Overview
It is recommended to prepare fresh solutions in working buffers before use, or aliquot stock solutions reconstituted in distilled water and keep at -20°C. Upon use, dilute the stock solution in the desired working buffer. Prevent repeated thawing and freezing cycles. Centrifuge all product preparations before use (10,000 g for 5 min).
α-conotoxin GeXIVA (αO-conotoxin GeXIVA or GeXIVA) is a 28 amino acid peptidyl toxin, which was discovered from a transcriptome analysis of the South China Sea mollusk, Conus generalis1. GeXIVA belongs to the O1-gene superfamily and is a potent and selective antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) subtype1. The toxin-mediated blockade of α9α10 nAChRs is voltage-dependent, suggesting that the toxin binding site might be allosterically coupled to a voltage-sensitive domain of the nAChR1,2. GeXIVA exhibits analgesic activity in animal models of pain without the development of tolerance1-4.
nAChRs are involved in a wide range of physiological functions in the central and peripheral nervous systems. Alterations in nAChR expression and/or function are associated with a number of pathophysiological conditions including pain, addiction, epilepsy, autism, schizophrenia, Alzheimer's and Parkinson's diseases, as well as many types of cancers2,6. The nAChRs are formed from the assembly of five homologous subunits and neuronal nAChRs are assembled from a combination of α- and β-subunits. They share a common basic structure, but their pharmacological and functional properties arise from the wide range of different subunit combinations which generate distinctive subtypes6. The α9α10 nAChR subtype is a potential target for treating chronic pain, wound healing, the pathophysiology of the auditory system, and various cancers4-7. GeXIVA potently alleviated neuropathic pain in several rat models1-4 and also exhibited an antitumor effect5,8.