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Medication, possessing anxiolytic activity. RU patent 2519191.

IPC classes for russian patent Medication, possessing anxiolytic activity. RU patent 2519191. (RU 2519191):

A61P25/22 - Anxiolytics

A61K31/4184 -

A61K31/38 - having sulfur as a ring hetero atom

A61K31/192 -

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Combination of anticancer agents / 2516027
Group of inventions refers to medicine, namely to oncology, and can be used for treating cancer in mammals, particularly lung cancer. That is ensured by administering the folate antimetabolite Pemetrexed in a combination with the antipurine/antipyrimidine endonuclease inhibitor Lucanton in therapeutically effective amounts into a mammal. There are also presented a pharmaceutical composition containing the above ingredients, and a kit comprising two pharmaceutical compositions of the above ingredients.

FIELD: chemistry.

SUBSTANCE: claimed is application of potassium salt 2-[1-(1,1-dioxothietanyl-3)benz-imidazolyl-2-thio]acetic acid (known as immunomodulator) as medication, possessing anxiolytic action. It is demonstrated that action of claimed medication on different anxiety components is comparable with effect of standard anxiolytics phenazepam and afobazole, but it is not accompanied by myorelaxant action characteristic of benzodiasepin anxiolytics (phenazepam).

EFFECT: improvement of composition efficiency.

2 tbl

The present invention relates to medicine and pharmacology, and can be used as a tool with anxiolytic activity.

Known substituted 2-[2-(3-exomorphic-4-yl)ethylthio]benzimidazole, with anxiolytic activity [patent RU 2373202, 2009].

The closest analogue of the invention are derivatives of 2-mercaptobenzimidazole with selective anxiolytic activity [patent RU 2061686, 1996].

The objective of the invention is to expand the Arsenal of biologically active substances, including with psychotropic effect with a pronounced anti-anxiety or anxiolytic properties.

The technical result - obtaining funds expressed anxiolytic activity.

The inventive use of potassium salt 2-[1-(1,1-dissociator-3)benzimidazole-2-thio]acetic acid (substance (I) formula

as a means, with anksioliticski action.

It is known that potassium salt of 2-[1-(1,1-dissociator-3)benzimidazole-2-thio]acetic acid (№ of state registration 9393889) has more immunomodulatory activity than levamisole with less 46.5 time toxicity. From available sources does not follow that the potassium salt of 2-[1-(1,1-dissociator-3)benzimidazole-2-thio]acetic acid (substance I) has anti-anxiety or anksioliticski action. This compound synthesized by boiling 1-(1,1-dissociator-3)-2-chlorobenzimidazole with thioglycolic acid in ethanol in alkaline medium receive 2-[1-(1,1-dissociator-3)benzimidazole-2-thio] acetic acid, passing in the interaction with caustic potash in ethanol in the target salt [patent RU 2115652, 1998].

For research anxiolytic actions using a variety of conflict behavior-collision positive (for example, drinking) and negative (fear of punishment) of motivations, as well as fear of various natural factors (e.g., height). Because anxiety is a complex phenomenon with many dimensions, with a study should be used several methods to estimate the effect of substances on different components of anxiety. The most popular ways to study anti-anxiety effects of substances are methods of conflict situations and uplifted cruciform labyrinth [T.A. Voronin, S. B. Seredenin. Methodical instructions for study tranquilizing (anxiolytic) actions pharmacological substances // Manual experimental (pre-clinical) studies of new pharmacological substances. / Under General edition of corresponding member of the Russian Academy of medical Sciences, Professor RU Khabriev. Second edition, revised and supplemented. - Moscow, 2005]. Methods the study was carried out in white outbred rats-males weighing 200-250 g

Anxiolytic effects potassium salt 2-[1-(1,1-dissociator-3)benzimidazole-2-thio]acetic acid (substance (I) was studied using a method of conflict situations and uplifted cruciform labyrinth, the most adequate to the task.

The conflict situation was created by the collision (conflict) in rats drinking motivation and electrobridge irritation [Liljiequist S. Engel J.A. The effects of GABA and benzodiazepine receptor antagonists on the anticonflict actions of diazepam or ethanol. // Pharmacology, Biochemistry & Behavior. - 1984. - Vol.21. - P.521-525; J. Vogel, Beer Century, Clody T. A simple and reliable conflict proceedure for testing antianxiety agents. // Psychopharmacologia. - 1971. - Vol.21. - P.1-7]. The study used developed in the laboratory psychopharmacology research Institute of pharmacology RAMS multilink installation conflict situations [Molodavkin G.M., Voronin T.A. Multichannel setup to search tranquilizers, and studying the mechanisms of their action by the method of conflicts // Experimental. and wedge Pharmacol. - 1995. - T, №2. - P.54-56]. The device consists of three parts: an experimental cameras, electronic block and counting device. Experimental baggage dimensions 275 x 275 x 450 mm made of organic glass. It is installed in a standard electrode floor, made of rods of stainless steel with a diameter of 4 mm with distance between them of 8-10 mm For each side wall of the camera attached drinking - glass vessel with a nipple in stainless steel. Nipple consisted of 2 cm at the camera at a height of 5 cm from the floor. Unlike many plants in our device drinking installed in the total volume of the camera, not in a darkened compartment. This is done for the reason that animals, being in a new environment in the power of instinct I try to hide in the dark compartment and can find the drinker is not the result of purposeful search for satisfaction of motivation, and by chance. Electrode floor and nipple drinkers were attached to the electronic module.

The electronic unit contains current stabilizers (one for each channel, allowing independent adjustment of current in them), the shapers of the output signals for counting device and shapers delay submission of punishment current drinkers in the day of the experiment. It provides registration not punishable takes water during the production of skill takes water (training, without a supply current drinkers), as well as punitive current and signals punishable takes water during the experiment.

Totalizer provides registration not punishable takes water during exercise and punishable takes water during the experiment. Some experiments registration of indicators was produced with the help of a personal computer Pentium III 550 MHz). For this purpose it was made a special device that converts the output signals of the electronic unit of the conflict situation in the standard pulses suitable for input into the serial port of the computer, and the program in language Basic) record events and time intervals in the disk files (with the EAST Solomaho). In future the data accumulated in these files were subjected to statistical analysis using statistical packages "Statgraf" and "Statistica for Windows.

The experiment was carried out in 3 days. On the first day of the animals were completely deprived of drinking. The next day, i.e. after a 24-hour deprivation, conducted the development of the skill of taking water from the trough. For this animal on 5 min placed in the experimental chamber. The animals were examined by the chamber, after some time found a drinker and started drinking. On this day the drinker and the floor of the chamber gave a weak current (mA 0,05), feel rats, so take water were not punishable, and their number has characterized the severity of drinking motivation. On the third day of the animals again on 10 mines were placed in the experimental chamber, but this time in 10 seconds after first taking on water nipple drinkers and electrode floor cameras filed a constant current to 0.25 mA, so that each take the water was punishable and to meet the thirst rats had to overcome fear, evolved as a result of punishment. In the experiment the power of punishment current exceeded the same indicator during exercise 5 times, and that created conditions of anxiety. Measure the severity of the effect was considered significant increase in the number punishable takes water from the trough animals in the experimental group compared to control.

Studies using the method of conflict situations in rats is developing very strong stress condition caused by drinking deprivation and electric shock. For this reason, behavioural studies also use a more gentle method uplifted cruciform labyrinth in which to evaluate the fear of rats height and open space [Pellow S., File S.E. Anxiolytic and anxiogenic drugs effects on exploratory activity in an elevated plus-maze. A novel test of anxiety in the rat. // Pharmacology, Biochemistry & Behavior. - 1986. - Vol.24. - P.525-529].

Method uplifted cruciform labyrinth

The work was carried out on white outbred rats weighing 200-250 g Labyrinth is a 2 sleeves of a width of 15 cm and a length of 1 m, fastened at right angles in the middle. 2 the opposite sleeves of the maze have wall dimensions 40 x 40 cm (they are closed), and the other two walls are not (they are considered open). All the device is installed at a height of 1 m above the floor level.

Rats were placed in the center of the labyrinth and within 3 minutes visually estimated the number of visits to public and private arm of the maze, stay in, and the number of smeshivanie in the open part of the maze. For registration of the estimated indicators used a program written in a language QBASIC 4.5, which made it possible to link behavioral acts carried out by the rat, with pressing certain keys of the computer keyboard. The program has calculated the indicators for each animal, built summary table of calculation of averages and standard deviations and write it to disk as a file [G.M. Molodavkin, T.A. Voronin. Computer programs for registration of the results of behavioral experiments. Experimental and clinical pharmacology, 2005, t, №6, p.55-58].

Substance I was injected intraperitoneally at doses of 2.5, 5 and 10 mg/kg for 30 minutes before experience. As Comparators used phenazepam at a dose of 0.5 mg/kg and blood in the dose of 5 mg/kg

When aggregated to calculate mean values and standard deviation at P<0.05. The significance of differences between groups were determined using analysis of variance [Borovikov VP Statistical art analysis of data on your computer. For professionals. - SPb.: Peter, 2001. - 656 with; B. Duke, data Processing on PC in the examples. Peter, St. Petersburg (1997)].

The results of a study investigating the impact of substance I in the behavior of rats in a conflict situation. As is known, the rats in the control group in the day experience rush to the drinkers, but, on receiving an electric shock, do not attempt to satisfy thirst. At the same time they carry out 80±66,88 (without the introduction of distilled water) and 124,2±66,2 (after the introduction of distilled water) is punishable takes water (table 1). Phenazepam at a dose of 0.5 mg/kg have anxiolytic effect, which manifested itself in the increase in the number punishable takes water to 382,9±36,96 (the difference with the control significantly at P<0.05). The effect of fenazepam accompanied miorelaksantny effect, visible, but parkovanim at this dose. Afobazole (5 mg/kg also have anxiolytic effect, increasing the number punishable takes water to 264,5±51,58 (the difference with the control also reliably). Afobazole, unlike phenazepam, had no miorelaksantnoe actions. Phenazepam on the severity engaged in anti-conflict effect surpassed afobazole by 45%. Substance I in a dose of 2.5 mg/kg has the effect similar action phenazepam and the effects, that is, also increases the number punishable takes water to 263,9±71,32 (table 1, the difference with the control reliably). In other doses (5, and 10 mg/kg) substance has less effect. Unlike phenazepam matter I do not has miorelaksantny actions.

It is established that the rats in the control group, being placed in the centre uplifted cruciform labyrinth, spending some time in it, leave in the private arm of the maze and spend most of the time there. Occasionally animals briefly come out in the open sleeves and do there are a small number of smeshivanie. This type of behavior is evidence of high anxiety. Anxiolytics (and phenazepam, and afobazole) increase the number of outputs in the open arm of the maze, stay in, and the number of smeshivanie (table 2). This indicates a decrease anxiety in rats. Substance I in a dose of 5 mg/kg has similar effects: increases the number of outputs in the open arm of the maze, while staying in them, increases the number of smeshivanie (table 2). Consequently, dose in this matter I also reduces anxiety rats (has anxiolytic effects). At introduction in other doses (2.5 and 10 mg/kg) material I has less effect.

Thus, in the result of the work using methods of conflict situations and uplifted cruciform labyrinth, it was found that the substance I renders anti-anxiety (anxiolytic) action comparable to the effects of reference anxiolytics phenazepam and the effects on both tests.

Anxiolytic effects of substance I not accompanied typical benzodiazepine anxiolytics (phenazepam) miorelaksantny effect. It can be assumed that the substance I have high potential as an anxiolytic.

TOOL THAT HAS ANXIOLYTIC ACTIVITY

Table 1

The impact of substance I in the number punishable takes water in a conflict situation in rats

Group

Dose, mg/kg

Among the punishable takes water

Control

Anti-lock brakes. Net

80,0±66,88

Control

Diest. In

124,2±66,2

Phenazepam

0,5

382,9±36,96 *

Afobazole

5,0

264,5±51,58 *

Substance I

2,5

263,9±71,32 *

Substance I

5,0

of 174.4±54,95

Substance I

10,0

88,8±31,65

Note:

* - the difference with the control group significantly at P<0.05.

The use of potassium salts 2-[1-(1,1-dissociator-3)benzimidazole-2-thio] acetic acid formula

as a means, with anksioliticski action.