PMID: 9175606Mar 1, 1997Paper

Stereoselective increase in cholinergic transmission by R-(+)-hyoscyamine

Neuropharmacology
C GhelardiniA Bartolini

Abstract

R-(+)-hyoscyamine, the dextro enantiomer of atropine, has been shown to amplify cholinergic transmission. R-(+)-hyoscyamine, unlike S-(-)-hyoscyamine, was able to increase acetylcholine release both in vitro and in vivo at a range of concentrations (10(-14) to 10(-12) M) and doses (5 microg/kg i.p.) which were inadequate for blocking muscarinic receptors. The increase over control values in ACh release was 15.9 +/- 2.1% in in vitro experiments performed in rat phrenic nerve-hemidiaphragm preparations (n = 6), and 63.3 + 16.3% in cortical microdialysis performed in free-moving rats (n = 5). The maximum ACh release was reached 60 min after R-(+)-hyoscyamine administration in in vivo experiments. At the same doses and concentrations, R-(+)-hyoscyamine was also able to elicit: antinociception of a cholinergic type (55.6-112.7% depending on the test used); complete prevention of scopolamine- and dicyclomine-induced amnesia; potentiation of muscular contractions electrically evoked in isolated guinea-pig ileum (16.7 +/- 3.6%) and in rat phrenic nerve-hemidiaphragm (19.9 +/- 3.2%) preparations. Antinociception was performed using the hot-plate and acetic acid abdominal constriction tests in mice, and the paw pressure test in rats, whi...Continue Reading

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Citations

Apr 29, 1999·Neuropharmacology·C GhelardiniA Bartolini
Aug 10, 2000·Fitoterapia·C GhelardiniA Bartolini
Sep 18, 2007·Current Opinion in Allergy and Clinical Immunology·Andrey Leonov, Leonard Bielory
Apr 12, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Bernard TestaAlessandro Pedretti
Dec 2, 1999·Japanese Journal of Pharmacology·C GhelardiniA Bartolini

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