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Literature DB >> 7470742

The size of the hydroxyl group and its contribution to the affinity of atropine for muscarine-sensitive acetylcholine receptors.

Abstract

1 From measurements of the affinity constants of hydratropyltropine and its methiodide for muscarine-sensitive acetylcholine receptors in the guinea-pig ileum, the increment in log K for the hydroxyl group in atropine is 2.06 and in the methiodide it is 2.16. These effects are slightly bigger than any so far recorded with these receptors. 2 The estimate of the increment in apparent molal volume for the hydroxyl group is 1.1 cm3/mol in atropine and 1.0 cm3/mol in the methobromide. 3 The large effect of the group on affinity may be linked to its small apparent size in water as suggested in the previous paper.

Entities: Chemical Species

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Year: 1980 PMID： 7470742 PMCID： PMC2044390 DOI： 10.1111/j.1476-5381.1980.tb10905.x

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

5 in total

1. Temperature coefficients of affinity constants for the binding of antagonists to muscarinic receptors in the rat cerebral cortex.

Authors: R B Barlow; N J Birdsall; E C Hulme
Journal: Br J Pharmacol Date: 1979-08 Impact factor: 8.739

2. Studies on the stereospecificity of closely related compounds which block postganglionic acetylcholine receptors in the guinea-pig ileum.

Authors: R B Barlow; F M Franks; J D Pearson
Journal: J Med Chem Date: 1973-05 Impact factor: 7.446

3. The ionization of phenolic amines, including apomorphine, dopamine and catecholamines and an assessment of zwitterion constants.

Authors: J Armstrong; R B Barlow
Journal: Br J Pharmacol Date: 1976-08 Impact factor: 8.739

4. The ionization of 5-hydroxytryptamine and related compounds and an appraisal of methods for the estimation of zwitterion constants.

Authors: R B Barlow; K N Burston
Journal: Br J Pharmacol Date: 1980-08 Impact factor: 8.739

5. Temperature coefficients of affinity and entropies of adsorption from enantiomeric pairs of compounds acting at muscarinic receptors in the guinea-pig ileum.

Authors: R B Barlow; K N Burston
Journal: Br J Pharmacol Date: 1979-08 Impact factor: 8.739

5 in total

4. The size of hydroxyl groups in solution and the changes in size associated with the ionization of phenolic, carboxylic and amino groups in phenolic quaternary ammonium salts, nicotine and some amino acids: possible implications for drug-water and drug-receptor interactions.

Authors: R B Barlow
Journal: Br J Pharmacol Date: 1980 Impact factor: 8.739

5. Affinities of the protonated and non-protonated forms of hyoscine and hyoscine N-oxide for muscarinic receptors of the guinea-pig ileum and a comparison of their size in solution with that of atropine.

Authors: R B Barlow; E A Winter
Journal: Br J Pharmacol Date: 1981-04 Impact factor: 8.739

5 in total

The size of the hydroxyl group and its contribution to the affinity of atropine for muscarine-sensitive acetylcholine receptors.

1. Temperature coefficients of affinity constants for the binding of antagonists to muscarinic receptors in the rat cerebral cortex.

2. Studies on the stereospecificity of closely related compounds which block postganglionic acetylcholine receptors in the guinea-pig ileum.

3. The ionization of phenolic amines, including apomorphine, dopamine and catecholamines and an assessment of zwitterion constants.

4. The ionization of 5-hydroxytryptamine and related compounds and an appraisal of methods for the estimation of zwitterion constants.

5. Temperature coefficients of affinity and entropies of adsorption from enantiomeric pairs of compounds acting at muscarinic receptors in the guinea-pig ileum.

1. Modelling of the binding site of the human m1 muscarinic receptor: experimental validation and refinement.

2. The molal volumes of atropine and hyoscine in relation to their respective potencies.

3. Enthalpy-entropy relationship in drug-cholinoceptor interaction: a new approach.

4. The size of hydroxyl groups in solution and the changes in size associated with the ionization of phenolic, carboxylic and amino groups in phenolic quaternary ammonium salts, nicotine and some amino acids: possible implications for drug-water and drug-receptor interactions.

5. Affinities of the protonated and non-protonated forms of hyoscine and hyoscine N-oxide for muscarinic receptors of the guinea-pig ileum and a comparison of their size in solution with that of atropine.