Experiments showed that a new drug composition containing pyrrolidone and pyroglutamic acid exhibits a significant cerebrovascular effect upon peroral administration in rats. The pharmacokinetics of pyrrolidone monitored upon its combined administration with pyroglutamic acid shows that this drug, as a component of the composition, is characterized by a high absolute bioavailability and permeability trough the blood-brain barrier. The presence of pyroglutamic acid slows down the absorption and elimination of pyrrolidone and enhances its distribution in the organs and tissues. There is a correlation between the concentration of pyrrolidone in the brain, on the one hand, and the levels of cerebral microcirculation and arterial pressure on the other hand. An increase in the concentration of pyrrolidone in the brain is accompanied by more intensive cerebral blood flow and by a decrease in the arterial pressure.

The pharmacokinetics of pyrrolidone in a composition with pyroglutamic acid was studied in white mongrel male rats. The former component exhibits cerebrovascular and neuroprotector activity. Pyrrolidone, detected in the blood plasma and brain for 8 h after peroral and intravenous administration, exhibits a high absolute bioavailability and the ability to penetrate via the blood-brain barrier.

The permeability through the blood-brain barrier of N-(4-hydroxy-3,3 dimethyl-2-oxo-1-butiryl) gamma-aminobutyric acid calcium salt, a new neurotropic drug calcium ketohomopantothenate (KPA-Ca), was studied in comparison with that of calcium homopantothenate, pantogam (P) Liquid chromatography analysis showed that after oral administration of KPA-Ca and P both forms of these agents, namely, oxy- and keto- derivatives of homopantothenic acid, were found in the brain of experimental rats, the KPA-Ca (ketoform) content being higher. Pharmacological studies showed that KPA-Ca penetrates the blood-brain barrier in greater amounts and causes a higher effect on the rate of cerebral blood flow when it is administered per os in a dose of 50 mg/kg.

The authors studied the permeability of the blood-brain barrier (CEB) to two nootropics: calcium ketogomopantothenate (KRA-Ca), a GABA derivative, and and calcium salt of oxybutyrate (OB-Ca), a derivative of GOBA. It was established that both preparations penetrate the CEB easily and are found in the brain at different intervals after their administration. However, essential differences in the distribution constant of these drugs were disclosed: KPA-Ca permeated the CEB more intensively and was accumulated in larger amounts in the late-term intervals.

The hemic hypoxia caused by the methemoglobin-inducing agent sodium nitrite (40 mg/kg intraperitoneally at days 10 to 19 of pregnancy) evokes a decrease in the birth and survival rates of pups, delayed disorders of motor coordination. Prenatal hypoxia was demonstrated to be able to disturb the habituation in the open field, learning and memory in passive avoidance paradigm, cognitive ability in the plus-maze extrapolative water escape test. The treatment of pregnant rats with sodium hydroxybutyrate (150 mg/kg orally 1-3 times daily at days 12 to 19 of pregnancy) normalizes offsprings' birth and survival rates, prevents the above-mentioned neuropsychological disturbances and improves learning in the active avoidance test.

The prenatal hemic hypoxia was caused by methemoglobin inducing agent, sodium nitrite, injected intraperitoneally in different doses from 10th to 19th day of pregnancy. It was shown that perinatal hemic hypoxia evoked delayed neurological deficit (disorders of motor coordination, hypodynamia) and disturbances of mnestic functions (impairment of learning and memory in passive and active avoidance paradigms and in the test of extrapolative water escape). The most pronounced disorders of CNS functions were shown in offsprings of male rats injected with sodium nitrite in a dose of 40 mg/kg.