Tetrahydroaminoacridine blocks voltage-dependent ion channels in hippocampal neurons

Michael A Rogawski

doi:10.1016/0014-2999(87)90670-4

Tetrahydroaminoacridine blocks voltage-dependent ion channels in hippocampal neurons

Michael A Rogawski

Research output: Contribution to journal › Article › peer-review

86 Scopus citations

Abstract

Tetrahydroaminoacridine (THA) is a centrally active anticholinesterase that may produce functional improvement in patients with Alzheimer's disease. Because of its structural similarity to the potassium channel (A-current) blocking drug 4-aminopyridine (4-AP), it has been speculated that some of the therapeutic benefit of THA might result from inhibition of potassium currents. In the present study, THA produced a dose-dependent, reversible block of the A-current in cultured hippocampal neurons (IC₅₀, 30 μM). However, at similar concentrations it also inhibited other voltage-dependent currents.

Original language	English (US)
Pages (from-to)	169-172
Number of pages	4
Journal	European Journal of Pharmacology
Volume	142
Issue number	1
DOIs	https://doi.org/10.1016/0014-2999(87)90670-4
State	Published - Oct 6 1987
Externally published	Yes

Keywords

Alzheimer's disease
Hippocampus
Potassium channel
Tacrine
Tetrahydroaminoacridine
Whole cell patch clamp recording

ASJC Scopus subject areas

Cellular and Molecular Neuroscience
Pharmacology

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10.1016/0014-2999(87)90670-4

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abstract = "Tetrahydroaminoacridine (THA) is a centrally active anticholinesterase that may produce functional improvement in patients with Alzheimer's disease. Because of its structural similarity to the potassium channel (A-current) blocking drug 4-aminopyridine (4-AP), it has been speculated that some of the therapeutic benefit of THA might result from inhibition of potassium currents. In the present study, THA produced a dose-dependent, reversible block of the A-current in cultured hippocampal neurons (IC50, 30 μM). However, at similar concentrations it also inhibited other voltage-dependent currents.",

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AB - Tetrahydroaminoacridine (THA) is a centrally active anticholinesterase that may produce functional improvement in patients with Alzheimer's disease. Because of its structural similarity to the potassium channel (A-current) blocking drug 4-aminopyridine (4-AP), it has been speculated that some of the therapeutic benefit of THA might result from inhibition of potassium currents. In the present study, THA produced a dose-dependent, reversible block of the A-current in cultured hippocampal neurons (IC50, 30 μM). However, at similar concentrations it also inhibited other voltage-dependent currents.

KW - Alzheimer's disease

KW - Hippocampus

KW - Potassium channel

KW - Tacrine

KW - Tetrahydroaminoacridine

KW - Whole cell patch clamp recording

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Tetrahydroaminoacridine blocks voltage-dependent ion channels in hippocampal neurons

Abstract

Keywords

ASJC Scopus subject areas

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