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Title: Point-mutations related to the loss of batrachotoxin binding abolish the grayanotoxin effect in Na(+) channel isoforms. Author: Ishii H, Kinoshita E, Kimura T, Yakehiro M, Yamaoka K, Imoto K, Mori Y, Seyama I. Journal: Jpn J Physiol; 1999 Oct; 49(5):457-61. PubMed ID: 10603430. Abstract: The effect of grayanotoxin (GTX) on site-specific mutants of the alpha-subunit of rat skeletal muscle Na(+) channels (micro1) (micro1-I433K, micro1-N434K and micro1-L437K), which are resistant to batrachotoxin (BTX) (Wang and Wang (1998) Proc Natl Acad Sci USA, 95, 2653-2658) was studied using a whole-cell patch-clamp method. The GTX modification of the Na(+) channels was detected as a characteristic-sustained Na(+) current flow with repetitive pulses. We also studied the GTX action on mutants of the alpha-subunit of rat heart Na(+) channels (RH1) (RH1-V406K and RH1-L410K) which match with micro1-I433 and micro1-L437. All the mutants lost their sensitivity to GTX. This finding indicates that GTX may share a binding site with BTX in transmembrane segment I-S6 of two different Na(+) channel isoforms, micro1 and RH1.[Abstract] [Full Text] [Related] [New Search]