Glyproline Pro-Ampakine with Neuroprotective Activity
Previously it was shown that neuropeptide cyclo-L-prolylglycine (CPG) is a positive modulator of AMPA receptors, which increases BDNF level in neuronal cell cultures. The spectrum of CPG’s pharmacological effects corresponds to that of BDNF. Dipeptide N-phenylacetyl-glycyl-L-proline ethyl ester (GZK...
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| Format: | Book Chapter |
| Language: | English |
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2020
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| Online Access: | https://www.intechopen.com/chapters/71098 |
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| author | Koliasnikova, Ksenia N. Povarnina, Polina Yu. Tallerova, Anna V. Firsova, Yulia N. Nikolaev, Sergei V. Antipova, Tatiana A. Nadorova, Anna V. Kolik, Larisa G. Gudasheva, Tatiana A. Seredenin, Sergei B. |
| author_browse | Antipova, Tatiana A. Firsova, Yulia N. Gudasheva, Tatiana A. Koliasnikova, Ksenia N. Kolik, Larisa G. Nadorova, Anna V. Nikolaev, Sergei V. Povarnina, Polina Yu. Seredenin, Sergei B. Tallerova, Anna V. |
| author_facet | Koliasnikova, Ksenia N. Povarnina, Polina Yu. Tallerova, Anna V. Firsova, Yulia N. Nikolaev, Sergei V. Antipova, Tatiana A. Nadorova, Anna V. Kolik, Larisa G. Gudasheva, Tatiana A. Seredenin, Sergei B. |
| author_sort | Koliasnikova, Ksenia N. |
| building | IntechOpen |
| collection | Acceso abierto |
| description | Previously it was shown that neuropeptide cyclo-L-prolylglycine (CPG) is a positive modulator of AMPA receptors, which increases BDNF level in neuronal cell cultures. The spectrum of CPG’s pharmacological effects corresponds to that of BDNF. Dipeptide N-phenylacetyl-glycyl-L-proline ethyl ester (GZK-111) was designed and synthesized as a linear analog of CPG. The aim of the present work was to reveal the pharmacological profile of GZK-111. Dipeptide GZK-111 was shown to metabolize into CPG in vitro and increased cell survival by 28% at concentrations of 10-7–10-6 M in a Parkinson’s disease cell model. In a model of cerebral ischemia, GZK-111, at a dose of 0.5 mg/kg, i.p., was found to have neuroprotective effects, reducing the cerebral infarct volume by 1.6 times. Similar to CPG, GZK-111, at the range 0.1–1.0 mg/kg, i.p., possessed a stereospecific antiamnesic activity. A significant anxiolytic effect was observed at a dose of 1.5 mg/kg. GZK-111, at the range 0.5–4.0 mg/kg, i.p., demonstrated analgesic activity. GZK-111, at a dose of 10 mg/kg/7 days, i.p., possessed antidepressant-like activity. So, the neuroprotective, nootropic, antihypoxic, anxiolytic, antidepressant-like, and analgesic effects of GZK-111 were revealed. Thus, GZK-111 can be considered as a pharmacologically active pro-ampakine with a BDNF-ergic mechanism of action. |
| doi_str_mv | 10.5772/intechopen.91192 |
| first_indexed | 2026-10-15T21:38:29Z |
| format | Book Chapter |
| fullrecord | <oai_dc:dc xmlns:oai_dc="http://www.openarchives.org/OAI/2.0/oai_dc/" xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xsi:schemaLocation="http://www.openarchives.org/OAI/2.0/oai_dc/ http://www.openarchives.org/OAI/2.0/oai_dc.xsd"><identifier>intech-71098</identifier><datestamp>2020-02-18</datestamp>
<dc:title>Glyproline Pro-Ampakine with Neuroprotective Activity</dc:title>
<dc:creator>Ksenia N. Koliasnikova</dc:creator>
<dc:creator>Polina Yu. Povarnina</dc:creator>
<dc:creator>Anna V. Tallerova</dc:creator>
<dc:creator>Yulia N. Firsova</dc:creator>
<dc:creator>Sergei V. Nikolaev</dc:creator>
<dc:creator>Tatiana A. Antipova</dc:creator>
<dc:creator>Anna V. Nadorova</dc:creator>
<dc:creator>Larisa G. Kolik</dc:creator>
<dc:creator>Tatiana A. Gudasheva</dc:creator>
<dc:creator>Sergei B. Seredenin</dc:creator>
<dc:subject>Health Sciences</dc:subject>
<dc:description>Previously it was shown that neuropeptide cyclo-L-prolylglycine (CPG) is a positive modulator of AMPA receptors, which increases BDNF level in neuronal cell cultures. The spectrum of CPG’s pharmacological effects corresponds to that of BDNF. Dipeptide N-phenylacetyl-glycyl-L-proline ethyl ester (GZK-111) was designed and synthesized as a linear analog of CPG. The aim of the present work was to reveal the pharmacological profile of GZK-111. Dipeptide GZK-111 was shown to metabolize into CPG in vitro and increased cell survival by 28% at concentrations of 10-7–10-6 M in a Parkinson’s disease cell model. In a model of cerebral ischemia, GZK-111, at a dose of 0.5 mg/kg, i.p., was found to have neuroprotective effects, reducing the cerebral infarct volume by 1.6 times. Similar to CPG, GZK-111, at the range 0.1–1.0 mg/kg, i.p., possessed a stereospecific antiamnesic activity. A significant anxiolytic effect was observed at a dose of 1.5 mg/kg. GZK-111, at the range 0.5–4.0 mg/kg, i.p., demonstrated analgesic activity. GZK-111, at a dose of 10 mg/kg/7 days, i.p., possessed antidepressant-like activity. So, the neuroprotective, nootropic, antihypoxic, anxiolytic, antidepressant-like, and analgesic effects of GZK-111 were revealed. Thus, GZK-111 can be considered as a pharmacologically active pro-ampakine with a BDNF-ergic mechanism of action.</dc:description>
<dc:publisher>IntechOpen</dc:publisher>
<dc:date>2020-02-18</dc:date>
<dc:type>Chapter, Part Of Book</dc:type>
<dc:identifier>https://www.intechopen.com/chapters/71098</dc:identifier>
<dc:identifier>doi:10.5772/intechopen.91192</dc:identifier>
<dc:language>en</dc:language>
<dc:relation>ISBN:978-1-83880-439-8</dc:relation>
<dc:rights>https://creativecommons.org/licenses/by/3.0/</dc:rights>
<dc:source>https://www.intechopen.com/books/8087 ; Neuroprotection - New Approaches and Prospects</dc:source>
</oai_dc:dc> |
| id | intech-71098 |
| institution | IntechOpen |
| isbn | 978-1-83880-439-8 |
| language | English |
| last_indexed | 2026-10-15T21:38:29Z |
| publishDate | 2020 |
| publishDateRange | 2020 |
| publishDateSort | 2020 |
| publisher | IntechOpen |
| publisherStr | IntechOpen |
| record_format | oai_dc |
| spelling | intech-710982020-02-18 Glyproline Pro-Ampakine with Neuroprotective Activity Ksenia N. Koliasnikova Polina Yu. Povarnina Anna V. Tallerova Yulia N. Firsova Sergei V. Nikolaev Tatiana A. Antipova Anna V. Nadorova Larisa G. Kolik Tatiana A. Gudasheva Sergei B. Seredenin Health Sciences Previously it was shown that neuropeptide cyclo-L-prolylglycine (CPG) is a positive modulator of AMPA receptors, which increases BDNF level in neuronal cell cultures. The spectrum of CPG’s pharmacological effects corresponds to that of BDNF. Dipeptide N-phenylacetyl-glycyl-L-proline ethyl ester (GZK-111) was designed and synthesized as a linear analog of CPG. The aim of the present work was to reveal the pharmacological profile of GZK-111. Dipeptide GZK-111 was shown to metabolize into CPG in vitro and increased cell survival by 28% at concentrations of 10-7–10-6 M in a Parkinson’s disease cell model. In a model of cerebral ischemia, GZK-111, at a dose of 0.5 mg/kg, i.p., was found to have neuroprotective effects, reducing the cerebral infarct volume by 1.6 times. Similar to CPG, GZK-111, at the range 0.1–1.0 mg/kg, i.p., possessed a stereospecific antiamnesic activity. A significant anxiolytic effect was observed at a dose of 1.5 mg/kg. GZK-111, at the range 0.5–4.0 mg/kg, i.p., demonstrated analgesic activity. GZK-111, at a dose of 10 mg/kg/7 days, i.p., possessed antidepressant-like activity. So, the neuroprotective, nootropic, antihypoxic, anxiolytic, antidepressant-like, and analgesic effects of GZK-111 were revealed. Thus, GZK-111 can be considered as a pharmacologically active pro-ampakine with a BDNF-ergic mechanism of action. IntechOpen 2020-02-18 Chapter, Part Of Book https://www.intechopen.com/chapters/71098 doi:10.5772/intechopen.91192 en ISBN:978-1-83880-439-8 https://creativecommons.org/licenses/by/3.0/ https://www.intechopen.com/books/8087 ; Neuroprotection - New Approaches and Prospects |
| spellingShingle | Health Sciences Koliasnikova, Ksenia N. Povarnina, Polina Yu. Tallerova, Anna V. Firsova, Yulia N. Nikolaev, Sergei V. Antipova, Tatiana A. Nadorova, Anna V. Kolik, Larisa G. Gudasheva, Tatiana A. Seredenin, Sergei B. Glyproline Pro-Ampakine with Neuroprotective Activity |
| title | Glyproline Pro-Ampakine with Neuroprotective Activity |
| title_full | Glyproline Pro-Ampakine with Neuroprotective Activity |
| title_fullStr | Glyproline Pro-Ampakine with Neuroprotective Activity |
| title_full_unstemmed | Glyproline Pro-Ampakine with Neuroprotective Activity |
| title_short | Glyproline Pro-Ampakine with Neuroprotective Activity |
| title_sort | glyproline pro ampakine with neuroprotective activity |
| topic | Health Sciences |
| url | https://www.intechopen.com/chapters/71098 |
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