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Design, synthesis, and pharmacological evaluation of soft glycopyrrolate and its analog.

Author: BodorN, HuangF, JiF, JuhaszA, WuW

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

Glycopyrrolate is a quaternary anticholinergic drug, but it has limitations due to side effects. This study designed a soft drug, methoxycarbonylphenyl-cyclopentylacetoxy-N,N-dimethyl-3-pyrrolidinium methyl sulfate (SG), and its analog, methoxycarbonylphenylcyclopentyl-acetoxyethyl-N,N,N-trimethylammon ium methyl sulfate (SGA). These soft drugs are expected to be locally active, but systemically inactive to increase the therapeutic index. SG and SGA are anticholinergics with subtype selectivity and moderate potency, and can be used as topical antiperspirants.
Paper Details　
Original Abstract of the Article :
Glycopyrrolate is a quaternary anticholinergic drug. Like for other anticholinergics, the usefulness of this agent is limited by its side effects. In this study, based on the structure of glycopyrrolate, we designed a soft drug, methoxycarbonylphenyl-cyclopentylacetoxy-N,N-dimethyl-3-p yrrolidinium ...See full text at original site
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引用元：
https://pubmed.ncbi.nlm.nih.gov/10756538

データ提供：米国国立医学図書館（NLM）

Creating a Softer Ride with Glycopyrrolate

Glycopyrrolate, a medication used to manage certain medical conditions, can sometimes have side effects that limit its usefulness. This study aimed to design a new type of glycopyrrolate, referred to as a 'soft drug,' to minimize these unwanted effects. The researchers created two variations of glycopyrrolate, SG and SGA, with the goal of making them locally active (working at the specific site of application) but less active in the body as a whole (systemically inactive). This approach aimed to improve the therapeutic index, meaning a greater benefit with fewer side effects.

Soft Drugs: A New Frontier in Medication Design

The study found that the newly synthesized SG and SGA showed promising results. They acted as anticholinergics with subtype selectivity, meaning they targeted specific receptors in the body, reducing the likelihood of affecting other systems. Additionally, their potency was moderate, which is beneficial in minimizing potential side effects. These findings suggest that SG and SGA have the potential to be used as topical antiperspirants, addressing issues related to excessive sweating.

Navigating the Landscape of Soft Drugs

This research offers a glimpse into the future of medicine, where drugs can be designed to target specific areas of the body, reducing the risk of unwanted side effects. However, further research is needed to fully understand the long-term effects and potential applications of these 'soft drugs.'

Dr.Camel's Conclusion

This study, like a camel traversing a vast desert, takes us on a journey through the development of new medications. The researchers, driven by their quest for better treatment options, have created 'soft drugs' with the potential to improve patient outcomes by minimizing side effects. The future of medicine, much like a desert oasis, holds promise for more innovative and targeted drug therapies, offering a better path to healing.

Date :
  1. Date Completed 2000-05-03
  2. Date Revised 2015-11-19
Further Info :

Pubmed ID

10756538

DOI: Digital Object Identifier

10756538

Related Literature

Article Analysis
・Side Effects of glycopyrronium topical
SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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