RgIA4

RgIA4 is an engineered α-conotoxin peptide derived from the marine cone snail Conus regius that acts as a highly potent and selective antagonist of α9α10 nicotinic acetylcholine receptors (nAChRs), with low-nanomolar affinity at both human and rodent α9α10 subtypes.[1][3][5][9] By selectively blocking α9-containing nAChRs, RgIA4 produces robust and long-lasting analgesia in rodent models of chemotherapy-induced neuropathic pain (particularly oxaliplatin-induced cold allodynia and mechanical hypersensitivity) and nerve injury, with effects persisting weeks beyond dosing and evidence of disease-modifying neuroprotective and anti-inflammatory actions in peripheral nerves and immune cells.[1][3][5] It shows minimal activity at other pain-relevant targets, including GABAB and opioid receptors, and its protective effect against acute oxaliplatin-induced cold allodynia requires both the α9 nAChR subunit (chrna9) and CD3-positive T cells, indicating a peripheral, immune–modulated mechanism.[1][2][3] RgIA4 remains a preclinical investigational peptide analgesic and tool compound for probing α9α10 nAChR biology and immune–neuronal interactions in chronic pain.[1][3][5][9]

Other names

RgIA4 conotoxin analogRgIA-4 conotoxin analogRgIA 4 conotoxin analogRgIA4 α-conotoxin analogRgIA4 peptideRgIA-4 peptideRgIA 4 peptide