Competitive inhibition of acetylcholinesterase by bretylium: Possible mechanism for its induction of norepinephrine release

Gabriel Schreiber; Mordechai Sokolovsky

doi:10.1097/00005344-198511000-00008

Competitive inhibition of acetylcholinesterase by bretylium: Possible mechanism for its induction of norepinephrine release

Gabriel Schreiber, Mordechai Sokolovsky

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

2 Scopus citations

Abstract

The antiarrhythmic drug bretylium tosylate competitively inhibits acetylcholinesterase activity. The K_i values for the inhibition of the purified enzyme (from electric eel), and acetylcholinesterase activity of crude rat ventricular and cortical homogenates were 6 × 10^-5, 3 × 10^-5 and 8 × 10^-5M, respectively. These values are close to the concentrations of the drug known to induce norepinephrine release from cardiac adrenergic presynaptic vesicles. It is suggested that inhibition of acetylcholinesterase activity by bretylium induces norepinephrine release through the effect of the accumulated acetylcholine on nicotinic receptors in adrenergic nerve terminals.

Original language	English
Pages (from-to)	1065-1068
Number of pages	4
Journal	Journal of Cardiovascular Pharmacology
Volume	7
Issue number	6
DOIs	https://doi.org/10.1097/00005344-198511000-00008
State	Published - 1 Jan 1985
Externally published	Yes

Keywords

Acetylcholinesterase
Bretylium
Norepinephrine release

ASJC Scopus subject areas

Pharmacology
Cardiology and Cardiovascular Medicine

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10.1097/00005344-198511000-00008

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title = "Competitive inhibition of acetylcholinesterase by bretylium: Possible mechanism for its induction of norepinephrine release",

abstract = "The antiarrhythmic drug bretylium tosylate competitively inhibits acetylcholinesterase activity. The Ki values for the inhibition of the purified enzyme (from electric eel), and acetylcholinesterase activity of crude rat ventricular and cortical homogenates were 6 × 10-5, 3 × 10-5 and 8 × 10-5M, respectively. These values are close to the concentrations of the drug known to induce norepinephrine release from cardiac adrenergic presynaptic vesicles. It is suggested that inhibition of acetylcholinesterase activity by bretylium induces norepinephrine release through the effect of the accumulated acetylcholine on nicotinic receptors in adrenergic nerve terminals.",

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year = "1985",

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T1 - Competitive inhibition of acetylcholinesterase by bretylium

T2 - Possible mechanism for its induction of norepinephrine release

AU - Schreiber, Gabriel

AU - Sokolovsky, Mordechai

PY - 1985/1/1

Y1 - 1985/1/1

N2 - The antiarrhythmic drug bretylium tosylate competitively inhibits acetylcholinesterase activity. The Ki values for the inhibition of the purified enzyme (from electric eel), and acetylcholinesterase activity of crude rat ventricular and cortical homogenates were 6 × 10-5, 3 × 10-5 and 8 × 10-5M, respectively. These values are close to the concentrations of the drug known to induce norepinephrine release from cardiac adrenergic presynaptic vesicles. It is suggested that inhibition of acetylcholinesterase activity by bretylium induces norepinephrine release through the effect of the accumulated acetylcholine on nicotinic receptors in adrenergic nerve terminals.

AB - The antiarrhythmic drug bretylium tosylate competitively inhibits acetylcholinesterase activity. The Ki values for the inhibition of the purified enzyme (from electric eel), and acetylcholinesterase activity of crude rat ventricular and cortical homogenates were 6 × 10-5, 3 × 10-5 and 8 × 10-5M, respectively. These values are close to the concentrations of the drug known to induce norepinephrine release from cardiac adrenergic presynaptic vesicles. It is suggested that inhibition of acetylcholinesterase activity by bretylium induces norepinephrine release through the effect of the accumulated acetylcholine on nicotinic receptors in adrenergic nerve terminals.

KW - Acetylcholinesterase

KW - Bretylium

KW - Norepinephrine release

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Competitive inhibition of acetylcholinesterase by bretylium: Possible mechanism for its induction of norepinephrine release

Abstract

Keywords

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