Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes

U Rudolph, F Knoflach - Nature reviews Drug discovery, 2011 - nature.com
GABAA (γ-aminobutyric acid, type A) receptors are a family of ligand-gated ion channels that
are essential for the regulation of central nervous system function. Benzodiazepines—which …

GABAkines–Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAA receptors

A Lippa, MM Poe, JL Smith, X Jin, X Ping… - Pharmacology & …, 2022 - Elsevier
Positive allosteric modulators of γ-aminobutyric acid-A (GABA A) receptors or GABAkines
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …

International Union of Basic and Clinical Pharmacology. CVI: GABAA receptor subtype-and function-selective ligands: key issues in translation to humans

W Sieghart, MM Savić, EH Ohlstein - Pharmacological reviews, 2018 - Elsevier
GABA A receptors are the major inhibitory transmitter receptors in the brain. They are ligand-
gated chloride channels and the site of action of benzodiazepines, barbiturates, neuroactive …

GABAA receptors: subtypes provide diversity of function and pharmacology

RW Olsen, W Sieghart - Neuropharmacology, 2009 - Elsevier
This mini-review attempts to update experimental evidence on the existence of GABAA
receptor pharmacological subtypes and to produce a list of those native receptors that exist …

Hooked on benzodiazepines: GABAA receptor subtypes and addiction

KR Tan, U Rudolph, C Lüscher - Trends in neurosciences, 2011 - cell.com
Benzodiazepines are widely used clinically to treat anxiety and insomnia. They also induce
muscle relaxation, control epileptic seizures, and can produce amnesia. Moreover …

Ion channels as therapeutic targets: a drug discovery perspective

SK Bagal, AD Brown, PJ Cox, K Omoto… - Journal of medicinal …, 2013 - ACS Publications
Ion channels are membrane proteins expressed in almost all living cells. The sequencing of
the human genome has identified more than 400 putative ion channels, but only a fraction of …

Mechanisms Underlying Tolerance after Long‐Term Benzodiazepine Use: A Future for Subtype‐Selective GABAA Receptor Modulators?

CH Vinkers, B Olivier - Advances in Pharmacological and …, 2012 - Wiley Online Library
Despite decades of basic and clinical research, our understanding of how benzodiazepines
tend to lose their efficacy over time (tolerance) is at least incomplete. In appears that …

GABA neuron alterations, cortical circuit dysfunction and cognitive deficits in schizophrenia

G Gonzalez-Burgos, KN Fish, DA Lewis - Neural plasticity, 2011 - Wiley Online Library
Schizophrenia is a brain disorder associated with cognitive deficits that severely affect the
patients′ capacity for daily functioning. Whereas our understanding of its pathophysiology …

Abuse and dependence liability of benzodiazepine-type drugs: GABAA receptor modulation and beyond

SC Licata, JK Rowlett - Pharmacology Biochemistry and Behavior, 2008 - Elsevier
Over the past several decades, benzodiazepines and the newer non-benzodiazepines have
become the anxiolytic/hypnotics of choice over the more readily abused barbiturates. While …

[引用][C] International Union of Pharmacology. LXX. Subtypes of γ-aminobutyric acidA receptors: classification on the basis of subunit composition, pharmacology, and …

RW Olsen, W Sieghart - Pharmacological reviews, 2008 - ASPET