Delving into the Latest Updates on Research Zakusov Institute of Pharmacology with Synapse

概览

排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

CCK receptor(胆囊收缩素受体)	1

关联

1

项与 Research Zakusov Institute of Pharmacology 相关的药物

Ranquilon

靶点

CCK receptor

作用机制

CCK receptor拮抗剂

在研机构

Valenta Pharmaceuticals JSC [+1]

原研机构

Research Zakusov Institute of Pharmacology

在研适应症

适应障碍 [+2]

非在研适应症-

最高研发阶段临床3期

首次获批国家/地区-

首次获批日期-

100 项与 Research Zakusov Institute of Pharmacology 相关的临床结果

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0 项与 Research Zakusov Institute of Pharmacology 相关的专利（医药）

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150

项与 Research Zakusov Institute of Pharmacology 相关的文献（医药）

2024-03-01·Pharmaceutical Chemistry Journal

Low Molecular Weight NGF Mimetic Enhances the Overall Plasma Antioxidant Capacity in Rats with Streptozotocin-Induced Diabetes

作者: Savina, A. D. ; Gudasheva, T. A. ; Selivanova, I. A. ; Ostrovskaya, R. U. ; Terekhov, R. P. ; Ivanov, S. V. ; Ilyasov, I. R. ; Olicheva, V. V.

Results from studies of the antidiabetic and antihyperglycemic activity of a low-mol.-weight NGF mimetic, compound GR-2 [bis-(N-monosuccinyl-L-glutamyl-L-lysine)hexamethylenediamide], on a streptozotocin-induced diabetes model in Wistar rats are presented.GK-2 administered perorally at a dose of 5 mg/kg for 28 d significantly reduced the glycemia level in diabetic rats and increased the overall plasma antioxidant capacity.The glycemia level and plasma antioxidant capacity were in an inverse exponential relationship and were closely correlated to each other (correlation coefficient 0.899).

2024-03-01·Pharmaceutical Chemistry Journal

Stereospecificity of the Cytoprotective and Antidepressant-Like Activities of GTS-301, a Dimeric Dipeptide Mimetic of Neurotrophin-3

作者: Nikolaev, S. V. ; Logvinov, I. O. ; Seredenin, S. B. ; Povarnina, P. Yu. ; Antipova, T. A. ; Nikiforov, D. M. ; Melnikova, M. V. ; Sazonova, N. M. ; Zhanataev, I. A. ; Gudasheva, T. A. ; Tarasiuk, A. V.

A dimeric dipeptide mimetic based on the β-turn of the 4^th loop of neurotrophin-3, bis-(N-monosuccinyl-L-asparaginyl-L-asparagine)hexamethylenediamide (GTS-301LL), was recently designed and synthesized by us.GTS-301, like the full-length neurotrophin, activated TrkC and TrkB receptors and exhibited neuroprotective activity on HT22 cells under oxidative stress conditions in the concentration range 10^-5 - 10^-12 M and antidepressant-like activity in the forced swimming test in mice (10 - 40 mg/kg, i.p.).The stereospecificity of the pharmacol. effects of GTS-301LL was revealed by synthesizing the LD, DL, and DD stereoisomers of GTS-301LL and studying their neuroprotective and antidepressant-like properties under the same conditions as for GTS-301LL.Both activities were found to disappear on going from the LL to the DL and DD stereoisomers and were retained on going to the LD stereoisomer.Thus, the stereospecificity of the neuroprotective and antidepressant-like activities of the dipeptide mimetic of neurotrophin-3 GTS-301LL at the N-terminal asparagine residue was proven, which indicated the key role of that amino-acid residue in the interaction with the receptor.

2024-03-01·Pharmaceutical Chemistry Journal

Study of the Pressing Process of N-Butyl-N-Methyl-1-Phenylpyrrolo-[1,2-a]Pyrazine-3-Carboxamide (GML-3) Tablets Using Mathematical Modeling Techniques

作者: Markeev, V. B. ; Tishkov, S. V. ; Blynskaya, E. V. ; Alekseev, K. V.

N-Butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3) is an original mol. developed at the Research Zakusov Institute of Pharmacol.GML-3 has both anxiolytic and antidepressant activity, which makes the development of tablets based on it a promising task.Optimization of the pressing process is currently an urgent task of the pharmaceutical industry because this technol. stage has a significant impact on the disintegration of tablets and the release of the active pharmaceutical ingredient.The Heckel and Kuenz-Leuenberger models were used to study the pressing process of GML-3 tablets.These models were compared to select the most reliable description of pressing GML-3 tablets from granules.Granules with polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC) as a binder were used.

100 项与 Research Zakusov Institute of Pharmacology 相关的药物交易

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100 项与 Research Zakusov Institute of Pharmacology 相关的转化医学

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