apamin

Apamin is an 18-amino acid globular peptide neurotoxin derived from bee venom (*Apis mellifera*). It is a highly selective blocker of small-conductance Ca2+-activated K+ (SK) channels, specifically the SK1, SK2, and SK3 subtypes, with the highest potency observed against SK2 (IC50 ~70 pM). Notably, apamin is the smallest known neurotoxin polypeptide and is unique for its ability to cross the blood-brain barrier. While it is not currently being developed as a therapeutic agent, apamin is widely utilized as a pharmacological tool in neuroscience research to study neuronal excitability and the role of SK channels in the afterhyperpolarization phase of action potentials. Furthermore, researchers are exploring modified versions of apamin as potential drug delivery vehicles to transport therapeutic agents across the blood-brain barrier for the treatment of spinal cord injuries and other central nervous system disorders.

Other names

apamine