Projects funded by the NCN

Information on the principal investigator and host institution

Information of the project and the call

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Dual histamine H3 and sigma-1 receptor ligands as novel pharmacological tools in the treatment of central nervous system disorders with the focus on neuropathic pain

2020/36/C/NZ7/00284

Keywords:

histamine H3 receptors sigma-1 receptors neuropathic pain polypharmacology

Descriptors:

  • NZ7_014:

Panel:

NZ7 - Diagnostic tools, therapies and public health: public health, epidemiology, environmental health risks and occupational medicine, medical ethics, drug discovery and therapies, pharmacology

Host institution :

Instytut Farmakologii im. Jerzego Maja Polskiej Akademii Nauk

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

Katarzyna Anna Szczepańska 

Number of co-investigators in the project: 3

Call: SONATINA 4 - announced on 2019-12-16

Amount awarded: 1 081 987 PLN

Project start date (Y-m-d): 2020-09-10

Project end date (Y-m-d): 2024-09-09

Project duration:: 48 months (the same as in the proposal)

Project status: Project completed

Project description

Download the project description in a pdf file

Note - project descriptions were prepared by the authors of the applications themselves and placed in the system in an unchanged form.

Information in the final report

  • Publication in academic press/journals (6)
  1. Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent
    Authors:
    Szczepańska K, Pockes S, Podlewska S, Höring C, Mika K, Latacz G, Bednarski M, Siwek A, Karcz T, Nagl M, Bresinsky M, Mönnich D, Seibel U, Kuder KJ, Kotańska M, Stark H, Elz S, Kieć-Kononowicz K
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2021, tom: 213, strony: 113041), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2020.113041 - link to the publication
  2. Oxypiperidine Ethers as Multiple Targeting Ligands at Histamine H3 Receptors and Cholinesterases
    Authors:
    Michalska B, Dzięgielewski M, Godyń J, Werner T, Bajda M, Karcz T, Szczepańska K, Stark H, Więckowska A, Walczyński K, Staszewski M
    Academic press:
    ACS Chemical Neuroscience (rok: 2024, tom: XXXX, XXX, XXX-XXX, strony: XXXX, XXX, XXX-XXX), Wydawca: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acschemneuro.3c00800 - link to the publication
  3. Novel object recognition test as an alternative approach to assessing the pharmacological profile of sigma-1 receptor ligands
    Authors:
    Szczepańska K, Bojarski AJ, Popik P, Malikowska-Racia N
    Academic press:
    Pharmacological Reports (rok: 2023, tom: 75(5), strony: 1291-1298), Wydawca: Springer Link
    Status:
    Published
    DOI:
    10.1007/s43440-023-00516-x - link to the publication
  4. Structural and Molecular Insight into Piperazine and Piperidine Derivatives as Histamine H3 and Sigma-1 Receptor Antagonists with Promising Antinociceptive Properties
    Authors:
    Szczepańska K, Podlewska S, Dichiara M, Gentile D, Patamia V, Rosier N, Mönnich D, Ruiz Cantero MC, Karcz T, Łażewska D, Siwek A, Pockes S, Cobos EJ, Marrazzo A, Stark H, Rescifina A, Bojarski AJ, Amata E, Kieć-Kononowicz K
    Academic press:
    ACS Chemical Neuroscience (rok: 2022, tom: 13, strony: 45672), Wydawca: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acschemneuro.1c00435 - link to the publication
  5. Dual Piperidine-Based Histamine H3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain
    Authors:
    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, Kieć-Kononowicz K
    Academic press:
    Journal of Medicinal Chemistry (rok: 2023, tom: 66(14), strony: 9658-9683), Wydawca: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.3c00430 - link to the publication
  6. Efficacy of the Multi-Target Compound E153 in Relieving Pain and Pruritus of Different Origins
    Authors:
    Mogilski S, Kubacka M, Świerczek A, Wyska E, Szczepańska K, Sapa J, Kieć-Kononowicz K, Łażewska D
    Academic press:
    Pharmaceuticals (rok: 2023, tom: 16(10), strony: 1481), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/ph16101481 - link to the publication

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