Pharmacological comparison between the actions of methamphetamine and 1-aminoindan stereoisomers on sympathetic nervous function in rat vas deferens
by
Glezer S, Finberg JP.
Department of Pharmacology,
Faculty of Medicine,
Technion, P.O. Box 9649,
Bat-Galim, Haifa 31096, Israel.
Eur J Pharmacol. 2003 Jul 11;472(3):173-7

ABSTRACT

The selective monoamine oxidase-B inhibitor selegiline (deprenyl) causes sympathomimetic effects and is metabolised to R(-)-methamphetamine and R(-)-amphetamine. The new monoamine oxidase-B inhibitor rasagiline is devoid of sympathomimetic effects and is metabolised to R(+)-1-aminoindan. Sympathomimetic effects of methamphetamine and 1-aminoindan enantiomers were compared in the rat vas deferens. R(-)-methamphetamine and S(+)-methamphetamine caused initial potentiation and subsequent inhibition of the field stimulation-induced twitch response of isolated rat vas deferens (0.1 Hz). EC(50) values for inhibition of twitch in prazosin-treated vas deferens were 0.36+/-0.13 and 1.64+/-0.10 microM (mean+/-S.E.M.) for S(+)- and R(-)-methamphetamine, respectively. There was no difference between S(+)-methamphetamine and R(-)-methamphetamine in potentiation of postsynaptic contractile response to noradrenaline. R(+)- and S(-)-1-aminoindan increased twitch response only at concentrations above 30 microM. R(-)-methamphetamine has similar potency to S(+)-methamphetamine in potentiation of noradrenaline-mediated responses and can therefore play a role in the sympathomimetic effects of selegiline.


Metabolites
Neuroprotection
Rasagiline: structure
MAO-b inhibitors/PD
Anti-apoptotic activity
Molecular mechanisms
Rasagiline pharmacology
Induction of pro-survival genes
Rasagiline and the mitochondria
Antioxidant strategies against aging
Anti-Alzheimer/anti-Parkinson's drugs
Rasagiline versus selegiline metabolites
Rasagiline/ anti-apoptotic bcl-2 gene family
Dual AChE and MAO inhibitors and Alzheimer's
Rasagiline v selegiline: neuronal survival effects
Rasagiline (Agilect) in early Parkinson's disease


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