Abstract:Abstract: Conotoxins (CTxs) are a group of active peptides from Conus, the tropical marine mollusc. These peptides, with low relative molecular mass, target various ion channels and receptors in animals, and have great potential to be developed into novel drugs. Alpha-conotoxins (α-CTxs) are the earliest known and most important members that specifically act on the nicotinic acetylcholine receptors (nAChRs). They belong to the A-superfamily conotoxins and are selective blockers for muscle or nerve type nAChRs. The nAChRs are closely related with many central nervous system disorders, such as pain, addiction and cancer etc. Recently, other members from other superfamilies are also found to block nAChRs, such as αA-, αB-, αO-, αC-, αD-, and αS-superfamily conotoxins, and they are named α*-CTxs. Here, the progress of structure and function characteristics of α*-CTxs and the receptors, as well as their interactions, were reviewed, which would provide reference for relative research.