Target intelligence / Profile preview

Gamma-aminobutyric acid receptor (Artemia salina) (GABA-R)

Target
GABA-R
Molecular classification
Ion channel, Ligand-gated ion channel, Cys-loop receptor family, Receptor
01

Overview

The Gamma-aminobutyric acid receptor (Artemia salina) is a ligand-gated ion channel that plays a fundamental role in the inhibitory neurotransmission of brine shrimp (Source: PubMed, PMID: 11440860). As a member of the Cys-loop receptor superfamily, it functions by conducting chloride ions across the neuronal membrane in response to GABA binding, thereby regulating neuronal excitability and motor behavior (Source: UniProt, P0C0S5). While not a primary therapeutic target for human diseases, these receptors are of high importance in environmental toxicology and the development of agrochemicals, serving as the site of action for several classes of insecticides and antiparasitic drugs like fipronil and ivermectin (Source: PubChem, CID 3352). They are extensively utilized in the Brine Shrimp Lethality Assay (BSLA) as a preliminary screening tool to evaluate the pharmacological potential and toxicity of natural and synthetic compounds (Source: NIH, PMC3131774). Research into these receptors helps in understanding the evolution of neurotransmitter systems and aids in the design of species-selective ligands to reduce ecological risks (Source: Wikipedia, Artemia salina). Mutations in these receptors, particularly in the RDL (Resistance to dieldrin) gene, are a major mechanism of insecticide resistance in various arthropods (Source: PubMed, PMID: 15590657). The study of Artemia GABA receptors provides insights into the comparative pharmacology of invertebrate versus vertebrate nervous systems (Source: Journal of Experimental Biology).

Other names
Artemia GABA receptorGABA-gated chloride channelRDL-like receptorGamma-aminobutyric acid-gated chloride channelArtemia salina GABA receptor
02

Mechanism of action

Agonist binding to the extracellular domain triggers a conformational change that opens a chloride-selective pore, resulting in an influx of chloride ions and subsequent hyperpolarization of the postsynaptic membrane.

03

Biological functions

Inhibitory neurotransmissionSignal transductionMotor coordinationOsmoregulation
04

Disease associations

InfectionPest infestationToxicity
05

Safety considerations

Non-target toxicity in aquatic ecosystemsPotential for cross-reactivity with mammalian GABA-A receptorsEmergence of resistance mutations
06

Interacting drugs

Gamma-aminobutyric acid

7 more in the full profile.

07

Biomarkers

Lethality (LC50)Swimming behaviorHatching rate

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