New AMPA receptor positive modulators for rehabilitation of patients after cerebral accidents

Pyatigorskaya N. V., Brkich G. E`., Lavrov M. I., Palyulin V. A., Alady'sheva Zh. I.

Journal of Pharmaceutical Sciences and Research

Vol.10, Issue5, P. 1103-1106

Опубликовано: 2018

Тип ресурса: Статья

Аннотация:

Stroke is an acute disorder of the cerebral circulation, characterized by a sudden appearance of focal neurological symptoms and/or cerebral symptoms, which persist for more than 24 hours or lead to death in a short period of time as a result of the cause of cerebrovascular origin. The search strategy for new drugs for the therapy of cognitive impairment and rehabilitation of patients who underwent acute brain hypoxia due to ischemia or other brain damage involves the search for substances affecting synaptic plasticity and having ability to increase the production of neurotrophic factors. A new class of AMPA receptor positive allosteric modulators (PAMs) based on the tricyclic derivatives of 3,7-diazabicyclo[3.3.1]nonane (bispidine) have been proposed using computer-aided molecular design techniques and further experimental studies. The innovative drug candidates with this scaffold provide the long-lasting activation of AMPA-receptors and production of neurotrophic factors, which allow

Ключевые слова:

AMPA receptors; BDNF; Brain-derived neurotrophic factor; Derivatives of 3, 7-diazabicyclo[3.3.1]nonane; NGF; PAM; Positive allosteric modulator; Rehabilitation of patients after brain damage

3,7 diazabicyclo[3.3.1]nonane; alpha amino 3 hydroxy 5 methyl 4 isoxazolepropionic acid; AMPA receptor; anticoagulant agent; bispidine; brain derived neurotrophic factor; dicarboxylic acid derivative; ion transport affecting agent; nerve growth factor; neuroprotective agent; neurotrophic factor; unclassified drug; allosterism; Article; brain function; brain hypoxia; brain ischemia; cerebrovascular accident; cognitive defect; computer aided design; glutamatergic synapse; human; learning; memory; molecular model; nerve cell plasticity; neurotransmission; nonhuman

Язык текста: Английский

ISSN: 0975-1459

Pyatigorskaya N. V. Natal`ya Valeryevna 1965-

Brkich G. E`. Galina E`duardovna 1967-

Lavrov M. I.

Palyulin V. A.

Alady'sheva Zh. I. Zhanna Igorevna 1967-

Пятигорская Н. В. Наталья Валерьевна 1965-

Бркич Г. Э. Галина Эдуардовна 1967-

Лавров М. И.

Палюлин В. А.

Аладышева Ж. И. Жанна Игоревна 1967-

New AMPA receptor positive modulators for rehabilitation of patients after cerebral accidents

Текст визуальный непосредственный

Journal of Pharmaceutical Sciences and Research

Vol.10, Issue5 P. 1103-1106

2018

Статья

AMPA receptors BDNF Brain-derived neurotrophic factor Derivatives of 3, 7-diazabicyclo[3.3.1]nonane NGF PAM Positive allosteric modulator Rehabilitation of patients after brain damage

3,7 diazabicyclo[3.3.1]nonane alpha amino 3 hydroxy 5 methyl 4 isoxazolepropionic acid AMPA receptor anticoagulant agent bispidine brain derived neurotrophic factor dicarboxylic acid derivative ion transport affecting agent nerve growth factor neuroprotective agent neurotrophic factor unclassified drug allosterism Article brain function brain hypoxia brain ischemia cerebrovascular accident cognitive defect computer aided design glutamatergic synapse human learning memory molecular model nerve cell plasticity neurotransmission nonhuman

Stroke is an acute disorder of the cerebral circulation, characterized by a sudden appearance of focal neurological symptoms and/or cerebral symptoms, which persist for more than 24 hours or lead to death in a short period of time as a result of the cause of cerebrovascular origin. The search strategy for new drugs for the therapy of cognitive impairment and rehabilitation of patients who underwent acute brain hypoxia due to ischemia or other brain damage involves the search for substances affecting synaptic plasticity and having ability to increase the production of neurotrophic factors. A new class of AMPA receptor positive allosteric modulators (PAMs) based on the tricyclic derivatives of 3,7-diazabicyclo[3.3.1]nonane (bispidine) have been proposed using computer-aided molecular design techniques and further experimental studies. The innovative drug candidates with this scaffold provide the long-lasting activation of AMPA-receptors and production of neurotrophic factors, which allow