Zobrazeno 1 - 10 of 43 pro vyhledávání: '"PYRAZOLOQUINOLINONES"'
1
Akademický článek
Demystifying the Molecular Basis of Pyrazoloquinolinones Recognition at the Extracellular α1+/β3- Interface of the GABAA Receptor by Molecular Modeling
Autor: Natesh Singh, Bruno O. Villoutreix
Publikováno v: Frontiers in Pharmacology, Vol 11 (2020)
GABAA receptors are pentameric ligand-gated ion channels that serve as major inhibitory neurotransmitter receptors in the mammalian brain and the target of numerous clinically relevant drugs interacting with different ligand binding sites. Here, we r
Externí odkaz: https://doaj.org/article/a8e0ce4d1fb14490bd1d1ca893f32071
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2
Akademický článek
Overcoming the Low Oral Bioavailability of Deuterated Pyrazoloquinolinone Ligand DK-I-60-3 by Nanonization: A Knowledge-Based Approach
Autor: Jelena R. Mitrović, Branka Divović-Matović, Daniel E. Knutson, Jelena B. Đoković, Aleksandar Kremenović, Vladimir D. Dobričić, Danijela V. Randjelović, Ivana Pantelić, James M. Cook, Miroslav M. Savić, Snežana D. Savić
Publikováno v: Pharmaceutics, Vol 13, Iss 8, p 1188 (2021)
Poor water solubility of new chemical entities is considered as one of the main obstacles in drug development, as it usually leads to low bioavailability after administration. To overcome these problems, the selection of the appropriate formulation t
Externí odkaz: https://doaj.org/article/5e2a79202ef0415b9129763a243ec430
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3
Pharmacological characterization of the influence of deuteration of selected pyrazoloquinolinones as GABAA receptor modulatores
Autor: Divović-Matović, Branka
Publikováno v: Универзитет у Београду
Važno mesto u istraživanjima poslednjih godina zauzimaju GABAA receptori (GABAAR) sa α6 podjedinicom u pentamernom receptorskom kompleksu. Ovi receptori imaju potencijalno važnu ulogu u razvoju trigeminalnog orofacijalnog bola, migreni, neuropsih
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=nardusnacion::1fd70a713a113a95b1a3d1127a2102dc
http://nardus.mpn.gov.rs/bitstream/id/151232/Izvestaj_Komisije_13573.pdf
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4
Behavioural interaction of pyrazoloquinolinone positive allosteric modulators at α6GABAA receptors and diazepam in rats: Anti-diazepam-induced ataxia action as a structure-dependent feature
Autor: Branka Divović Matović, Dan Knutson, Jelena Mitrović, Vladimir Stevanović, Boban Stanojević, Snežana Savić, James M. Cook, Miroslav M. Savić
Publikováno v: Basic and Clinical Pharmacology and Toxicology
Basic & Clinical Pharmacology & Toxicology
Several pyrazoloquinolinone (PQ) ligands were recently discovered as functionally selective positive modulators at the PQ site of α6-containing GABAA receptors. PQs are also neutral modulators at the benzodiazepine site. We assessed the influence of
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f64dc87816764503b7780f333b94239
https://farfar.pharmacy.bg.ac.rs/handle/123456789/4289
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5
Akademický článek
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6
Demystifying the Molecular Basis of Pyrazoloquinolinones Recognition at the Extracellular α1+/β3- Interface of the GABAA Receptor by Molecular Modeling
Autor: Singh, Natesh, Villoutreix, Bruno O.
Publikováno v: Frontiers in Pharmacology
GABAA receptors are pentameric ligand-gated ion channels that serve as major inhibitory neurotransmitter receptors in the mammalian brain and the target of numerous clinically relevant drugs interacting with different ligand binding sites. Here, we r
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::c42e97e347b79992795f780d1abea75b
http://europepmc.org/articles/PMC7518038
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7
Nanocrystal dispersion of DK-I-56–1, a poorly soluble pyrazoloquinolinone positive modulator of α6 GABAA receptors: Formulation approach toward improved in vivo performance
Autor: Snežana Savić, Miroslav M. Savić, James M. Cook, Predrag Vulić, Vladimir Dobričić, Branka Divović, Jelena Đoković, Daniel E. Knutson, Jelena R Mitrović, Danijela Randjelovic, Bojan Čalija
Publikováno v: European Journal of Pharmaceutical Science
Eur J Pharm Sci
European Journal of Pharmaceutical Sciences
DK-I-56–1 (7‑methoxy‑2-(4‑methoxy‑d3-phenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one), a recently developed deuterated pyrazoloquinolinone, has been recognized as a lead candidate for treatment of various neuropsychiatric disorders. Du
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4814c7e74b26cb71ce3035875bdaceff
https://cer.ihtm.bg.ac.rs/handle/123456789/3635
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8
Synthesis and pharmacological evaluation of pyrazolo[4,3-c]quinolinones as high affinity GABAA-R ligands and potential anxiolytics
Autor: Elizabeth L. Moyano, Elena Anahi Bignante, Marisa Juana Lopez Rivilli, María A. Perillo, Anahi del Valle Turina, Margarita C. Briñón, Victor Hugo Cena Molina
Publikováno v: Bioorganic & Medicinal Chemistry. 26:3967-3974
The synthesis, in vitro ligand binding study and in vivo Elevated Plus Maze test (EPM) of a series of pyrazolo[4,3-c]quinolin-3-ones (PQs) are reported. Multistep synthesis of PQs started from anilines and diethyl 2-(ethoxymethylene)malonate to give
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7906d0bc6ce0559d24674a7c134cd5ca
https://doi.org/10.1016/j.bmc.2018.06.021
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9
Akademický článek
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10
Akademický článek
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