New Phenylglycinamide Derivatives with Hybrid Structure as Candidates for New Broad-Spectrum Anticonvulsants

Autor: Marcin Jakubiec, Michał Abram, Mirosław Zagaja, Marta Andres-Mach, Aleksandra Szewczyk, Gniewomir Latacz, Bartłomiej Szulczyk, Katarzyna Socała, Dorota Nieoczym, Piotr Wlaź, Cameron S. Metcalf, Karen Wilcox, Rafał M. Kamiński, Krzysztof Kamiński

Publikováno v: Cells, Vol 11, Iss 12, p 1862 (2022)

In the present study, a focused combinatorial chemistry approach was applied to merge structural fragments of well-known TRPV1 antagonists with a potent anticonvulsant lead compound, KA-104, that was previously discovered by our group. Consequently,

Externí odkaz: https://doaj.org/article/9d34a801f4aa4feab4747cefcea04a31

Beneficial Effects of Capsaicin in Disorders of the Central Nervous System

Autor: Michał Pasierski, Bartłomiej Szulczyk

Publikováno v: Molecules, Vol 27, Iss 8, p 2484 (2022)

Capsaicin is a natural compound found in chili peppers and is used in the diet of many countries. The important mechanism of action of capsaicin is its influence on TRPV1 channels in nociceptive sensory neurons. Furthermore, the beneficial effects of

Externí odkaz: https://doaj.org/article/26e87504502743f69c454d4dd2ff1c90

KA‐104, a new multitargeted anticonvulsant with potent antinociceptive activity in preclinical models

Autor: Michał Abram, Kamil Kuś, Szczepan Mogilski, Karolina Matyjaszczyk, Krzysztof Kamiński, Anna Rapacz, Bartłomiej Szulczyk, Maria Walczak, Rafał M. Kamiński, Gniewomir Latacz

Publikováno v: Epilepsia. 61:2119-2128

Objective The main objective of the present work was to assess the utility of KA-104 as potential therapy for drug-resistant seizures and neuropathic pain, and to characterize its druglike properties in a series of absorption, distribution, metabolis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::55f18909a3f37e2768c466c3216b2569
https://doi.org/10.1111/epi.16669

Identification of New Compounds with Anticonvulsant and Antinociceptive Properties in a Group of 3-substituted (2,5-dioxo-pyrrolidin-1-yl)(phenyl)-Acetamides

Autor: Michał Abram, Marcin Jakubiec, Anna Rapacz, Szczepan Mogilski, Gniewomir Latacz, Bartłomiej Szulczyk, Małgorzata Szafarz, Katarzyna Socała, Dorota Nieoczym, Elżbieta Wyska, Piotr Wlaź, Rafał M. Kamiński, Krzysztof Kamiński

Publikováno v: International Journal of Molecular Sciences
International Journal of Molecular Sciences; Volume 22; Issue 23; Pages: 13092
International Journal of Molecular Sciences, Vol 22, Iss 13092, p 13092 (2021)

We report herein a series of water-soluble analogues of previously described anticonvulsants and their detailed in vivo and in vitro characterization. The majority of these compounds demonstrated broad-spectrum anticonvulsant properties in animal sei

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03a8ea4fd73cd7e78348534ade4042ae
http://europepmc.org/articles/PMC8658016

Prefrontal cortex pyramidal neurons express functional Nav1.8 tetrodotoxin-resistant sodium currents

Autor: Maciej Gawlak, Michał Pasierski, Bartłomiej Szulczyk

Publikováno v: Clinical and experimental pharmacologyphysiologyREFERENCES. 49(3)

It has been repeatedly proved that Nav1.8 tetrodotoxin (TTX)-resistant sodium currents are expressed in peripheral sensory neurons where they play important role in nociception. There are very few publications that show the presence of TTX-resistant

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9ab408980351f04c30cc1dc67c1c395
https://pubmed.ncbi.nlm.nih.gov/34750860