Target intelligence / Profile preview

Glycine Receptor Subunit Alpha-1 (GlyR α1)

Target
GlyR α1
Molecular classification
Ligand-gated ion channel, Ion channel, Receptor
01

Overview

Glycine receptor subunit alpha-1 (GlyR α1) is a protein that forms part of the glycine receptor, a pentameric ligand-gated chloride channel that mediates fast inhibitory neurotransmission in the central nervous system. Activation by glycine leads to chloride influx, hyperpolarization, and reduced neuronal excitability. Mutations in GLRA1, the gene encoding GlyR α1, can cause hyperekplexia (startle disease). The receptor is also implicated in stiff-person syndrome spectrum disorders. Pharmacological modulation of the receptor affects motor control, respiratory rhythm, and pain signaling.

Other names
Glycine receptor, alpha 1Glycine receptor strychnine-binding subunitSTHE
02

Mechanism of action

Glycine and other agonists bind to the extracellular domain of the GlyR α1 subunit, leading to the opening of the chloride channel. This influx of chloride ions hyperpolarizes the neuron, reducing its excitability and mediating inhibitory neurotransmission. Strychnine blocks glycine binding, acting as an antagonist. Ethanol enhances channel opening, acting as a positive allosteric modulator.

03

Biological functions

Inhibitory neurotransmissionMotor coordinationRegulation of respiratory rhythmPain signaling/nociception
04

Disease associations

Hyperekplexia (startle disease)Stiff-person syndrome spectrum disorders (e.g., PERM)
05

Safety considerations

Strychnine is highly toxic and can cause convulsions and respiratory failure.Dysfunction or autoimmunity can lead to neurological disorders.
06

Interacting drugs

Glycine

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