Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D 3,4-dihydroquinolin-2(1)-one Derivatives Related to Aripiprazole

Overview

Journal Biomolecules

Publisher MDPI

Specialties Biochemistry
Molecular Biology

Date 2021 Sep 28

PMID 34572475

Citations 1

Authors

Radomir Juza

Kristyna Stefkova

Wim Dehaen

Alena Randakova

Tomas Petrasek

Iveta Vojtechova

Tereza Kobrlova

Lenka Pulkrabkova

Lubica Muckova

Marko Mecava

Lukas Prchal

Eva Mezeiova

Kamil Musilek

Ondrej Soukup

Jan Korabecny

Affiliations

Soon will be listed here.

Abstract

In this pilot study, a series of new 3,4-dihydroquinolin-2(1)-one derivatives as potential dopamine receptor D (DR) modulators were synthesized and evaluated in vitro. The preliminary structure-activity relationship disclosed that compound exhibited the highest DR affinity among the newly synthesized compounds. In addition, showed a very low cytotoxic profile and a high probability to cross the blood-brain barrier, which is important considering the observed affinity. However, molecular modelling simulation revealed completely different binding mode of compared to USC-D301, which might be the culprit of the reduced affinity of toward DR in comparison with USC-D301.

Citing Articles

Dopamine Dynamics and Neurobiology of Non-Response to Antipsychotics, Relevance for Treatment Resistant Schizophrenia: A Systematic Review and Critical Appraisal.

Iasevoli F, Avagliano C, DAmbrosio L, Barone A, Ciccarelli M, De Simone G Biomedicines. 2023; 11(3).

PMID: 36979877 PMC: 10046109. DOI: 10.3390/biomedicines11030895.

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