The Benzodiazepine Binding Sites of GABA Receptors.

Sigel, Erwin; Ernst, Margot (2018). The Benzodiazepine Binding Sites of GABA Receptors. Trends in Pharmacological Sciences, 39(7), pp. 659-671. Elsevier 10.1016/j.tips.2018.03.006

[img] Text
The Benzo.pdf - Published Version
Restricted to registered users only
Available under License Publisher holds Copyright.

Download (2MB)

Everyday activity is based on a subtle equilibrium of excitatory and inhibitory neuronal systems. The most prominent players in neuronal inhibition are synaptic and extrasynaptic GABA receptors. Benzodiazepines are popular drugs that act as positive allosteric modulators of a subset of these receptors. Benzodiazepines have sedative, hypnotic, muscle-relaxant, and anticonvulsive effects, and are of outstandingly low overdose risk. The discovery of a large number of subtypes of GABA receptors has raised hopes for a clear separation of this spectrum of actions. We discuss here how far this separation has been achieved, and outline recent progress towards the discovery of novel ligands for canonical and non-canonical binding sites.

Item Type:

Journal Article (Review Article)

Division/Institute:

04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Biochemistry and Molecular Medicine

UniBE Contributor:

Sigel, Erwin

Subjects:

500 Science > 570 Life sciences; biology
600 Technology > 610 Medicine & health

ISSN:

1873-3735

Publisher:

Elsevier

Language:

English

Submitter:

Barbara Franziska Järmann-Bangerter

Date Deposited:

07 Mar 2019 09:43

Last Modified:

05 Dec 2022 15:25

Publisher DOI:

10.1016/j.tips.2018.03.006

PubMed ID:

29716746

Uncontrolled Keywords:

GABA GABA(A) receptor benzodiazepine receptor subtypes

BORIS DOI:

10.7892/boris.125036

URI:

https://boris.unibe.ch/id/eprint/125036

Actions (login required)

Edit item Edit item
Provide Feedback