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On Benzofuroindole Analogues as Smooth Muscle Relaxants
Joint Authors
dela Peña, Ike
Cheong, Jae Hoon
Source
Journal of Biomedicine and Biotechnology
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-7, 7 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2011-09-20
Country of Publication
Egypt
No. of Pages
7
Main Subjects
Abstract EN
At least two laboratories have independently reported the synthesis of benzofuroindole compounds having potential therapeutic implications in many disease states including those that involve smooth muscle hyperactivity.
Through a series of in vitro screenings, they demonstrated the efficacy (and selectivity) of these compounds to potentiate large conductance calcium- (Ca2+-) activated K+ (BKCa) channels, by far, the most characterized of all Ca2+-dependent K+ channels.
Interestingly, promising benzofuroindole derivatives such as compound 7 (10H-benzo[4,5]furo[3,2-b]indole) and compound 22 (4-chloro-7-trifluoromethyl-10H-benzo[4,5]furo[3,2-b]indole-1-carboxylic acid) both exhibited high bladder (versus aorta) selectivity, making them attractive alternative treatments for bladder overactivity.
In recent reports, compound 22 (LDD175 or TBIC) also showed inhibition of ileum and uterine contractions, indicating multiple target tissues, which is not surprising as BKCa channels are ubiquitously expressed in the animal and human tissues.
In this paper, the authors discuss the value of benzofuroindole compounds and the challenges that need to be overcome if they were considered as smooth muscle relaxants.
American Psychological Association (APA)
dela Peña, Ike& Cheong, Jae Hoon. 2011. On Benzofuroindole Analogues as Smooth Muscle Relaxants. Journal of Biomedicine and Biotechnology،Vol. 2011, no. 2011, pp.1-7.
https://search.emarefa.net/detail/BIM-468193
Modern Language Association (MLA)
dela Peña, Ike& Cheong, Jae Hoon. On Benzofuroindole Analogues as Smooth Muscle Relaxants. Journal of Biomedicine and Biotechnology No. 2011 (2011), pp.1-7.
https://search.emarefa.net/detail/BIM-468193
American Medical Association (AMA)
dela Peña, Ike& Cheong, Jae Hoon. On Benzofuroindole Analogues as Smooth Muscle Relaxants. Journal of Biomedicine and Biotechnology. 2011. Vol. 2011, no. 2011, pp.1-7.
https://search.emarefa.net/detail/BIM-468193
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-468193