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Information on the principal investigator and host institution

Information of the project and the call

Keywords

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Functionalized amino acids - inibitors of GABA uptake with antianalgetic activity

2014/15/B/NZ7/00930

Keywords:

functionalized amino acids GABA uptake inhibitors neuropathic pain

Descriptors:

  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology
  • ST5_16:

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 :

Uniwersytet Jagielloński - Collegium Medicum, Collegium Medicum, Wydział Farmaceutyczny

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

dr Paula Zaręba 

Number of co-investigators in the project: 8

Call: OPUS 8 - announced on 2014-09-15

Amount awarded: 691 943 PLN

Project start date (Y-m-d): 2015-07-13

Project end date (Y-m-d): 2020-12-12

Project duration:: 65 months (the same as in the proposal)

Project status: Project settled

Equipment purchased [PL]

  1. -.
  2. Wyparka rotacyjna z systemem próżniowym, pokrywą ochonną, łaźnią oraz termostatem cyrkulacynym (55 000 PLN)
  3. Chłodziarka zanurzeniowa (30 000 PLN)
  4. Homogenizator ultradźwiękowy (30 000 PLN)
  5. Analgezymetr do pomiaru bólu spontanicznego (32 000 PLN)
  6. Liofilizator wraz z pompą.

Information in the final report

  • Publication in academic press/journals (7)
  • Articles in post-conference publications (2)
  1. Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity
    Authors:
    Paula Zaręba, Kinga Sałat, Georg C. Höfner, Kamil Łątka, Marek Bajda, Gniewomir Latacz, Krzysztof Kotniewicz, Anna Rapacz, Adrian Podkowa, Maciej Maj, Krzysztof Jóźwiak, Barbara Filipek, Klaus T. Wanner, Barbara Malawska, Katarzyna Kulig
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2020, tom: 221, strony: 113512), Wydawca: Elsevier
    Status:
    Published
    DOI:
    brak - link to the publication
  2. Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice
    Authors:
    Paula Zaręba, Beata Gryzło, Katarzyna Malawska, Kinga Sałata, Georg C. Höfner, Alicja Nowaczyk, Łukasz Fijałkowski, Anna Rapacz, Adrian Podkowa, Anna Furgała, Paweł Żmudzki, Klaus T. Wanner, Barbara Malawska, Katarzyna Kulig
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2020, tom: 188, strony: 111920), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2019.111920 - link to the publication
  3. Development, recent achievements and current directions of research into GABA uptake inhibitors
    Authors:
    Paula Zaręba, Beata Gryzło, Gabriela Mazur, Barbara Malawska
    Academic press:
    Current Medicinal Chemistry (rok: 2021, tom: 28, strony: 750-776), Wydawca: BenthamScience
    Status:
    Published
    DOI:
    10.2174/0929867325666191010120236 - link to the publication
  4. Novel functionalized amino acids as inhibitors of GABA transporters with analgesic activity
    Authors:
    Gryzło Beata; Zaręba Paula; Malawska Katarzyna; Mazur Gabriela; Rapacz Anna; Łątka Kamil; Höfner Georg; Sałat Kinga; Latacz Gniewomir; Bajda Marek; Wanner Klaus; Malawska Barbara; Kulig Katarzyna
    Academic press:
    ACS Chemical Neuroscience (rok: 2021, tom: brak danych, strony: brak danych), Wydawca: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acschemneuro.1c00351 - link to the publication
  5. Docking and pharmacodynamic studies on hGAT1 inhibition activity in the presence of selected neuronal and astrocytic inhibitors. Part I.
    Authors:
    Nowaczyk A, Fijałkowski Ł, Zaręba P, Sałat K
    Academic press:
    Journal of Molecular Graphics and Modelling (rok: 2018, tom: 85, strony: 171-181), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.jmgm.2018.09.003 - link to the publication
  6. Studies on the Activity of Selected Highly Lipophilic Compounds toward hGAT1 Inhibition. Part II.
    Authors:
    Nowaczyk A, Fijałkowski Ł, Kowalska M, Podkowa A, Sałat K
    Academic press:
    ACS Chemical Neuroscience (rok: 2019, tom: 10 (1), strony: 337–347), Wydawca: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acschemneuro.8b00282 - link to the publication
  7. Experimental Drugs for Neuropathic Pain
    Authors:
    Salat K, Gryzlo B, Kulig K
    Academic press:
    Current Neuropharmacology (rok: 2018, tom: 16(8), strony: 1193-1209), Wydawca: Bentham Science
    Status:
    Published
    DOI:
    10.2174/1570159X16666180510151241 - link to the publication
  1. Design, synthesis and evaluation of 2-substituted derivatives of butanamides as gaba uptake inhibitors. Elucidation of the structure-activity studies.
    Authors:
    Paula Zaręba, Kinga Sałat, Georg Hoefner, Adrian Podkowa, Klaus T. Wanner, Katarzyna Kulig
    Conference:
    5th SEQT Medicinal Chemistry Summer School "Medicinal Chemistry in Drug Discovery: the Pharma Perspective" (rok: 2016, ), Wydawca: SEQT
    Data:
    konferencja 14-16.06.2016
    Status:
    Published
    DOI:
    link to the publication
  2. 4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl derivatives of N-benzylamides as mGAT3/4 inhibitors with analgesic activity
    Authors:
    Paula Zaręba, Beata Gryzło, Katarzyna Malawska, Kinga Sałat, Georg C. Höfner, Anna Rapacz, Adrian Podkowa, Anna Furgała, Klaus T. Wanner, Barbara Malawska, Katarzyna Kulig
    Conference:
    EFMC-ISMC & EFMC-YMCS Virtual Poster Session (rok: 2020, ), Wydawca: LD Organisation srl
    Data:
    konferencja 7-11.09.2020
    Status:
    Published

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