Enhancement of Ganglionic Muscarinic Activity by Gallamine

Gardier, Robert W.; Ganansia, M. F.; Delaunois, A. L.; Hamelberg, William

doi:10.1097/00000542-197405000-00016

Cited by 13 publications

(3 citation statements)

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“…Gallamine has been shown to be an antagonist for muscarinic receptors on noradrenergic nerves to the heart (Libet & Tosaka, 1970), on dopaminergic interneurones (Gardier et al, 1978) and on the soma of ganglion cells (Gardier et al, 1974;Ashe & Yarosh, 1984) in the sympathetic ganglia. All of these receptors have an inhibitory function.…”

Section: Discussionmentioning

confidence: 99%

“…Inhibitory muscarinic receptors have been demonstrated in autonomic nerves innervating the intestine (Dzieniszewski & Kilbinger, 1978), blood vessels (Shepherd et al, 1978), heart (Loffelholz & Muscholl, 1970), bladder (Gallagher et al, 1982), and nictitating membrane (Gardier et al, 1974). Similar neuronal receptors have recently been reported to attenuate parasympathetic nerve activity to the guinea-pig lung (Fryer & Maclagan, 1984).…”

Section: Introductionmentioning

confidence: 91%

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Neuronal muscarinic receptors attenuate vagally‐induced contraction of feline bronchial smooth muscle

Blaber

Fryer

Maclagan

1985

British J Pharmacology

122

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1In anaesthetized cats, stimulation of the vagus nerves produced bradycardia and a bronchoconstriction which was measured as an increase in lung resistance (RL) and a fall in dynamic lung compliance (Cdyn); these effects were abolished by atropine.2 Gallamine potentiated vagally-mediated changes in RL and Cdyn at doses that blocked muscarinic receptors in the heart and inhibited neuromuscular transmission. (+ )-Tubocurarine and suxamethonium did not affect the response of the lung or the heart to vagal stimulation. 3 Bronchoconstriction induced by intravenous acetylcholine was not potentiated by gallamine, indicating that postsynaptic muscarinic receptors in the lung and changes in muscle tone were not involved. 4 Potentiation of vagally-induced bronchoconstriction appears to be due to blockade of inhibitory muscarinic receptors located in the pulmonary parasympathetic nerves innervating both central and peripheral airways. 5 Pilocarpine was an agonist for these neuronal receptors as it inhibited vagally-induced bronchoconstriction at low doses (lO ng to 1 pg kg-).6 The results demonstrate that gallamine is an antagonist and pilocarpine an agonist at neuronal muscarinic receptors which attenuate parasympathetic nerve activity in feline lung.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 91%

Neuronal muscarinic receptors attenuate vagally‐induced contraction of feline bronchial smooth muscle

Blaber

Fryer

Maclagan

1985

British J Pharmacology

122

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“…There is, at present, no antagonist sufficiently selective to block the neuronal receptors without an action on the postjunctional M3 receptors. However, gallamine and pilocarpine have been shown to act as an antagonist and an agonist respectively, for the prejunctional receptors on pulmonary cholinergic nerves, at doses which are several fold lower than those needed to affect postjunctional muscarinic receptors on airway smooth muscle (Gardier et al, 1974;1978;Fryer & Maclagan, 1984;Faulkner et al, 1986).…”

Section: Effect Ofa Muscarinic Agonistmentioning

confidence: 99%

Evidence for prejunctional M₂ muscarinic receptors in pulmonary cholinergic nerves in the rat

Aas

Maclagan

1990

British J Pharmacology

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1 The effects of muscarinic antagonists considered to be selective for M1 receptors (pirenzepine) and for M2 receptors (gallamine and methoctramine) were used to investigate the existence of prejunctional muscarinic receptors on cholinergic nerves in the rat lung. The tracheal tube preparation was used in vitro, and contraction of the trachealis muscle was induced by electrical field stimulation (EFS) and by application of an exogenous muscarinic agonist (pilocarpine), and measured as an increase in intraluminal pressure in the tube. 2 The muscarinic antagonists, gallamine and methoctramine, enhanced the contractions induced by nerve stimulation, while contractions elicited by exogenous application of pilocarpine were inhibited by the antagonists. 3 In contrast, pirenzepine blocked contractions induced by both EFS and pilocarpine in a dosedependent manner (EC50 O.1 pM) due to blockade of the postjunctional muscarinic receptors on airway smooth muscle. Potentiation of the response to EFS was never seen with this antagonist. 4 The muscarinic agonist, pilocarpine, caused a slow maintained increase in tone of the tracheal tube and at the same time reduced the contractions induced by EFS. This inhibitory effect was blocked by gallamine and methoctramine. 5 The results suggest that prejunctional inhibitory muscarinic receptors may be localised on the parasympathetic cholinergic nerve terminals innervating tracheal smooth muscle in the rat. This confirms previous findings obtained by measuring transmitter release in this species. The present results suggest that these receptors are of the M2 subtype. Blockade of these autoreceptors with gallamine or methoctramine would increase the output of acetylcholine (ACh) and thereby enhance the nerve-induced contraction of tracheal smooth muscle.

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Antimuscarinic and Ganglion-Blocking Activity of Neuromuscular Blocking Agents

Харкевич¹,

Shorr²

1986

New Neuromuscular Blocking Agents

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Enhancement of Ganglionic Muscarinic Activity by Gallamine

Cited by 13 publications

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Neuronal muscarinic receptors attenuate vagally‐induced contraction of feline bronchial smooth muscle

Neuronal muscarinic receptors attenuate vagally‐induced contraction of feline bronchial smooth muscle

Evidence for prejunctional M₂ muscarinic receptors in pulmonary cholinergic nerves in the rat

Antimuscarinic and Ganglion-Blocking Activity of Neuromuscular Blocking Agents

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Enhancement of Ganglionic Muscarinic Activity by Gallamine

Cited by 13 publications

References 0 publications

Neuronal muscarinic receptors attenuate vagally‐induced contraction of feline bronchial smooth muscle

Neuronal muscarinic receptors attenuate vagally‐induced contraction of feline bronchial smooth muscle

Evidence for prejunctional M2 muscarinic receptors in pulmonary cholinergic nerves in the rat

Antimuscarinic and Ganglion-Blocking Activity of Neuromuscular Blocking Agents

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Evidence for prejunctional M₂ muscarinic receptors in pulmonary cholinergic nerves in the rat