to obtain drugs which are more selective at benzodiazepine (bzd) receptors, design and synthesis of functionally selective ligands for bzd receptors is the current strategy of our pharmaceutical chemistry department. the affinity of newly synthesized ligands is assessed by radioligand receptor binding assays. based on our previous studies, 2-phenyl-5-oxo-7-methyl-1,3,4-oxadiazolo[a,2,3]-pyrimid...

Recent advances in molecular biology and complementary information derived from neuropharmacology, biochemistry and behavior have dramatically increased our understanding of various aspects of GABAA receptors. These studies have revealed that the GABAA receptor is derived from various subunits such as alpha1-alpha6, beta1-beta3, gamma1-gamma3, delta, epsilon, pi, and rho1-3. Furthermore, two ad...

To obtain drugs which are more selective at benzodiazepine (BZD) receptors, design and synthesis of functionally selective ligands for BZD receptors is the current strategy of our pharmaceutical chemistry department. The affinity of newly synthesized ligands is assessed by radioligand receptor binding assays. Based on our previous studies, 2-phenyl-5-oxo-7-methyl-1,3,4-oxadiazolo[a,2,3]-pyrimid...

Modulatory agents of gamma-aminobutyric acid type A (GABAA) receptors have been widely used for more than 40 years to treat anxiety, epilepsy, and sleep disorders; these drugs are generally safe, well tolerated, and effective. Recently, there has been a substantial growth in understanding of the mechanism of action of these drugs, which act at different sites on GABAA receptors. A variety of GA...

The properties of the inhibitory influence of neurons in the perigeniculate (PGN) nucleus on thalamocortical cells were examined with intracellular recordings in the ferret geniculate slice maintained in vitro. Activation of PGN neurons with the local application of glutamate caused IPSPs in thalamocortical neurons that were mediated by both GABAA and GABAB receptors, as well as the activation ...

Social anxiety disorder (SAD) is the one of the most common anxiety disorders. Despite its high prevalence, the disorder is still considerably undiagnosed and untreated. The disease places a massive burden on patient’s lives, affecting not only their social interactions but also their educational and professional activities, thereby constituting a severe disability. γ-aminobutyric acid (GABA) s...

To obtain drugs which are more selective at benzodiazepine (BZD) receptors, design and synthesis of functionally selective ligands for BZD receptors is the current strategy of our pharmaceutical chemistry department. The affinity of newly synthesized ligands is assessed by radioligand receptor binding assays. Based on our previous studies, 2-phenyl-5-oxo-7-methyl-1,3,4-oxadiazolo[a,2,3]-pyrimid...

Fear can be considered as a functional defense behavior to protect living beings against dangerous situation. In our studies we have investigated the fear behavior in rats in elevated plus maze .The increase in two parameters percent of open arm entries (%OAE) and percent of time spent in the open arms (% OAT) and decrease in the percent of time spent in closed arm (%CAT) was considered as fear...

Fear can be considered as a functional defense behavior to protect living beings against dangerous situation. In our studies we have investigated the fear behavior in rats in elevated plus maze .The increase in two parameters percent of open arm entries (%OAE) and percent of time spent in the open arms (% OAT) and decrease in the percent of time spent in closed arm (%CAT) was considered as fear...