A new class of 5-HT1A receptor antagonists with procognitive and antidepressant properties-Reference-Cited by-同舟云学术

A new class of 5-HT1A receptor antagonists with procognitive and antidepressant properties

Published:2021-09 Issue:18 Volume:13 Page:1497-1514
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Jankowska Agnieszka¹^ORCID,Satała Grzegorz²^ORCID,Świerczek Artur³^ORCID,Pociecha Krzysztof³^ORCID,Partyka Anna⁴^ORCID,Jastrzębska-Więsek Magdalena⁴^ORCID,Głuch-Lutwin Monika⁵^ORCID,Bojarski Andrzej J²^ORCID,Wyska Elżbieta³^ORCID,Chłoń-Rzepa Grażyna¹^ORCID

Affiliation:

1. Jagiellonian University Medical College, Faculty of Pharmacy, Department of Medicinal Chemistry, 9 Medyczna Street, 30-688, Kraków, Poland

2. Polish Academy of Sciences, Maj Institute of Pharmacology, Department of Medicinal Chemistry, 12 Smętna Street, 31-343, Kraków, Poland

3. Jagiellonian University Medical College, Faculty of Pharmacy, Department of Pharmacokinetics & Physical Pharmacy, 9 Medyczna Street, 30-688, Kraków, Poland

4. Jagiellonian University Medical College, Faculty of Pharmacy, Department of Clinical Pharmacy, 9 Medyczna Street, 30-688, Kraków, Poland

5. Jagiellonian University Medical College, Faculty of Pharmacy, Department of Pharmacobiology, 9 Medyczna Street, 30-688, Kraków, Poland

Abstract

Aims: 5-HT1A receptor antagonists constitute a potential group of drugs in the treatment of CNS diseases. The aim of this study was to search for new procognitive and antidepressant drugs among amide derivatives of aminoalkanoic acids with 5-HT1A receptor antagonistic properties. Materials & methods: Thirty-three amides were designed and evaluated in silico for their drug-likeness. The synthesized compounds were tested in vitro for their 5-HT1A receptor affinity and functional profile. Moreover, their selectivity over 5-HT7, 5-HT2A and D2 receptors and ability to inhibit phosphodiesterases were evaluated. Results: A selected 5-HT1A receptor antagonist 20 ( Ki = 35 nM, Kb = 4.9 nM) showed procognitive and antidepressant activity in vivo. Conclusion: Novel 5-HT1A receptor antagonists were discovered and shown as potential psychotropic drugs.

Funder

National Science Centre, Poland

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2020-0363

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