Literature DB >> 6509264

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

S Cohen, F Haberman.   

Abstract

The partial molal volumes, V2, at infinite dilution of atropine and hyoscine were determined in each of eight different solvents having cohesive energy densities in the range 64 to 144 cal cm-3. V2 for hyoscine in a given solvent was invariably and significantly smaller than that of atropine in the same solvent. The difference being 1.58 cm3 mol-1 in the least polar solvent (n-propylbenzene) and 4.29 cm3 mol-1 in the most polar one (acetonitrile) in the series studied. It is proposed that the lower affinity of atropine relative to that of hyoscine for the muscarinic cholinoceptor could be accounted for by the relative increase in enthalpy in the adsorption of atropine to the receptor with respect to the same process with hyoscine.

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Year:  1984        PMID: 6509264      PMCID: PMC1987068          DOI: 10.1111/j.1476-5381.1984.tb16236.x

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


  10 in total

1.  A biophysical basis of ligand-induced activation of excitable membranes and associated enzymes. A thermodynamic study using acetylcholinesterase as a model receptor.

Authors:  B Belleau; J L Lavoie
Journal:  Can J Biochem       Date:  1968-11

2.  Interaction of atropine with the muscarinic receptor.

Authors:  P J Pauling; T J Petcher
Journal:  Nature       Date:  1970-11-14       Impact factor: 49.962

3.  A theoretical model study of the comparative effectiveness of atropine and scopolamine action in the central nervous system.

Authors:  H Weinstein; S Srebrenik; S Maayani; M Sokolovsky
Journal:  J Theor Biol       Date:  1977-01-21       Impact factor: 2.691

4.  The central and peripheral activities of anti-acetylcholine drugs. Some concepts of practical relevance.

Authors:  T D Inch; D M Green; P B Thompson
Journal:  J Pharm Pharmacol       Date:  1973-05       Impact factor: 3.765

5.  Characterization of muscarinic acetylcholine receptors from mouse brain: evidence for regional heterogeneity and isomerization.

Authors:  Y Kloog; Y Egozi; M Sokolovsky
Journal:  Mol Pharmacol       Date:  1979-05       Impact factor: 4.436

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

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

7.  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

8.  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

9.  Densitometric determination of the solubility parameter and molal volume of compounds of medicinal relevance.

Authors:  Z Liron; S Cohen
Journal:  J Pharm Sci       Date:  1983-05       Impact factor: 3.534

10.  A comparison of phenylalkyl- and phenoxyalkyl- trimethylammonium and triethylammonium salts; their apparent molal volumes at infinite dilution and effects on the frog rectus and guinea-pig ileum preparations.

Authors:  R B Barlow; F M Franks
Journal:  Br J Pharmacol       Date:  1973-11       Impact factor: 8.739

  10 in total
  1 in total

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

Authors:  S Cohen; F Haberman
Journal:  Br J Pharmacol       Date:  1985-08       Impact factor: 8.739

  1 in total

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