For a long time Asian scorpion Buthus martensi Karsch (BmK) has been used in Chinese traditional medicine to cure many diseases of nervous system. Here we report the purification and characterization of a pharmacologically active neurotoxin from the scorpion BmK. This toxin had little toxicity in mice and insects but was found to have an anti-epilepsy effect in rats, and is thus named as BmK antiepilepsy peptide (BmK AEP). Its amino-acid sequence was determined by lysylendopeptidase digestion, Edman degradation and mass spectrographic analysis. Based on the determined sequence, the gene coding for this peptide was also cloned and sequenced by the 3 H and 5 H RACE methods. It encodes a precursor of 85 amino-acid residues including a signal peptide of 21 residues, a mature peptide of 61 residues and three additional residues Gly-Lys-Lys at the C-terminus. The additional Gly sometimes followed by one or two basic residues is prerequisite for the amidation of its C-terminus. C-terminal amidation was also verified by the molecular-mass determination of BmK AEP. This anti-epilepsy peptide toxin shares homology with other depressant insect toxins. The remarkable difference between them was mainly focused at residues 6, 7 and 39; these residues might relate to the unique action of BmK AEP.Keywords: amidation; epilepsy; RACE; scorpion neurotoxin; sequence.Scorpion venom is a rich source of polypeptide neurotoxins that affect ion channels specifically; they can be classified into two groups according to their molecular sizes, namely long-chain and short-chain neurotoxins. Among the longchain neurotoxins, some are only toxic to mammals [1,2] and others are insect-specific neurotoxins [3±5]. Thus, they are called mammalian-specific and insect-specific neurotoxins, respectively. According to the effect on housefly larvae, insect-specific neurotoxins can be further divided into two groups. The depressant toxins induce a slow progressive flaccid paralysis preceded by a short transient phase of contraction [5±7], while the excitatory toxins induce an immediate reversible fast contraction paralysis [5,8].The neurotoxins from the scorpion Buthus martensi Karsch (BmK), a species widely distributed in China, have been studied thoroughly. Up to now, several mammalianspecific neurotoxins, BmK M1, M4, M8 For a long time, the whole body or tail of the scorpion BmK has been used as a Chinese traditional medicine to cure some neural diseases. Therefore, it is worth searching for some pharmacologically effective components from this BmK venom. For example, an excitatory insect neurotoxin with an analgesic effect on mice was purified and characterized [8]. In the late 1980s, a peptide with an anti-epilepsy effect was found from the same venom, named as BmK AEP, and its partial N-terminal sequence was also determined [22]. This peptide had remarkable inhibitory effect on coriaria lactone-induced epilepsy in rats but little toxicity in mice. In addition, BmK AEP had hardly any effect on heart rate, electroencephalogram and breathing rate, an...