Carla Ghelardini1, Nicoletta Galeotti1, Lia Fantetti1,
Fulvio Gualtieri2,
Serena Scapecchi2 and Alessandro Bartolini1
1Department of Pharmacology, University of Florence, Viale
G. Pieraccini, 6, I-50139 Florence, Italy
2Department of Pharmaceutical Sciences, University of Florence,
Via G. Capponi, 9, I-50121 Florence, Italy
Abstract: R-(+)-Hyoscyamine (1 - 10 Ęg/kg, s.c.) dose-dependently
increased the local anesthetic effect of procaine (50 Ęg/ml) and lidocaine
(50 Ęg/ml) in the conjunctival reflex test in the rabbit. This potentiating
effect is completely prevented by the M1 antagonist dicyclomine
(10 mg/kg, s.c.). The intensity of R-(+)-hyoscyamine antinociception
was comparable to that induced by morphine (2 mg/kg, s.c.) and minaprine
(15 mg/kg, s.c.), used as analgesic reference drugs. In the same experimental
conditions, the S-(-)-enantiomer of atropine (0.1 - 10 Ęg/kg, s.c.),
was completely ineffective. The present results confirm the ability of R-(+)-hyoscyamine
to produce a paradoxical antinociceptive effect mediated by a cholinergic
mechanism not only in rodents but also in the rabbit.
Keywords: Atropine, R-(+)-Hyoscyamine, Antinociception, Local
anesthetics, Cholinergic system