The hypothesis that benzodiazepine-induced hyperphagia is due to a specific enhancement of the palatability of foods has been supported by previous 'taste reactivity' studies of affective (hedonic and aversive) reactions to taste palatability. Diazepam and chlordiazepoxide enhance hedonic reactions of rats (rhythmic tongue protrusions, etc.) to sweet tastes in a receptor-specific fashion. A rol...

The expedient synthesis of various 1,4-benzodiazepine-2,5-dione compounds, particularly those having substituents at the C3-, N1- and N4-positions is achieved. The important features in these synthetic strategies include: (i) using the coupling reaction of isatoic anhydride with alpha-amino ester for direct construction of the core structure of 1,4-benzodiazepine-2,5-dione; (ii) using potassium...

A recognition site for benzodiazepines structurally different from that linked to the gamma-aminobutyric acid receptor subtype A or the "central type" benzodiazepine receptor has been located mainly in the outer membranes of mitochondria and designated mitochondrial benzodiazepine receptor (MBR). A putative endogenous ligand for MBR is the peptide, diazepam binding inhibitor (DBI), which inhibi...

A single 5 min exposure to the elevated plus-maze test of anxiety renders animals insensitive to the anxiolytic effects of the benzodiazepines in this test. The purpose of the present experiments was to explore whether this phenomenon resulted from a change in the functional state of benzodiazepine receptors in the dorsal raphe nucleus. The benzodiazepine receptor agonist midazolam (0.5, 1, and...

The globus pallidus occupies a critical position in the 'indirect' pathway of the basal ganglia and, as such, plays an important role in the modulation of movement. In recent years, the importance of the globus pallidus in the normal and malfunctioned basal ganglia is emerging. However, the function and operation of various transmitter systems in this nucleus are largely unknown. GABA is the ma...

In a previous study, it was found that positive, palatability-dependent consummatory reactions in rats to intraorally infused tastes were facilitated by chlordiazepoxide (10 mg/kg). In contrast, the rats' more neutral or aversive reactions to these tastes were not facilitated by chlordiazepoxide. This suggested that chlordiazepoxide might selectively enhance the positive palatability of tastes....

The anticonvulsant activity of Astragalus squarrosus total extract was assessed in pentylenetetrazole (PTZ)-induced convulsion in mice, with diazepam as the standard drug, while mechanistic studies were also conducted using flumazenil, a GABA A-benzodiazepine receptor complex site antagonist. The extract produced protection against convulsion at 400 mg/kg, comparable with protection of benzodia...

In this study, we investigated the effects of the peripheral benzodiazepine ligands, Ro5-4864 (putative agonist) and PK 11195 (putative antagonist) on prolactin stimulated mitogenesis in Nb2 cells. Ro5-4864 and PK 11195 at 10-9 M maximally enhanced prolactin stimulated mitogenesis. At 10-6 M Ro5-4864 inhibited prolactin stimulated mitogenesis. Clonazepam, a ligand for the central benzodiazepine...