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Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.
TLDR
The synthesis and pharmacological properties of imidazobenzodiazepines with both high affinity and selectivity for α5-containing GABAA receptors are described and these compounds behaved as GABA negative ligands in r...
Benzodiazepine receptor-mediated experimental "anxiety" in primates.
TLDR
The results suggest that the benzodiazepine receptor is involved in both the affective and physiological manifestations of anxiety, and that the administration of beta-carboxylic acid ethyl ester to monkeys may provide a reliable and reproducible animal model of human anxiety.
A Novel α5GABAAR-Positive Allosteric Modulator Reverses Hyperactivation of the Dopamine System in the MAM Model of Schizophrenia
TLDR
Treatment with the α5GABAAR PAM reduced the number of spontaneously active DA neurons in the VTA of MAM animals to levels observed in SAL rats, both when administered systemically and when directly infused into the ventral HPC.
Regulating anxiety with extrasynaptic inhibition
TLDR
The findings reveal that the neuronal circuits that mediate fear and anxiety overlap at the level of defined subpopulations of central amygdala neurons and demonstrate that persistent changes in the excitability of a single cell type can orchestrate complex behavioral changes.
Contribution of α1GABAA and α5GABAA Receptor Subtypes to the Discriminative Stimulus Effects of Ethanol in Squirrel Monkeys
Ethanol's ability to enhance GABA neurotransmission via GABAA receptors has been implicated as an important mechanism underlying its discriminative stimulus (DS) effects in animals and subjective
eEF2K/eEF2 Pathway Controls the Excitation/Inhibition Balance and Susceptibility to Epileptic Seizures
TLDR
It is shown that eEF2K activity negatively regulates GABAergic synaptic transmission and is identified as a potential novel target for antiepileptic drugs, since pharmacological and genetic inhibition of e EF2K can revert the epileptic phenotype in a mouse model of human epilepsy.
Development of a comprehensive pharmacophore model for the benzodiazepine receptor.
TLDR
A unified pharmacophore model of the benzodiazepine receptor (BzR) has been developed using the techniques of chemical synthesis, radioligand binding, and receptor mapping and qualitatively accounts for the relative affinities, efficacies, and functional effects displayed by various ligands at the BzR.
Pharmacophore/Receptor Models for GABAA/BzR Subtypes (α1β3γ2, α5β3γ2, and α6β3γ2) via a Comprehensive Ligand-Mapping Approach
TLDR
Examining the affinities of 151 BzR ligands at five distinct recombinant GABAA/BzR receptor subtypes from at least nine different structural families indicated that region L2 for the α5-containing subtype appeared to be larger in size than the analogous region of the other receptor subtype.
An updated unified pharmacophore model of the benzodiazepine binding site on gamma-aminobutyric acid(a) receptors: correlation with comparative models.
A successful unified pharmacophore/receptor model which has guided the synthesis of subtype selective compounds is reviewed in light of recent developments both in ligand synthesis and structural
The Reinforcing Properties of Alcohol are Mediated by GABAA1 Receptors in the Ventral Pallidum
TLDR
The present study indicates that βCCt is capable of antagonizing the reinforcing and the sedative properties of alcohol and may represent a prototype of a pharmacotherapeutic agent to effectively reduce alcohol drinking behavior in human alcoholics.
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