[Results of a clinical study of a new anxiolytic, a blocker of central cholecystokinin receptors]. / Rezul'taty klinicheskogo issledovaniia novogo anksiolitika, blokatora tsentral'nykh kholetsistokininovykh retseptorov.

AIM: To evaluate anxiolytic action of GB-115, a low-affinity blocker of central cholecystokinin receptors, used in tablets in a dose of 1 mg for the treatment of patients with anxiety disorders in order to determine effective dose, safety, tolerability and efficacy in clinical settings. MATERIAL AND METHODS: The study included 31 patients (22 women, 9 men) diagnosed with generalized anxiety disorder (GAD, F41.1 according to ICD-10), aged from 22 to 53 years. The duration of treatment was 21 days. The Hamilton Anxiety Rating scale, Psychopathologic symptoms severity evaluation scale (PSSES), Spilberger State-Anxiety Inventory, Multidimensional Fatigue Inventory (MFI), Clinical Global Impression scale (CGI), computerized battery for evaluation of cognitive functions ('NS-Psychotest') were used. RESULTS AND CONCLUSION: The effective dose of GB-115 was determined at 6 mg per day. Drug action is characterized by fast onset of anxiolytic effect with stimulating properties and beneficial effect on sleep disturbances and autonomic symptoms. GB-115 treatment was associated with favorable changes in attention parameters, reaction time and overall performance. In contrast to first-line drugs for GAD treatment (SSRIs and SNRIs), GB-115 does not induce initial overactivation, anxiety and sleep disturbances. GB-115 is safe and has a good tolerability.

Pharmacological Correction of Alcohol Motivation Depends on the Phenotype of the Response to Emotional Stress.

The specific features of alcohol behavior were studied in MR and MNRA rats that exhibit an opposite reaction to emotional stress. We evaluated the effect of a dipeptide anxiolytic GB-115 (N-phenyl-hexanoyl-glycyl-L-tryptophan amide, neuropeptide cholecystokinin-4 analogue with antagonistic activity) on alcohol motivation in rats, which was formed over 12 months. High-emotionality MR rats were more sensitive to the anxiolytic effect of ethanol in the conflict situation test than low-emotionality MNRA rats. MNRA rats consumed a greater amount of ethanol under a free-choice condition with 15% ethanol solution and water (as in comparison with MR rats). However, the behavior of MR rats was transformed due to a significant increase in alcohol motivation from the 5th month of long-term free access to ethanol. An anxiolytic GB-115 (0.025 mg/kg intraperitoneally for 14 days) with selective activity in high-emotionality rats was shown to reduce significantly the average daily consumption and alcohol-deprivation effect in MR rats, but did not modulate ethanol addiction in MNRA rats.

[Prospects for designing Russian gene engineering agents for medicine. Rastan is the first Russian recombinant human growth hormone].

The development of modern pharmacology cannot be imagined without the use of genetic engineering methods (recombinant DNA technology). The success of medicine is increasingly based on the active use of protein preparations obtained using the technology of transferring hereditary information (genes) from one organism to another. The emergence of the ability to express foreign genes in the cells of various organisms (both eukaryotes and prokaryotes) has become one of the revolutionary events in the science of the last two decades of the 20th century and laid the foundations of modern biotechnology.