Allosteric modulation of GABAA receptors via multiple drug-binding sites

W Sieghart - Advances in pharmacology, 2015 - Elsevier
GABA A receptors are ligand-gated ion channels composed of five subunits that can be
opened by GABA and be modulated by multiple pharmacologically and clinically important …

GABA receptors: pharmacological potential and pitfalls

M Jazvinscak Jembrek, J Vlainic - Current pharmaceutical …, 2015 - ingentaconnect.com
Gamma-amino butyric acid (GABA), the major inhibitory neurotransmitter in the mammalian
central nervous system, plays a key role in the regulation of neuronal transmission …

A propofol binding site on mammalian GABAA receptors identified by photolabeling

GMS Yip, ZW Chen, CJ Edge, EH Smith… - Nature chemical …, 2013 - nature.com
Propofol is the most important intravenous general anesthetic in current clinical use. It acts
by potentiating GABAA (γ-aminobutyric acid type A) receptors, but where it binds to this …

Multiple Propofol-binding Sites in a γ-Aminobutyric Acid Type A Receptor (GABAAR) Identified Using a Photoreactive Propofol Analog*♦

SS Jayakar, X Zhou, DC Chiara, Z Dostalova… - Journal of Biological …, 2014 - ASBMB
Propofol acts as a positive allosteric modulator of γ-aminobutyric acid type A receptors
(GABA A Rs), an interaction necessary for its anesthetic potency in vivo as a general …

Glycine receptors and glycine transporters: targets for novel analgesics?

HU Zeilhofer, MA Acuña, J Gingras… - Cellular and Molecular …, 2018 - Springer
Glycinergic neurotransmission has long been known for its role in spinal motor control.
During the last two decades, additional functions have become increasingly recognized …

Structural Studies of GABAA Receptor Binding Sites: Which Experimental Structure Tells us What?

R Puthenkalam, M Hieckel, X Simeone… - Frontiers in molecular …, 2016 - frontiersin.org
Atomic resolution structures of cys-loop receptors, including one of a γ-aminobutyric acid
type A receptor (GABAA receptor) subtype, allow amazing insights into the structural …

Glycine receptors in spinal nociceptive control—an update

HU Zeilhofer, K Werynska, J Gingras, GE Yévenes - Biomolecules, 2021 - mdpi.com
Diminished inhibitory control of spinal nociception is one of the major culprits of chronic pain
states. Restoring proper synaptic inhibition is a well-established rational therapeutic …

The effects of general anesthetics on synaptic transmission

X Hao, M Ou, D Zhang, W Zhao, Y Yang… - Current …, 2020 - ingentaconnect.com
General anesthetics are a class of drugs that target the central nervous system and are
widely used for various medical procedures. General anesthetics produce many behavioral …

Schisandrin B, a dual positive allosteric modulator of GABAA and glycine receptors, alleviates seizures in multiple mouse models

J Wu, M Zhao, Y Jin, M Li, K Yu, H Yu - Acta Pharmacologica Sinica, 2024 - nature.com
Epilepsy is a prevalent and severe neurological disorder and approximately 30% of patients
are resistant to existing medications. It is of utmost importance to develop alternative …

Multisite binding of a general anesthetic to the prokaryotic pentameric Erwinia chrysanthemi ligand-gated ion channel (ELIC)

R Spurny, B Billen, RJ Howard, M Brams… - Journal of Biological …, 2013 - ASBMB
Pentameric ligand-gated ion channels (pLGICs), such as nicotinic acetylcholine, glycine, γ-
aminobutyric acid GABA A/C receptors, and the Gloeobacter violaceus ligand-gated ion …