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J Capillary Electrophor. 1998 May-Aug;5(3-4):153-8.
Determination of drugs used as anti-Parkinson's disease drugs in urine and serum by capillary electrophoresis.

Vargas G, Havel J, Babackova L, Patocka J.

Department of Analytical Chemistry, Faculty of Science, Masaryk University, Brno, Czech Republic.

A new capillary electrophoresis method to determine simultaneously eight of the most important anti-Parkinson's disease compounds has been developed. The generic names of the drugs studied are benactyzine (BA), trihexyphenidyl (TP), fenpiverin (FP), diphemin (DF), scopolamine (BL), adiphenine (TS), diethylaminoethylester 1-phenylcyclopentane-1-carboxylate (EKK), and diethylaminoethylester tetramethoxydiphenylacetate (EKO). An untreated fused-silica capillary tube (75 microns i.d., 57 cm total length, 49.5 cm length to the detector) was used with detection at 190 nm. The optimal separation conditions were 50 mM phosphate buffer (pH 2.7) with 7 mM-beta-cyclodextrin, electrokinetic injection for 15 sec at 5 kV, temperature 25 degrees C, and 15-20 kV separation voltage. Complete separation of all compounds was achieved in less than 16 min. The procedure was applied for the determination in urine and serum. The limits of detection (LOD, S/N = 3) for serum were 209 (FP), 234 (EKO), 168 (DF), 182 (BA), 168 (TP), 220 (BL), 174 (TS), and 163 (EKK) ppb. The method can be used for the therapeutic drug monitoring of these central active cholinolytics in clinical laboratories.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10797881&dopt=Abstract




Pharmacol Res. 2000 Jun;41(6):671-7.
Excitatory and inhibitory effects of second-generation cholinesterase inhibitors on rat gastrointestinal transit.

Braida D, Virag W, Ottonello F, Sala M.

Department of Pharmacology, Chemotherapy and Medical Toxicology, University of Milan, Via Vanvitelli 32, Milan, 20129, Italy.

We investigated the influence of increasing oral doses of second generation acetylcholinesterase inhibitors (AChEI) such as tacrine (0.25, 0.5, 1, 2, 3, 4, 10, and 20 mg kg(-1)), eptastigmine (0.5, 4, 8, 12, 20 and 40 mg kg(-1)) and E2020 (0.18, 0.25, 0.5, 1, 2, 3, 4 and 10 mg kg(-1)) on the distance travelled by a charcoal meal administered 30 min after each compound, in comparison with physostigmine (0.5, 1, 2, 4, 8 and 12 mg kg(-1)). An inverted U regression was observed with a significant parabola between the centimetres travelled and the log of the doses for all AChEI. The maximal stimulating doses (mg kg(-1)) were 2 for physostigmine, 4 for eptastigmine, 3 for tacrine and E2020, while the inhibitory doses were 12 for physostigmine, 40 for eptastigmine, 20 for tacrine and 10 for E2020. The stimulating and inhibiting effects on gastrointestinal propulsion were significantly reversed by 0.25 mg kg(-1)of scopolamine hydrobromide. A dose of scopolamine hydrobromide (0.06 mg kg(-1)) or methylbromide (0.25 mg kg(-1)), pirenzepine dihydrochloride (0.25 mg kg(-1)) and mecamylamine hydrochloride (0.5 mg kg(-1)), which per se did not affect gastrointestinal propulsion, antagonized both the stimulating and inhibitory effect of eptastigmine. Thus, the biphasic effect is peripherally mediated through both muscarinic (at least M(1)) and nicotinic receptors. Copyright 2000 Academic Press.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10816338&dopt=Abstract




Pharmacol Biochem Behav. 1989 Mar;32(3):707-10.
The effects of scopolamine and methylscopolamine on visual and auditory discriminations in male and female Wistar rats.

van Haaren F, van Hest A.

Netherlands Institute for Brain Research, Amsterdam.

The present experiment was designed to investigate whether or not the administration of scopolamine hydrobromide would differentially disrupt auditory or visual discrimination performance in male and female Wistar rats. Two groups of male and female Wistar rats were trained to discriminate between a continuous and intermittent visual stimulus, while two other groups were trained to discriminate between a continuous or intermittent auditory stimulus in a discrete-trial discrimination procedure. Once discrimination performance had stabilized, subjects were treated with different doses (0.125, 0.25, 0.50 or 1.0) of scopolamine hydrobromide or scopolamine methylbromide. Treatment effects were assessed with respect to discrimination performance, as well as with respect to the number of trials which were not completed. Scopolamine hydrobromide, but not scopolamine methylbromide, disrupted visual and auditory discrimination performance. The auditory discrimination was more seriously disrupted. However, both the administration of scopolamine hydrobromide and of scopolamine methylbromide increased the number of trials which were not completed suggesting that the accuracy of visual and auditory discriminations after drug treatment may have been influenced by other variables than drug effects on memory processes. Sex differences were not observed, neither with respect to discrimination performance, nor with respect to the number of trials which were not completed.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2740423&dopt=Abstract













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