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Your search keyword '"Pilarski Bogusław"' showing total 8 results
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8 results on '"Pilarski Bogusław"'

4. Dual Piperidine-Based Histamine H3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain

Author

Szczepańska, Katarzyna, primary, Karcz, Tadeusz, additional, Dichiara, Maria, additional, Mogilski, Szczepan, additional, Kalinowska-Tłuścik, Justyna, additional, Pilarski, Bogusław, additional, Leniak, Arkadiusz, additional, Pietruś, Wojciech, additional, Podlewska, Sabina, additional, Popiołek-Barczyk, Katarzyna, additional, Humphrys, Laura J., additional, Ruiz-Cantero, M. Carmen, additional, Reiner-Link, David, additional, Leitzbach, Luisa, additional, Łażewska, Dorota, additional, Pockes, Steffen, additional, Górka, Michał, additional, Zmysłowski, Adam, additional, Calmels, Thierry, additional, Cobos, Enrique J., additional, Marrazzo, Agostino, additional, Stark, Holger, additional, Bojarski, Andrzej J., additional, Amata, Emanuele, additional, and Kieć-Kononowicz, Katarzyna, additional

Published
2023
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5. Dual Piperidine-Based Histamine H3 and Sigma‑1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.

Author

Szczepańska, Katarzyna, Karcz, Tadeusz, Dichiara, Maria, Mogilski, Szczepan, Kalinowska-Tłuścik, Justyna, Pilarski, Bogusław, Leniak, Arkadiusz, Pietruś, Wojciech, Podlewska, Sabina, Popiołek-Barczyk, Katarzyna, Humphrys, Laura J., Ruiz-Cantero, M. Carmen, Reiner-Link, David, Leitzbach, Luisa, Łażewska, Dorota, Pockes, Steffen, Górka, Michał, Zmysłowski, Adam, Calmels, Thierry, and Cobos, Enrique J.

Published
2023
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7. Dual Piperidine-Based Histamine H3and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain

Author

Szczepańska, Katarzyna, Karcz, Tadeusz, Dichiara, Maria, Mogilski, Szczepan, Kalinowska-Tłuścik, Justyna, Pilarski, Bogusław, Leniak, Arkadiusz, Pietruś, Wojciech, Podlewska, Sabina, Popiołek-Barczyk, Katarzyna, Humphrys, Laura J., Ruiz-Cantero, M. Carmen, Reiner-Link, David, Leitzbach, Luisa, Łażewska, Dorota, Pockes, Steffen, Górka, Michał, Zmysłowski, Adam, Calmels, Thierry, Cobos, Enrique J., Marrazzo, Agostino, Stark, Holger, Bojarski, Andrzej J., Amata, Emanuele, and Kieć-Kononowicz, Katarzyna

Abstract

In search of new dual-acting histamine H3/sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active in vivoligands previously studied and described by our team. However, we kept in mind that within the previous series, a pair of closely related compounds, KSK67and KSK68, differing only in the piperazine/piperidine moiety in the structural core showed a significantly different affinity at sigma-1 receptors (σ1Rs). Therefore, we first focused on an in-depth analysis of the protonation states of piperazine and piperidine derivatives in the studied compounds. In a series of 16 new ligands, mainly based on the piperidine core, we selected three lead structures (3, 7, and 12) for further biological evaluation. Compound 12showed a broad spectrum of analgesic activity in both nociceptive and neuropathic pain models based on the novel molecular mechanism.

Published
2023
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8. Dual Piperidine-Based Histamine H 3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.

Author

Szczepańska K, Karcz T, Dichiara M, Mogilski S, Kalinowska-Tłuścik J, Pilarski B, Leniak A, Pietruś W, Podlewska S, Popiołek-Barczyk K, Humphrys LJ, Ruiz-Cantero MC, Reiner-Link D, Leitzbach L, Łażewska D, Pockes S, Górka M, Zmysłowski A, Calmels T, Cobos EJ, Marrazzo A, Stark H, Bojarski AJ, Amata E, and Kieć-Kononowicz K

Subjects
Humans, Histamine, Ligands, Nociception, Piperazine, Piperidines pharmacology, Piperidines therapeutic use, Piperidines chemistry, Structure-Activity Relationship, Sigma-1 Receptor, Receptors, Histamine H3 chemistry, Receptors, sigma, Neuralgia drug therapy
Abstract

In search of new dual-acting histamine H 3 /sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active in vivo ligands previously studied and described by our team. However, we kept in mind that within the previous series, a pair of closely related compounds, KSK67 and KSK68 , differing only in the piperazine/piperidine moiety in the structural core showed a significantly different affinity at sigma-1 receptors (σ 1 Rs). Therefore, we first focused on an in-depth analysis of the protonation states of piperazine and piperidine derivatives in the studied compounds. In a series of 16 new ligands, mainly based on the piperidine core, we selected three lead structures ( 3 , 7 , and 12 ) for further biological evaluation. Compound 12 showed a broad spectrum of analgesic activity in both nociceptive and neuropathic pain models based on the novel molecular mechanism.

Published
2023
Full Text
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