Invertebrate glutamate-gated chloride receptor (GluClR)

Invertebrate glutamate-gated chloride receptors (GluClRs) are pentameric ligand-gated ion channels that mediate inhibitory neurotransmission in protostome invertebrates, including nematodes and arthropods [2, 3]. These receptors belong to the Cys-loop superfamily and are activated by the neurotransmitter glutamate, which triggers the influx of chloride ions, resulting in membrane hyperpolarization and the suppression of neuronal or muscular activity [1, 5]. GluClRs are critical for regulating essential behaviors, including locomotion, feeding, and sensory processing [3, 6]. Since these receptors are not found in vertebrates, they serve as highly selective targets for antiparasitic and insecticidal agents [1, 7]. Macrocyclic lactones, most notably ivermectin, bind to an allosteric site within the transmembrane domain, locking the channel in an open state and causing irreversible paralysis of the target organism [1, 2]. However, the widespread use of these drugs has led to the emergence of resistance, often linked to specific mutations in the receptor subunits, which remains a major challenge in veterinary and human medicine [4, 7].

Other names

Glutamate-gated chloride channelGluClGluClRInhibitory glutamate receptoriGluRH-receptor

Allosteric activation and potentiation of chloride ion conductance, leading to persistent membrane hyperpolarization and flaccid paralysis of the organism.