The synthesis of new 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2, 4]benzotriazine 5-oxides and their binding activities at the central benzodiazepine receptor (BZR) are reported. The derivatives substituted at the 3-position with electron-rich five-membered rings, such as pyrrole 11, 2-thiophene 13c, or 3-thiophene 13d, showed good affinity values for BZR. In in vivo tests the 3-(thien-3-yl)-8-chl...

Recent studies have suggested that 3,4-methylenedioxymethamphetamine (MDMA; "ecstasy"), a synthetic amphetamine derivative, might exhibit an anxiogenic-like activity in rodents. In this work, we examined the effects of MDMA (1, 8 and 15 mg kg(-1), i.p.) on social encounters between male mice using an ethopharmacological approach. Likewise, we compared the behavioural profile of MDMA with that i...

Monoclonal antibodies to a purified benzodiazepine/GABAA receptor complex from bovine cerebral cortex were used to determine the localization of this receptor in immunohistochemical preparations of the human hippocampal formation. The regional localization of the receptor was compared with the autoradiographic distribution of binding sites for a benzodiazepine antagonist, Ro 15-1788, and very s...

The interactions of the anthelmintic agent avermectin B1a, the anticonvulsant pentobarbital, and the anxiolytic tracazolate with the gamma-aminobutyric acid (GABA) receptor . chloride ion channel complex in rat brain membrane were studied. The results indicated that they all potentiated ligand binding to the GABA and benzodiazepine receptors. The stimulatory effects of avermectin B1a and pentob...

Separate sub-populations of benzodiazepine receptors are involved in determining hippocampal theta frequency in freely moving rats. Systemic injection of the benzodiazepine chlordiazepoxide (CDP) reduced the frequency of theta elicited by stimulation of the brainstem reticular formation, and theta recorded during fixed interval (FI) bar pressing. Infusion of the benzodiazepine receptor antagoni...

Benzodiazepines (BDZs) are known to increase the amplitude and duration of IPSCs. Moreover, at low [GABA], BDZs strongly enhance GABAergic currents suggesting the up-regulation of agonist binding while their action on gating remains a matter of debate. In the present study we have examined the impact of flurazepam and zolpidem on mIPSCs by investigating their effects on GABA(A)R binding and gat...

Benzodiazepine agonists stimulate feeding in animals. This paper reviews evidence which indicates that benzodiazepine-induced feeding is due to a specific enhancement of the perceived palatability of food and fluids, and is not a mere secondary consequence of anxiety reduction. In studies of the effect of benzodiazepines on affective reactions that are naturally elicited from rats by tastes, we...

Receptor binding studies were undertaken in an attempt to identify and characterize pharmacologically and functionally distinct receptor sites for gamma-aminobutyric acid (GABA) in rat brain. The results indicated that the potency of bicuculline, a GABA receptor antagonist, to displace membrane-bound [3H]GABA varies significantly among different brain regions, with the greatest potency found in...