Structural Requirements for Modulating 4-Benzylpiperidine Carboxamides from Serotonin/Norepinephrine Reuptake Inhibitors to Triple Reuptake Inhibitors

Overview

Journal Biomol Ther (Seoul)

Specialty Pharmacology

Date 2021 May 31

PMID 34053940

Citations 2

Authors

Suresh Paudel

Eunae Kim

Anlin Zhu

Srijan Acharya

Xiao Min

Seung Hoon Cheon

Kyeong-Man Kim

Affiliations

Soon will be listed here.

Abstract

8k: bound tightly to the binding pocket of all three monoamine reuptake transporters; however.

7j: showed poor docking with DAT. Co-expression of DAT with the dopamine D receptor (DR) significantly inhibited DA-induced endocytosis of DR probably by reuptaking DA into the cells. Pretreatment of the cells with.

8f: , which is one of the compounds with good inhibitory activity on DAT, blocked DAT-induced inhibition of DR endocytosis. In summary, this study identified critical structural features contributing to the selectivity of a molecule for each of the monoamine transporters, critical residues on the compounds that bound to the transporters, and the functional role of a DA reuptake inhibitor in regulating DR function.

Citing Articles

Discovery and Development of Monoamine Transporter Ligands.

Aggarwal S, Mortensen O Adv Neurobiol. 2023; 30:101-129.

PMID: 36928847 PMC: 10074400. DOI: 10.1007/978-3-031-21054-9_4.

Design, Synthesis, and Functional Evaluation of 1, 5-Disubstituted Tetrazoles as Monoamine Neurotransmitter Reuptake Inhibitors.

Paudel S, Wang S, Kim E, Kundu D, Min X, Shin C Biomol Ther (Seoul). 2021; 30(2):191-202.

PMID: 34789584 PMC: 8902459. DOI: 10.4062/biomolther.2021.119.

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