Characterization and molecular basis for the block of Kv1.3 channels induced by carvedilol in HEK293 cells

Yang, Jinfeng; Neng, Cheng; Sheng, Ren; Liu, Xiangming; Li, Xiantao

doi:10.1016/j.ejphar.2018.07.025

Cited by 2 publications

(1 citation statement)

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“…Therefore, the authors postulated that carvedilol acts directly on Kv1.3 currents by inducing closed-and open-channel blocks. [178] Exposure to carvedilol in human atrial myocytes causes a considerable block of I Kur at a concentration equivalent to therapeutic plasma levels, with an IC 50 value of 0.39 μM. This drug also demonstrates a blocking effect on cloned cardiac Kv1.5 channels expressed in Chinese hamster ovary (CHO) cells, however at a slightly higher concentration (IC 50 of 2.56 μM).…”

Section: Carvedilol Potassium Channels Blockingmentioning

confidence: 99%

Multitargeting in cardioprotection: An example of biaromatic compounds

Mokrov

2023

Archiv der Pharmazie

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A multitarget drug design approach is actively developing in modern medicinal chemistry and pharmacology, especially with regard to multifactorial diseases such as cardiovascular diseases, cancer, and neurodegenerative diseases. A detailed study of many well‐known drugs developed within the single‐target approach also often reveals additional mechanisms of their real pharmacological action. One of the multitarget drug design approaches can be the identification of the basic pharmacophore models corresponding to a wide range of the required target ligands. Among such models in the group of cardioprotectors is the linked biaromatic system. This review develops the concept of a “basic pharmacophore” using the biaromatic pharmacophore of cardioprotectors as an example. It presents an analysis of possible biological targets for compounds corresponding to the biaromatic pharmacophore and an analysis of the spectrum of biological targets for the five most known and most studied cardioprotective drugs corresponding to this model, and their involvement in the biological effects of these drugs.

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Section: Carvedilol Potassium Channels Blockingmentioning

confidence: 99%