The mechanism of action of two hemicholiniums at the neuromuscular junction

M. Orsetti; M. C. Cassone

The mechanism of action of two hemicholiniums at the neuromuscular junction

M. Orsetti
, M. C. Cassone

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

Abstract

The activity of two hemicholiniums on the response of the frog rectus abdominis muscle to the acetylcholine (Ach) has been evaluated. These drugs modify the Ach effects by different mechanisms of action. Hemicholinium-3 has a weak anticholinesterase activity and curare-like action. On the contrary hemicholinium-15 acts as a noncompetitive sensitizer and potentiates the response to the muscle to the Ach. It is hypothesized that hemicholinium-15 interacts with a site on the nicotinic receptor which is different from the binding site for Ach. Moreover the interaction of the drug with this site increases the affinity between the Ach and the nicotinic receptor.

Original language	English
Pages (from-to)	134-135
Number of pages	2
Journal	IRCS Medical Science
Volume	11
Issue number	2
Publication status	Published - 1983
Externally published	Yes

Cite this

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abstract = "The activity of two hemicholiniums on the response of the frog rectus abdominis muscle to the acetylcholine (Ach) has been evaluated. These drugs modify the Ach effects by different mechanisms of action. Hemicholinium-3 has a weak anticholinesterase activity and curare-like action. On the contrary hemicholinium-15 acts as a noncompetitive sensitizer and potentiates the response to the muscle to the Ach. It is hypothesized that hemicholinium-15 interacts with a site on the nicotinic receptor which is different from the binding site for Ach. Moreover the interaction of the drug with this site increases the affinity between the Ach and the nicotinic receptor.",

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AU - Orsetti, M.

AU - Cassone, M. C.

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N2 - The activity of two hemicholiniums on the response of the frog rectus abdominis muscle to the acetylcholine (Ach) has been evaluated. These drugs modify the Ach effects by different mechanisms of action. Hemicholinium-3 has a weak anticholinesterase activity and curare-like action. On the contrary hemicholinium-15 acts as a noncompetitive sensitizer and potentiates the response to the muscle to the Ach. It is hypothesized that hemicholinium-15 interacts with a site on the nicotinic receptor which is different from the binding site for Ach. Moreover the interaction of the drug with this site increases the affinity between the Ach and the nicotinic receptor.

AB - The activity of two hemicholiniums on the response of the frog rectus abdominis muscle to the acetylcholine (Ach) has been evaluated. These drugs modify the Ach effects by different mechanisms of action. Hemicholinium-3 has a weak anticholinesterase activity and curare-like action. On the contrary hemicholinium-15 acts as a noncompetitive sensitizer and potentiates the response to the muscle to the Ach. It is hypothesized that hemicholinium-15 interacts with a site on the nicotinic receptor which is different from the binding site for Ach. Moreover the interaction of the drug with this site increases the affinity between the Ach and the nicotinic receptor.

UR - https://www.scopus.com/pages/publications/0020677301

M3 - Article

SN - 0305-6651

VL - 11

SP - 134

EP - 135

JO - IRCS Medical Science

JF - IRCS Medical Science

IS - 2

ER -

The mechanism of action of two hemicholiniums at the neuromuscular junction

Abstract

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