Objectives: The purpose of this review is to reiterate this basic theme and, in particular, the proposition that current concepts of pharmacological efficacy can be effectively used to examine behavioral effects of drugs with abuse or dependence potential in a way that contributes to the discovery ...
In recent years, there has been an intense discovery effort to find more efficacious and better tolerated drugs that target GABA-mediated inhibition. In this review, we focus on the important role of GABA in the modulation of neuronal excitability and seizure activity and control, and we review ...
The activity of GABAAreceptors is modulated by subtype-selective agonists and antagonists belonging to different chemical families such as benzodiazepines or barbiturates and including anesthetic, anxiolytic or antiepileptic drugs. Since primary and transfected cells can often express several subtypes simultaneo...
Other ligands include GABA agonists and antagonists, which are compounds that bind to and cause activation and inactivation of the GABA receptors, respectively. Bicuculline is a GABAA receptor antagonist which competitively inhibits the binding of GABA to its receptors. Studies have shown that the ...
It has been proposed that paradoxical arousal effects of GABA agonists such as zolpidem in minimally conscious state, or benzodiazepines in catatonia may occur when these agents inhibit the globus pallidus, thereby removing tonic inhibition of the intralaminar thalamus (Brown et al., 2010; Giacino ...
First, the effect of GABAergic drugs may vary depending on the precise location of drug infusion. As discussed above, post-training BZs may be more effective at disrupting retention if administered centrally as opposed to systemtically. In addition, GABAA receptor agonists may actually facilitate ...
Here, we will present some examples of medications that work on the GABA system and represent promising thera- pies for the treatment of alcohol and drugs use disorders, ie, baclofen, gabapentin, and topiramate. It should also be noted that these medications are not direct dopaminergic drugs ...
(30 µM, Sigma, Denmark) and baclofen (10 µM, Sigma, Denmark) were used as agonists of the GABAAand GABABreceptors, respectively. Stock solutions were stored in appropriate aliquots at -20oC prior and diluted in ACSF to final concentrations before use, and all drugs were applied via ...
Benzodiazepine agonists represent the currently most useful group of agents in the general class of depressant drugs, which also includes barbiturates, that show anticonvulsant, anxiolytic and sedative–hypnotic activity (see Chs. 40 and 57). Well-known examples include diazepam and chlordiazepoxide, ...
diversity of GABAARs, the native isoforms have to be identified by their localization in the brain and by their pharmacology. In heterologous expression systems, channels require the presence of α, β, and γ subunits in order to mimic the full repertoire of native receptor responses to drugs,...