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Beschreibung

Blocks neuromuscular transmission by irreversible binding to motor end-plate acetylcholine receptor (Kd = 1 pM to 1 nM) but does not depress acetylcholine release from motor nerve endings. Blocks nicotine-induced increase of intracellular Ca2+ in PC12 cells (IC50 = 310 nM), and prevents opening of nicotinic receptor-associated ion channels. Reconstitution experiments in Xenopus oocytes have shown the effects of alpha-bungarotoxin on neuronal nAChR to be highly specific for the alpha7-subtype (IC50 = 1.6 nM), but not for the alpha3beta4-subtype (IC50 >3 µ,M)., A polypeptide composed of 74 amino acids containing 5 disulfide bridges. Blocks neuromuscular transmission by irreversible binding to the motor end-plate acetylcholine receptor (Kd = 1 nM to 1 pM) but does not depress acetylcholine release from motor nerve endings. Blocks nicotine-induced augmentation in intracellular Ca2+ in PC12 cells (IC50 = 310 nM). Prevents opening of nicotinic receptor-associated ion channels. Reconstitution experiments in Xenopus oocytes have shown the effects of alpha-Bungarotoxin on neuronal nAChR to be highly specific for the alpha7-subtype (IC50 = 1.6 nM), but not for the alpha3beta4-subtype (IC50 >3 µ,M).