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Selectivities of dihydropyridine derivatives in blocking Ca(2+) channel subtypes expressed in Xenopus oocytes.

Author: FurukawaT, MideraT, MoriY, NukadaT, SagawaT, YamakawaT

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

This study investigated the blocking effects of 10 dihydropyridines (DHPs) on four subtypes of Ca(2+) channels. Amlodipine, benidipine, cilnidipine, nicardipine, and barnidipine were found to significantly block N-type and P/Q-type Ca(2+) channels.
Paper Details　
Original Abstract of the Article :
Some dihydropyridines (DHPs), such as amlodipine and cilnidipine, have been shown to block not only L-type but also N-type Ca(2+) channels; therefore, DHPs are no longer considered as L-type-specific Ca(2+) channel blockers. However, selectivity of DHPs for Ca(2+) channel subtypes including N-, P/Q-...See full text at original site
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引用元：
https://pubmed.ncbi.nlm.nih.gov/10525060

データ提供：米国国立医学図書館（NLM）

Understanding the Selectivity of Dihydropyridine Derivatives

Dihydropyridines (DHPs) are a class of medications commonly used to treat cardiovascular conditions. These drugs work by blocking calcium channels, which are essential for the function of heart muscle cells. However, DHPs are not just selective for one type of calcium channel, and their impact on different subtypes of calcium channels is not fully understood.

This research aims to shed light on the selectivity of DHPs for various calcium channel subtypes, including L-, N-, P/Q-, and R-types. The researchers investigated the blocking effects of ten different DHPs on these channel subtypes using a Xenopus oocyte expression system. Their findings showed that while all DHPs effectively blocked L-type channels, their selectivity for other subtypes varied considerably.

DHPs: More Than Just L-Type Blockers

The study revealed that five of the ten DHPs tested significantly blocked N-type and P/Q-type channels. This suggests that DHPs are not simply L-type-specific calcium channel blockers, as previously believed. Understanding these subtype-specific blocking actions is crucial for optimizing their therapeutic use and minimizing potential side effects.

Implications for Drug Development and Patient Care

The findings of this research have important implications for the development of new DHPs with enhanced selectivity for specific calcium channel subtypes. This could lead to more targeted treatments with fewer side effects. Additionally, the study highlights the need for clinicians to consider the potential impact of DHPs on different calcium channel subtypes when prescribing these medications.

Dr. Camel's Conclusion

The world of calcium channels can be as complex as a desert oasis, with its intricate network of interconnected pathways. This research takes us deeper into this complex world, unraveling the intricate interactions between DHPs and different calcium channel subtypes. It reminds us that understanding these nuances is crucial for ensuring effective and safe medical treatment.

Date :
  1. Date Completed 1999-11-24
  2. Date Revised 2006-11-15
Further Info :

Pubmed ID

10525060

DOI: Digital Object Identifier

10525060

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English

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