FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to compounds, which possess agonistic or antagonistic activity of NGF and BDNF neutrophins and represent monomer or dimmer substituted dipeptides, which are analogues of exposed outside parts of loops 1 and 4 of said neutrophins, close to beta-bends of said loops or coinciding with them. Effects in vivo are demonstrated by claimed compounds within dose interval 0.01-10 mg/kg in intraperitoneal introduction.
EFFECT: claimed compounds possess neuroprotective and differentiating activity on cell models, increase concentration of phosphorylated form of tyrosine kinase A and proteins of heat shock Hsp32 and Hsp70 in concentrations10-5-10-9 M, they also possess neuroprotective, antiparkinsonian, anti-stroke, antiischemic, antidepressant, antiamnestic activity on animal models and demonstrate activity on experimental models of Alzheimer's disease.
20 cl, 33 dwg, 23 tbl, 18 ex
Title | Year | Author | Number |
---|---|---|---|
SULFOMALEIMIDE-BASED LINKERS AND CORRESPONDING CONJUGATES | 2019 |
|
RU2815199C2 |
ANTIBODY AND DRUG CONJUGATES (ADC) AND ANTIBODY AND PRODRUG CONJUGATES (APDC) CONTAINING ENZYMATICALLY CLEAVABLE GROUPS | 2016 |
|
RU2751512C2 |
CONJUGATES OF BINDER AND ACTIVE SUBSTANCE (ADC) HAVING ENZYMATICALLY CLEAVABLE GROUPS | 2017 |
|
RU2761390C2 |
CALICHEAMICIN DERIVATIVES AND THEIR ANTIBODY-DRUG CONJUGATES | 2018 |
|
RU2732568C1 |
ANTIBODY AND DRUG CONJUGATES FOR DESTRUCTION OF HEMATOPOIETIC STEM CELLS | 2017 |
|
RU2781444C2 |
AMIDE-BASED PRODRUGS OF GLUCAGON SUPERFAMILY PEPTIDES | 2009 |
|
RU2550696C2 |
CONJUGATE ANTIBODY-DERIVATIVE OF PYRROLOBENZODIAZEPINE | 2018 |
|
RU2820928C2 |
EXENATIDE ANALOGUE CONJUGATES WITH DELAYED RELEASE | 2017 |
|
RU2764547C2 |
ANTIBODY-DRUG CONJUGATES INCLUDING ANTIBODY AGAINST HUMAN DLK1 AND THEIR USE | 2020 |
|
RU2801630C2 |
PRODRUG COMPOSITIONS WITH HIGH DEGREE OF PENETRATION BASED ON PEPTIDES AND RELATED COMPOUNDS | 2010 |
|
RU2627065C2 |
Authors
Dates
2011-01-27—Published
2009-02-16—Filed