Molecules, Vol. 26, Pages 6124: A Novel Phenylpyrrolidine Derivative: Synthesis and Effect on Cognitive Functions in Rats with Experimental Ishemic Stroke
Molecules, Vol. 26, Pages 6124: A Novel Phenylpyrrolidine Derivative: Synthesis and Effect on Cognitive Functions in Rats with Experimental Ishemic Stroke
Molecules doi: 10.3390/molecules26206124
Authors:
Denis A. Borozdenko
Aiarpi A. Ezdoglian
Tatiana A. Shmigol
Darya I. Gonchar
Dmitri N. Lyakhmun
Dmitri V. Tarasenko
Yaroslav V. Golubev
Elvira A. Cherkashova
Daria D. Namestnikova
Ilya L. Gubskiy
Alexey A. Lagunin
Leonid V. Gubsky
Vladimir P. Chekhonin
Sophia S. Borisevich
Maxim A. Gureev
Anastasia D. Shagina
Nina M. Kiseleva
Vadim V. Negrebetsky
Yuri I. Baukov
We performed an in silico, in vitro, and in vivo assessment of a potassium 2-[2-(2-oxo-4-phenylpyrrolidin-1-yl) acetamido]ethanesulfonate (compound 1) as a potential prodrug for cognitive function improvement in ischemic brain injury. Using in silico methods, we predicted the pharmacological efficacy and possible safety in rat models. In addition, in silico data showed neuroprotective features of compound 1, which were further supported by in vitro experiments in a glutamate excitotoxicity-induced model in newborn rat cortical neuron cultures. Next, we checked whether compound 1 is capable of crossing the blood–brain barrier in intact and ischemic animals. Compound 1 improved animal behavior both in intact and ischemic rats and, even though the concentration in intact brains was low, we still observed a significant anxiety reduction and activity escalation. We used molecula...
Source: Molecules - Category: Chemistry Authors: Denis A. Borozdenko Aiarpi A. Ezdoglian Tatiana A. Shmigol Darya I. Gonchar Dmitri N. Lyakhmun Dmitri V. Tarasenko Yaroslav V. Golubev Elvira A. Cherkashova Daria D. Namestnikova Ilya L. Gubskiy Alexey A. Lagunin Leonid V. Gubsky Vladimir P. Chekhonin Sop Tags: Article Source Type: research