LABORATORY OF PHARMACOLOGY

Organized in 1968 the Laboratory of Pharmacology of Institute of Chemistry named after V.I. Nikitin in Tajikistan Academy of Sciences, is the center of creating new therapeutic drugs. Establishing of Laboratory of Pharmacology at the Institute of Chemistry, has enabled the Institute to go out with her preparations to the international arena and to obtain a high recognition of the international community of pharmacists. Long-term experimental and theoretical studies have allowed the laboratory to open new trends of pharmacology in this area.This is the only center that has its own subsidiaries in screening studies of new chemical compounds in the Tajik State National University and Tajik State Medical University.

The laboratory staff had pharmacological screening tests of more than five thousand chemically synthesized compounds and plant products for the selection of high-level connections for further in-depth study and creation of new drugs. Long-term experimental and theoretical studies have allowed members of the laboratory of pharmacology under the supervision of Academician of AS RT Karim Khaidarovich Khaidarov, open new trends in this area.

KARIM KHAIDAROVICH KHAIDAROV

Head of Laboratory, Winner of the Council of Ministers prize of the Tajik SSR (1985), Honored Inventor of the Republic of Tajikistan (1989), Winner of prize of AS RT named after Academician - S. U. Umarov (2008), Academician of the AS RT, doc. of medical sciences, prof.

Has been studied comparative effects of papaverine and its N-derivatives, given pharmacological characteristics of alkaloids aporfine series, in particular - kabudina. Kabudin - new aporfine alkaloid, for the first time isolated from the meadow-rue (isopiroid) at the Institute of Chemistry of the Academy of Sciences of RT. Its sulfate and iodmetilat first subjected to pharmacological analysis showed its an anti-arrhythmic and a hypotensive properties.

In trying to find new anesthetic the laboratory pharmacology has studied local anesthetic properties of new β-aminoketones derivatives of tiochromanov and tiaindanov.

Investigated the pharmacological activity and choleretic properties of derivatives of ksantogenat acid.

Under the guidance of Academician Khaidarova K.H. and doc. of chem. sciences, prof. Kadirov A.H. first developed preparative methods of synthesis of glycerol ester of cholic and chenodezoxicholic acids, which can be used as an oral litolitic medication. The new obtained compounds - derivatives of cholic acid have the greatest ability to dissolve cholesterol gallstones compared with the known means of similar purpose. (Patent № TJ RT 237 - Glycerine ester of 3 α, 7 α - dyhydroxicholic acid, the method of its production and its use as a medicament. Kadirov A.K., Khaidarov K.H., Nazarova Z.D., Nazarov V.A.).

On the basis of these compounds produced a new drug "Trioin 'patented RT.

Senior staff scientist, cand. of chem. sciences. Nazarova Z. and main staff scientist., Winner of prize of AS RT named after Academician S. U. Umarov (2008), doctor of chemical sciences A.H. Kadirov.

Studies on development of obtaining technology of cholic acid from the bile of cattle. (Development and implementation of technology for cholic acid obtaining qual. CP from the bile of cattle. Ministry of Health Committee Tajikfarmindustry, from 12.03.1997.) These substances may be used by the Ministry of Health, the Committee Tajikfarmindustry.

To solve the problems of diagnosis and effective treatment of gallstone disease and other disorders of the liver in the laboratory of pharmacology, first developed the technique of determining the content of bile and fatty acids in bile and serum by gas-liquid chromatography. Here was established the depending of the content of bile and fatty acids on the stages of gallstone disease and other diseases of the liver. The results are implemented in the clinics of the Institute of Gastroenterology, Academy of Sciences of Tajikistan and a number of other clinics in the CIS countries.

The technological scheme for producing balm "Sino" products based on medicinal plants, with a view to expanding the range of balms with a high biological value. For the first time found that the balm "Sino" exhibits choleretic, litolitic, hypolipidemic, as well as anti-inflammatory effect. (Eurasian patent number 005,233 on the application number 20,010,154. 12/30/2004. The composition of ingredients for balm "Sino." Authors: Kadyrov AK, Khaidarov KH Ishankulova BA, AA Kadyrov)

At the Laboratory of Pharmacology learned a huge amount of organic compounds containing a heteroatom in the structure of sulfur. Among these compounds are found drugs with hypnotic, anticonvulsant, mioreluxing, drug, antibacterial, leykostimuliruyuschim, anti-inflammatory actions.

Leading scientific officer, doctor of medical sciences A.A. Saidov.

Based on the analysis of the modern state of drug treatment of epilepsy, a new original product - karbatin, surpassing in its pharmacological properties known anticonvulsants. Currently karbatin is a major antiepileptic drug with a broad spectrum of activity compared to phenobarbital and carbamazepine.

Very valuable and original researches are studies of pharmacological activity of derivatives chlorbenzotiofena the results of which formed the basis for the search of the compounds of this class of substances, anti-arrhythmic action.

Laboratory staff at work. Left to right: cand.med.scinces F.M. Khodjaevа main staff scientist, Laureate of State Prize of the Council of Ministers of the Tajik SSR (1988), doc.med.sciences, Rakhimov I.F., a graduate E.R. Arutyunyan.

Study of sensitizing activity of derivatives of alcohol and dithiocarbamic ksantogenat acids are subject to search among this group of substances of antialcohol products.

Along with the screening of new chemical compounds in the laboratory of pharmacology have been developed and researched in the field of pharmacotherapy. In particular, given the comparative analysis of sulfonamides on the effect of the blood clotting system.

Here was analyzed of comparative pharmacological study of sea buckthorn oil, obtained by different methods. Studied its biochemical mechanism of action, identified antiulcerogenic effect.

Khaidarov K.H. with the laboratory staff have created a "bank" of data on the dependence of the "structure-effect" among a number of original compounds, which allows researchers to perform targeted synthesis of biologically active substances and their search on the basis of high-performance drugs.

In the base of Laboratory of Pharmacology and scientific advice of academician Khaidarova K.H. develop research in the development of immuno-modulatory drugs on the basis of low molecular weight peptides with activity thymic hormones and their biocoordinate compounds with biologically important metals.

Within the laboratory of pharmacology has developed and recommended to the medical industry the following products:

1. New koronarorasshiryayuschego drug "Triakantin"

2. Antiepileptic drug "Karbatin"

3. Common regenerative drug "Sea-buckthorn oil," resulting in new technology.

4. Immuno-modulatory drugs "Timogar" and "Timotsin" used in the treatment of liver diseases, gastrointestinal, musculoskeletal system, physical fatigue.

5. The new alkaloid "Kabudin" of local medicinal plants used in the treatment of cardiac arrhythmias.

6. A new analeptic based on the alkaloid cytisine, cytisine superior.

7. New choleretic drug "Berolina" based on derivatives of the alkaloid "berberine", isolated from barberry.

At the Laboratory of Pharmacology of Institute of Chemistry of AS RT protected 13 doctoral and 35 master's theses, received 100 patents. Published over 500 scientific articles in various magazines, both national press and in foreign literature. Received eight innovations.

Issued 4 books on the chemistry of heterocyclic compounds and their physiological activity, derivatives cholic acid and their physiological activity, therapeutic plants in Tajikistan, the methods of developing new drugs.

We are now preparing a monograph "Karbotin - a new epileptic agent." The laboratory has close links with the Institute of Pharmacology of Russian Academy of Medical Sciences, All-Union Scientific Research Chemical-Pharmaceutical Institute named after S. Ordzhonikidze, Institutes of Pharmacology of Czech and Bulgarian Academies, the Department of Pharmacology of the Tajik State Medical University named after Abu Ali Ibn Sina.