Glycine receptor antagonist

A glycine receptor antagonist is a substance that blocks the activity of glycine receptors, which are involved in the modulation of neuronal excitability by inhibitory neurons. Examples of glycine receptor antagonists include strychnine, which can block reciprocal inhibition during locomotion, and certain substances found in ASW that can potentiate NMDA receptor response in the hippocampus.From: Dictionary of Biological Psychology [2003], Sleep Disorders [2019], Potential clinical applications of Ashwagandha (Withania somnifera) in medicine and neuropsychiatry [2022]

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Published in Philip Winn, Dictionary of Biological Psychology, 2003

Philip Winn

The inhibition that occurs between motor bursts (called mid-cycle or RECIPROCAL INHIBITION) is coincident with activity in antagonistic motor neurons. The inhibition hyperpolarizes the membrane potential of motor neurons and reduces their input resistance to prevent action potentials. During reciprocal inhibition, chloride ion channels open to allow the influx of negatively charged chloride ions into motor neurons. The channels are associated with membrane bound receptors for the inhibitory amino acid GLYCINE and they are opened when spinal inhibitory INTERNEURONS release glycine onto motor neurons. Reciprocal inhibition during locomotion can be blocked by the glycine receptor antagonist, strychnine. The mid-cycle inhibition helps to ensure that antagonists are active in alternation.

An update on NMDA antagonists in depression

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Published in Expert Review of Neurotherapeutics, 2019

Bartłomiej Pochwat, Gabriel Nowak, Bernadeta Szewczyk

4-Cl-KYN (AV-101) is a potent and selective glycine receptor antagonist [128] for which antidepressant-like activity was demonstrated in animal studies [17]. Currently AV-101 is under evaluation in a phase 2 randomized, controlled clinical trials (NCT02484456).

Glycine receptor antagonist

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An update on NMDA antagonists in depression