The Cholinergic Receptor

Waser, Peter G.

doi:10.1111/j.2042-7158.1960.tb12714.x

Cited by 60 publications

(20 citation statements)

References 28 publications

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“…The major function of AChE is generally considered to be the hydrolysis of ACh following its production of the postsynaptic potential in order to insure the rapid termination of the localised depolarisation. Very little is known about the nature of an additional component of cholinergic systems, the ACh-receptor (Chagas, 1959;Ehrenpreis, 1960) or cholinoceptive site (Dale, 1954), as was pointed out by Waser (1960) in a previous lecture in this series.…”

Section: Components Of Cholinergic Neurons: Choiine Acetylase (Chac)mentioning

confidence: 99%

A New General Concept of the Neurohumoral Functions of Acetylcholine and Acetylcholinesterase

Koelle

1962

Journal of Pharmacy and Pharmacology

257

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Section: Components Of Cholinergic Neurons: Choiine Acetylase (Chac)mentioning

confidence: 99%

A New General Concept of the Neurohumoral Functions of Acetylcholine and Acetylcholinesterase

Koelle

1962

Journal of Pharmacy and Pharmacology

257

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“…There is evidence for fairly rapid cell penetration and binding of decamethonium in the end-plate of skeletal muscle (Taylor, Creese, Nedergaard & Case, 1965;Waser, 1960) although transmembrane exchange of decamethonium-like compounds may be slow (Creese, Taylor & Tilton, 1963). It was anticipated that uptake of a proportion of the labelled cations diffusing through rat diaphragm in the present experiments might be detected as an apparent increase in tortuosity factor.…”

Section: Diffusion Measurementmentioning

confidence: 99%

Diffusion of labelled substances through isolated rat diaphragm

Brookes

Mackay

1971

British J Pharmacology

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“…Waser (30) has estimated that fewer than 10% of the ACh receptors in the rat diaphragm are activated during transmission. Saturation of receptor responses, which would occur if the number of receptors available during transmission were not large, is not normally observed (14).…”

Section: The Model Kinetic Schemementioning

confidence: 99%

A Kinetic Model for the Action of Xylocaine on Receptors for Acetylcholine

Steinbach

1968

The Journal of General Physiology

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A kinetic scheme postulating the rapid formation of a partially active acetylcholine-receptor-drug complex from Xylocaine (or a derivative) and the active acetylcholine-receptor complex can account for the effects of Xylocaine and its derivatives at the neuromuscular junction. Transmembrane currents generated by an analogue computer programmed according to the scheme can exactly match end plate currents produced by nerve stimulation in the presence of the drugs. The scheme also accounts for the qualitatively different effects of the drugs on the end plate potential and on responses to iontophoretically applied acetylcholine. The analysis presented is consistent with very rapid reactions between acetylcholine and receptors, characterized by rate coefficients in the range 104 to 106 sec-'. It is based on the hypothesis that the activation of receptors by acetylcholine changes the structure of the receptors and thus their affinity for Xylocaine. The analysis does not require pharmacological separability of sodium and potassium conductances during the end plate current.Procaine, Xylocaine, and derivatives of Xylocaine depress and modify the response of the postsynaptic receptors of the neuromuscular junction to acetylcholine (ACh) (22,25). The most striking aspect of the effects of these drugs is the production of a prolonged component of the end plate potential (e.p.p.) that cannot be ascribed to an anticholinesterase action. In this respect, and in many other details, the actions of the drugs differ greatly from that of dtubocurarine (d-TC) and other chemicals that also depress the response of receptors. However, the site of action of Xylocaine and procaine, like that of d-TC, appears to be at the postsynaptic receptors (22,25). This suggests that these drugs modify the kinetics of the receptor response, although they do not produce a response themselves. Thus, an analysis of the effects of Xylocaine and procaine at the neuromuscular junction should offer the opportunity to find out more about the receptors themselves.

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The Cholinergic Receptor

Cited by 60 publications

References 28 publications

A New General Concept of the Neurohumoral Functions of Acetylcholine and Acetylcholinesterase

A New General Concept of the Neurohumoral Functions of Acetylcholine and Acetylcholinesterase

Diffusion of labelled substances through isolated rat diaphragm

A Kinetic Model for the Action of Xylocaine on Receptors for Acetylcholine

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