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Title: The pharmacological activity of benzylamide derivatives of amino acids – inhibitorsof the selected SLC6 family transporters
Abstract:
SLC6 transporters are a group of protein carriers involved in thetransport of neurotransmitters, e.g. GABA and monoamines. One of the ways oftreating neurological and neuropsychiatric diseases is to inhibit the transportersbelonging to the SLC6 family.The aim of the work was to investigate the pharmacological activity ofcompounds that are inhibitors of GABA and monoamine carriers.It was assumed that the inhibition of SLC6 transporters evoked by thetested compounds would produce adequate pharmacological effects, especiallyanticonvulsant, anxiolytic, analgesic and antidepressant ones.In the experimental part of the work the methodology of in vitro and invivo studies on mice was presented. The research was divided into basic studies,in which the activity of all fifteen compounds was checked, and into expandedones, which were performed for the selected structures.Based on the results, the selective inhibition of the mGAT1 transporterhas been found responsible for the potent effect in the tests assessing anticonvulsant,anxiolytic, analgesic and antidepressant effects in mice. It seems thatthe inhibition of the remaining GABA transporters was less significant, whereasprocognitive activity may be a result of an inhibitory effect on the DAT transporterand moderate inhibition of the mGAT1 transporter.Compounds GT-53, GT-54, GT-94, GT-104 and GT-118 turned out tobe the most active ones i ; n the performed tests. It seems reasonable for thesecompounds to carry out additional studies concerning different mechanisms ofaction.
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Last modified:
Mar 14, 2023
In our library since:
May 6, 2019
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2
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All available object's versions:
http://dl.cm-uj.krakow.pl:8080/publication/4277
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| Edition name | Date |
|---|---|
| ZB-128301 | Mar 14, 2023 |
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