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- W2006292009 abstract "NIK-247 (9-amino-2,3,5,6,7,8-hexahydro-lH-cyclopenta[b]-quinoline hydrochloride hydrate), an acetylcholinesterase inhibitor, is structurally related to 4-aminopyridine (AP). Its effects on ionic currents were examined in the artificial node of the crayfish axon under voltage-clamp. When applied externally, NIK-247 reversibly suppressed both inward and outward currents. Effects on K currents were further studied in the presence of tetrodotoxin. NIK-247 suppressed the K current dose-dependently, but with an IC50 at of 10-3 M. THA (9-amino-1,2,3,4-tetra-hydroacridine hydrochloride hydrate), a related inhibitor, similarly suppressed the K current with an IC50 of 5 × 10-4 M, in comparison with 3-AP and 4-AP which had IC50’s of 3 × 10-5 M and at 10-5 M, respectively. Furthermore, NIK-247 (and THA) suppressed the K current uniformly for the whole time course, whereas AP the AP’s suppressed mainly the fast activating and inactivating K current with a voltage- and frequency-dependent recovery. Therefore, NIK-247 and THA seem to be neither potent nor very specific as ionic channel blockers. With respect to the K current, however, they clearly differ from the AP’s in their mode of suppression." @default.
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- W2006292009 date "1991-01-01" @default.
- W2006292009 modified "2023-09-23" @default.
- W2006292009 title "NIK-247 Blocks Voltage-Dependent Ionic Currents in Crayfish Axon." @default.
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- W2006292009 doi "https://doi.org/10.1254/jjp.57.545" @default.
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