Picamilon

Acute experiments were conducted on rats under nembutal anesthesia to compare the efficacy of emoxipin with that of lithium oxybutyrate and picamilon in the postischemic period after preventive and therapeutic injections in various doses. Emoxipin proved to be most effective in prevention of postischemic non-restoration of the flow of blood in the brain and in preservation of the autoregulation responses of the cerebral vessels. The possible mechanisms of the effect of the drug are discussed.

Streptosotocin-induced diabetes in rats is accompanied by the development of diabetic complications such as neuropathies. [2-14C]serotonin and [U-14C]GABA release from the neurotransmitter pre-loaded synaptosomes showed significant elevation. Aldose reductase inhibitors (AL-1576, sorbinil) administration leads to partial restoration of serotonin and GABA release, while picamilon restored only GABA release. It was shown that Na+,K(+)-ATPase activities decreased in synaptosomes, synaptic membranes and sciatic nerve of diabetic rats compared to control...

A craniocerebral trauma was modelled in experiments on one-month-old rats. Oxidative phosphorylation in the brain mitochondria was studied by polarography 1, 4, 7 days and 4 weeks after the trauma. In the posttraumatic period the animals received piracetam (1 g/kg), picamilon (500 mg/kg), pyriditol (100 mg/kg), pantogam (160 mg/kg), ACTH (5-10) (0.1 mg/kg), nooglutyl (25 mg/kg), and GVS (0.5 mg/kg). It was found that piracetam, picamilon, and nooglutyl have a protective effect on the function of the brain mitochondria during the course of a craniocerebral trauma...

An open craniocerebral trauma was simulated in rat experiments. Oxidative phosphorylation in the brain mitochondria was studied by polygraphy 24 h after the trauma. It was found that trauma to the brain leads to inhibition of respiration in mitochondria in various metabolic states. Nooglutil in a dose of 50 mg/kg prevents these changes. Nooglutil is more effective than picamilon (500 mg/kg) and piriditol (100 mg/kg).

During four weeks rats were learned to visit consequently 4 baited arms in the 8-armed radial maze. Picamilone (nicotinoyl-GABA) in a dose of 10 mg/kg daily accelerated rats to reach 80% level of learning (to 20-28 trials). After picamilone injections rats obtained the maximal level of short-term memory as just 3-5 trials. Piracetam in a dose of 200 mg/kg daily exerted no effects on long-term and short-term memory of rats in the radial maze.

The antihypoxic properties of GABA-containing vitamin derivatives (pyridoxalphosphate-GABA, picamilone, pantogam, sodium homopantothenate) as compared with GABA were studied. All agents were found to increase mouse life expectancy under hypoxia in contrast to GABA.

Picamilon, a sodium salt of N-nicotinoyl-gamma-aminobutyric acid, was shown to induce a significant increase of cerebral blood flow in conscious cats. Picamilon was found to inhibit neurogenic spasms of cerebral vessels that was followed by suppression of tonic activity and reflectory discharges in sympathetic nerves. Picamilon led to restoration of the initial condition of cerebral hemodynamics disturbed by a previous administration of serotonin.

Methisergide and nicergoline act as competitive inhibitors whereas tolfenamic acid as a non-competitive inhibitor of 3H-serotonin accumulation which occurs with the involvement of the high-affinity system of serotonin uptake by the rat brain synaptosomes. Methisergide, nicergoline and tolfenamic acid at concentrations ranging close to Ki value were found to enhance the basal and K(+)-induced release of 3H-serotonin from the rat brain synaptosomes. The findings obtained indicate the ability of the drugs to disturb serotonin transport...

Male Wistar rats were divided in free choice conditions into heavy-drinkers consuming greater than 3.5 g/kg of ethanol daily (HD), and light-drinkers consuming less than 2.0 g/kg/day (LD). Subsequent 30 day intragastric administration of 25% ethanol (8-11 g/kg/day) caused an increase in permeability of the BBB to 14C-tyrosine, 14C-tryptophan and 14C-DOPA at all the stages of alcoholization. At late stages of intoxication (20-30 days) the penetration of horseradish peroxidase (HRP) indicating pinocytosis was present...

The velocity of absorption of GABA and its derivative picamilon carbon-labelled by isolated bovine retina has been studied. It is shown that maximal velocity of GABA and picamilon absorption falls at the second incubation minute, then it decreases. In all the cases the picamilon absorption velocity is higher than the GABA absorption velocity. With an increase of concentration in the incubation medium of the labeled preparation under study the absorption velocity of GABA remains practically unchanged, while that of picamilon slightly increases...