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Literature DB >> 4451745

On the simultaneous action of two competitive antagonists.

Abstract

1 A hypothesis is outlined predicting the conditions in which the addition of a second competitive antagonist will increase rather than reduce the response to an agonist.2 Experiments were performed with the guinea-pig ileum as the test tissue, hexyltrimethyl ammonium as the agonist, benzilyltropine methiodide as the ;slow' antagonist and pentyltriethyl ammonium as the ;fast' antagonist.3 The results are consistent with the hypothesis, if the affinity constant for hexyltrimethyl ammonium is between 2.7 and 3.7 x 10(4)M(-1), if the dissociation time constant for the slow antagonist is greater than 10 min and if that for the fast antagonist is less than 10 seconds.

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Year: 1974 PMID： 4451745 PMCID： PMC1776755 DOI： 10.1111/j.1476-5381.1974.tb09659.x

Source DB: PubMed Journal: Br J Pharmacol ISSN： 0007-1188 Impact factor: 8.739

11 in total

1. A modification of receptor theory.

Authors: R P STEPHENSON
Journal: Br J Pharmacol Chemother Date: 1956-12

2. The kinetics of action of acetylcholine antagonists in smooth muscle.

Authors: H P Rang
Journal: Proc R Soc Lond B Biol Sci Date: 1966-04-19

3. The rate of equilibration in a competitive n drug system and the auto-inhibitory equations of enzyme kinetics: some properties of simple models for passive sensitization.

Authors: D Colquhoun
Journal: Proc R Soc Lond B Biol Sci Date: 1968-06-11

2. Interaction of competitive antagonists: the anti-curare action of hexamethonium and other antagonists at the skeletal neuromuscular junction.

Authors: J G Blackman; R W Gauldie; R J Milne
Journal: Br J Pharmacol Date: 1975-05 Impact factor: 8.739

9. Potentiation of nerve-induced bladder responses by tetraethylammonium in relation to junctional and extrajunctional muscarinic receptors.

Authors: F G Carpenter
Journal: Br J Pharmacol Date: 1978-11 Impact factor: 8.739

9 in total

On the simultaneous action of two competitive antagonists.

1. A modification of receptor theory.

2. The kinetics of action of acetylcholine antagonists in smooth muscle.

3. The rate of equilibration in a competitive n drug system and the auto-inhibitory equations of enzyme kinetics: some properties of simple models for passive sensitization.

4. Potentiation by an antagonist.

5. On the analysis of pharmacological experiments in terms of an allosteric receptor model.

6. The binding of labelled tetrodotoxin to non-myelinated nerve fibres.

7. Relationships between chemical structure and affinity for acetylcholine receptors.

8. The rate of action of atropine.

9. On the excitability and cooperativity of the electroplax membrane.

10. An anti-curare effect of hexamethonium at the mammalian neuromuscular junction.

1. Dual effect of alpha-adrenoceptor antagonists in rat isolated vas deferens.

2. Interaction of competitive antagonists: the anti-curare action of hexamethonium and other antagonists at the skeletal neuromuscular junction.

3. Enhancement by an antagonist of transmitter release from frog motor nerve terminals.

4. The effect of tubocurarine competition on the kinetics of agonist action on the nicotinic receptor.

5. The kinetics of competitive antagonists on guinea-pig ileum.

6. The interaction between hexamethonium and tubocurarine on the rat neuromuscular junction.

7. Lack of involvement of alpha-adrenoceptors in sympathetic neural vasoconstriction in the hindquarters of the rabbit.

8. The inhibitory effect of gallamine on muscarinic receptors.

9. Potentiation of nerve-induced bladder responses by tetraethylammonium in relation to junctional and extrajunctional muscarinic receptors.