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GABA A receptors as targets for anaesthetics and analgesics and promising candidates to help treat coronavirus infections: A mini-review.

Yujia LuoThomas Balle
Published in: Basic & clinical pharmacology & toxicology (2022)
GABA is a major inhibitory neurotransmitter that regulates the balance between excitatory and inhibitory circuits in the human nervous system. The GABA receptors are divided into three main subtypes, GABA A , GABA B , and GABA C (also termed GABA A rho) receptors. GABA A receptors are pentameric ligand-gated ion channels widely expressed throughout the central and peripheral nervous system. The activation of GABA A receptors results in opening of an anion-selective channel that mainly gates chloride ions and allows them to flow into the neuron, causing hyperpolarization of the cell membrane that dampens neural excitability. This makes GABA A receptors critical anaesthetic and analgesic targets for existing as well as for the development of novel drugs. In this review, we first summarize the biochemical properties of GABA A receptors and the clinical anaesthetics and analgesics targeting the receptors. In a forward-looking section, we summarize the emerging role of GABAergic signalling in treatment of COVID-19 related infections. Finally, we discuss the opportunities arising from targeting specific and unique subunit interfaces for the development of novel anaesthetics and analgesics leading to more efficient therapies.
Keyphrases
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