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11 results on '"Nichugovskaya A"'

2. Discovery of Trace Amine-Associated Receptor 1 (TAAR1) Agonist 2-(5-(4′-Chloro-[1,1′-biphenyl]-4-yl)-4H-1,2,4-triazol-3-yl)ethan-1-amine (LK00764) for the Treatment of Psychotic Disorders

Author

Mikhail Krasavin, Alexey Lukin, Ilya Sukhanov, Andrey S. Gerasimov, Savelii Kuvarzin, Evgeniya V. Efimova, Mariia Dorofeikova, Anna Nichugovskaya, Andrey Matveev, Kirill Onokhin, Konstantin Zakharov, Maxim Gureev, and Raul R. Gainetdinov

Subjects
schizophrenia, trace amine-associated receptor 1, agonism, 1,2,4-triazoles, dopamine transporter knockout rats, dopamine, Microbiology, QR1-502
Abstract

A focused in-house library of about 1000 compounds comprising various heterocyclic motifs in combination with structural fragments similar to β-phenylethylamine or tyramine was screened for the agonistic activity towards trace amine-associated receptor 1 (TAAR1). The screening yielded two closely related hits displaying EC50 values in the upper submicromolar range. Extensive analog synthesis and testing for TAAR1 agonism in a BRET-based cellular assay identified compound 62 (LK00764) with EC50 = 4.0 nM. The compound demonstrated notable efficacy in such schizophrenia-related in vivo tests as MK-801-induced hyperactivity and spontaneous activity in rats, locomotor hyperactivity of dopamine transporter knockout (DAT-KO) rats, and stress-induced hyperthermia (i.p. administration). Further preclinical studies are necessary to evaluate efficacy, safety and tolerability of this potent TAAR1 agonist for the potential development of this compound as a new pharmacotherapy option for schizophrenia and other psychiatric disorders.

Published
2022
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4. Discovery of Trace Amine-Associated Receptor 1 (TAAR1) Agonist 2-(5-(4′-Chloro-[1,1′-biphenyl]-4-yl)-4H-1,2,4-triazol-3-yl)ethan-1-amine (LK00764) for the Treatment of Psychotic Disorders

Author

Krasavin, Mikhail, primary, Lukin, Alexey, additional, Sukhanov, Ilya, additional, Gerasimov, Andrey S., additional, Kuvarzin, Savelii, additional, Efimova, Evgeniya V., additional, Dorofeikova, Mariia, additional, Nichugovskaya, Anna, additional, Matveev, Andrey, additional, Onokhin, Kirill, additional, Zakharov, Konstantin, additional, Gureev, Maxim, additional, and Gainetdinov, Raul R., additional

Published
2022
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5. Dielectric Characteristics of a Silica–Water Nanocomposite

Author

O. V. Rogazinskaya, S. D. Milovidova, B. M. Darinskii, and E. S. Nichugovskaya

Subjects
010302 applied physics, Nanocomposite, Materials science, 010308 nuclear & particles physics, Nanoporous, Composite number, General Physics and Astronomy, Humidity, Dielectric, 01 natural sciences, Amorphous solid, Nanopore, Chemical engineering, 0103 physical sciences, Molecule
Abstract

The dielectric properties of an amorphous nanoporous silica/water composite are studied. The dielectric constant of SiO2 is shown to rise from 10 (for a pretreated sample) to 105 upon raising humidity to ~80%. The results demonstrate the possibility of obtaining a superparaelectric state of water molecules in silica nanopores.

Published
2019

11. Discovery of Trace Amine Associated Receptor 1 (TAAR1) Agonist 2-(5-(4'-Chloro-[1,1'-biphenyl]-4-yl)-4 H -1,2,4-triazol-3-yl)ethan-1-amine (LK00764) for the Treatment of Psychotic Disorders.

Author

Krasavin M, Lukin A, Sukhanov I, Gerasimov AS, Kuvarzin S, Efimova EV, Dorofeikova M, Nichugovskaya A, Matveev A, Onokhin K, Zakharov K, Gureev M, and Gainetdinov RR

Subjects
Animals, Rats, Biphenyl Compounds, Receptors, G-Protein-Coupled agonists, Psychotic Disorders
Abstract

A focused in-house library of about 1000 compounds comprising various heterocyclic motifs in combination with structural fragments similar to β-phenethylamine (PEA) or tyramine was screened for the agonistic activity towards trace amine-associated receptor 1 (TAAR1). The screening yielded two closely related hits displaying EC50 values in the upper submicromolar range. Extensive analog synthesis and testing for TAAR1 agonism in a BRET-based cellular assay identified compound 62 (LK00764) with EC 50 = 4.0 nM. The compound demonstrated notable efficacy in such schizophrenia-related in vivo tests as MK-801-induced hyperactivity and spontaneous activity in rats, locomotor hyperactivity of dopamine transporter knockout (DAT-KO) rats, and stress-induced hyperthermia (i.p. administration). Further preclinical studies are necessary to evaluate efficacy, safety and tolerability of this potent TAAR1 agonist for the potential development of this compound as a new pharmacotherapy option for schizophrenia and other psychiatric disorders.

Published
2022
Full Text
View/download PDF

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