and no statistically significant changes in alpha 2-adrenoceptor binding were found at any of these times. Administration of the benzodiazepine antagonist Ro 15-1788 at the same time as FG 7142 prevented the rise in beta-adrenoceptor density. We discuss the possibility that the beta-adrenoceptor upregulation is related to the behavioural effects of FG 7142.
D000818:Animals; D001067:Appetite Depressants / Q000494:pharmacology*; D002243:Carbolines / Q000494:pharmacology*; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D004082:Dihydroalprenolol; D005442:Flumazenil / Q000494:pharmacology; D008297:Male; D051379:Mice; D011943:Receptors, Adrenergic, beta / Q000096:biosynthesis*
D001067:Appetite Depressants; D002243:Carbolines; D011943:Receptors, Adrenergic, beta; D005442:Flumazenil; D004082:Dihydroalprenolol; C035874:FG 7142