bemethyl and Brain-Ischemia

It was established that a new 3-hydroxypyridine (3-HP) derivative, 2-ethyl-6-methyl-3-hydroxypyridine L-aspartate (3-HP), in small doses (1 and 5 mg/kg) increased physical performance in treadmill and swimming tests on rats. The new substance showed greater or equal effects compared to the reference actoprotector drugs metaprot and ladasten in much higher doses. The gluconeogenesis inhibitor tryptophan significantly (74 ± 5%, p < 0.01) prevented this stimulatory effect of 3-HPA in the treadmill test on rats. 3-HPA at a higher dose (30 mg/kg) had marked antiamnesic effect on various models of amnesia in mice. It was more effective than reference drugs mexidol (another 3-HP derivative) in a dose of 30 mg/kg and nootropic drug piracetam in a dose of 200 mg/kg, but had equal effect with these drugs in doses of 50 and 800 mg/kg, respectively. 3-HPA (30 mg/kg per day) had neuroprotective effect in rats with brain ischemia and decreased the neurologic deficiency more effectively than mexidol (50 mg/kg per day).

Topics: Adamantane; Amnesia; Animals; Animals, Outbred Strains; Anticonvulsants; Benzimidazoles; Brain Ischemia; Disease Models, Animal; Exercise Test; Gluconeogenesis; Male; Mice; Neuroprotective Agents; Nootropic Agents; Physical Conditioning, Animal; Picolines; Piracetam; Rats; Swimming; Tryptophan

Cerebral ischemia in rats (both carotid arteries occlusion) during 30 min, 3 hours and recirculation (1 hour) after ischemia (30 min) stimulated diene conjugates and fluorescent products accumulation in brain tissue. Intraperitoneal injection of sodium hydroxybutyrate (100 mg/kg), bemitil (50 mg/kg), ethomersol (50 mg/kg) reduced brain lipid peroxidation and did not yield in this respect to emoxypin (5 mg/kg). In contrast to emoxypin, sodium hydroxybutyrate, bemitil and ethomersol had no antiradical activity.

Topics: Animals; Antioxidants; Arterial Occlusive Diseases; Benzimidazoles; Brain Ischemia; Carotid Artery Diseases; Picolines; Rats; Rats, Wistar; Sodium Oxybate

Influence of natrii hydroxybutyrate (100 mg/kg), ascorbate (100 mg/kg), cavinton (5 mg/kg), bemitil (50 mg/kg), ethomersol (50 mg/kg) on Hb-O2 affinity and cortex PO2 after both carotid artery occlusion in rats was investigated. Correlation (r-0.87; P less than 0.05) between lowering of Hb-O2 affinity and antihypoxic effect was demonstrated in the line of these drugs.

Topics: Acute Disease; Animals; Antioxidants; Ascorbic Acid; Benzimidazoles; Brain Ischemia; Drug Evaluation, Preclinical; Hemoglobins; Hypoxia, Brain; Oxygen; Rats; Sodium Oxybate; Vasodilator Agents; Vinca Alkaloids