Biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a Novel Class of Potent Competitive N-methyl-?-aspartate Receptor Antagonists. II—Pharmacological characterization in Vivo

1996 ◽  
Vol 35 (6) ◽  
pp. 655-669
Author(s):  
S Urwyler
Keyword(s):  
Heptanoic Acid ◽  
Receptor Antagonists ◽  
Pharmacological Characterization ◽  
Aspartate Receptor ◽  
Methyl Aspartate ◽  
Derivatives Of

Kainic acid neurotoxicity: in vivo test of two new non-N-methyl-d-aspartate receptor antagonists

1991 ◽  
Vol 81 (3) ◽  
pp. 255-260 ◽  
Author(s):  
M. Berg ◽  
T. Bruhn ◽  
F. F. Johansen ◽  
P. Krogsgaard-Larsen ◽  
N. H. Diemer
Keyword(s):  
Kainic Acid ◽  
Receptor Antagonists ◽  
In Vivo Test ◽  
Aspartate Receptor

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

2021 ◽  
Author(s):  
Agnieszka Jankowska ◽  
Grzegorz Satała ◽  
Artur Świerczek ◽  
Krzysztof Pociecha ◽  
Anna Partyka ◽  
...  
Keyword(s):  
Antidepressant Drugs ◽  
Antidepressant Activity ◽  
Functional Profile ◽  
Receptor Antagonists ◽  
Receptor Affinity ◽  
New Class ◽  
Amide Derivatives ◽  
Derivatives Of

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.

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