Simple pharmacological test battery to assess efficacy and side effect profile of centrally acting muscle relaxant drugs.

Introduction: Centrally muscle relaxants (CMRs) are used mainly for treating muscle spasticities of neurological origin, and painful muscle spasms due to rheumatologic conditions. Their use is frequently associated with dose-limiting adverse effects. New drugs with improved side-effect characteristics are badly needed.

[Human positron emission tomography with oral 11C-vinpocetine].

Introduction: Positron emission tomography (PET) is a useful tool for the investigation of certain physiological changes and for the evaluation of the distribution, and receptor binding of drugs labelled with positron emitting isotopes. Vinpocetine (ethyl-apovincaminate) is a neuroprotective drug widely used in the prevention and treatment of cerebrovascular diseases. In the clinical practice vinpocetine is usually administered to the patients in intravenous infusion followed by long-term oral treatment.

[Cerebral uptake and regional distribution of [11C]-vinpocetin after intravenous administration to healthy men: a PET study].

Introduction: Vinpocetine is a compound widely used in the prevention and treatment of cerebrovascular diseases. The exact mechanism of action of the drug is still not known. The objective of the present investigation was to determine the global uptake and regional distribution of radiolabelled vinpocetine in the human brain.

[Neuroprotective effects of vinpocetine in vivo and in vitro. Apovincaminic acid derivatives as potential therapeutic tools in ischemic stroke].

The aim of the present study was to review neuroprotective therapy from the preclinical point of view as a potential tool for the treatment of stroke, as well as to discuss neuroprotective effects of the apovincaminic acid derivative vinpocetine (Cavinton). Our own in vivo and in vitro experiments were aimed at further characterizing pharmacological effects involved in the vinpocetine-induced neuroprotection. The effect of vinpocetine on infarct volume (obtained by 2,3,5-triphenyltetrazolium-chloride staining) was studied in permanent middle cerebral artery occlusion (MCAO) in rats (3 mg/kg i.

[TRH analogs at Gedeon Richter Ltd.: highlights of experimental and clinical efficacy of posatirelin].

The chemical research for dissociation of the central nervous system effects of thyrotropin-releasing hormone (TRH) from its hormonal activity resulted in the selection of RGH-2202 (posatirelin) for further development. Posatirelin showed stronger vigilance enhancing effect than TRH in a variety of commonly used neuro-psychopharmacological model in mice, rats and cats. This drug had positive effects in animal models of disturbed consciousness, and counteracted the decline of learning and memory capacity shown by aged or memory impaired rats.

[Investigation of neuromuscular blocking agents at Richter Ltd].

Investigation of new neuromuscular blocking agents was started 30 years ago in Richter Ltd. This paper presents the results obtained by Richter's scientists. 2 compounds out of 100 bisquaternary ammonio steroid having androstane skeleton were selected for further pharmacological study.

[Investigation of vasoactive agents with indole skeletons at Richter Ltd].

Investigation of agents with indol skeleton was started in Richter Ltd. 50 years ago. This paper presents the results obtained by Richter's scientists.

Clinical and non-clinical investigations using positron emission tomography, near infrared spectroscopy and transcranial Doppler methods on the neuroprotective drug vinpocetine: a summary of evidences.

Vinpocetine (Cavinton, Gedeon Richter, Budapest) is widely used as a neuroprotective drug in the prevention and treatment of cerebrovascular diseases. Vinpocetine is a potent inhibitor of the voltage-dependent Na(+) channels and a selective inhibitor of the Ca(2+)/caldmoduline-dependent phosphodiesterase 1. The clinical efficacy has been supported by several previous studies.

Drug distribution in man: a positron emission tomography study after oral administration of the labelled neuroprotective drug vinpocetine.

Direct information on the distribution of a drug requires measurements in various tissues. Such data have until now been obtained in animals, or have indirectly been calculated from plasma measurements in humans using mathematical models. Here we suggest the use of positron emission tomography (PET) as a method to obtain direct measurements of drug distribution in the human body.