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Transient receptor potential vanilloid type 1 antagonists: a patent review (2011-2014)

Title
Transient receptor potential vanilloid type 1 antagonists: a patent review (2011-2014)
Authors
Lee, YoonjiHong, SunhyeCui, MinghuaSharma, Pankaz K.Lee, JeewooChoi, Sun
Ewha Authors
최선Pankaz Kumar Sharma
SCOPUS Author ID
최선scopus
Issue Date
2015
Journal Title
EXPERT OPINION ON THERAPEUTIC PATENTS
ISSN
1354-3776JCR Link1744-7674JCR Link
Citation
vol. 25, no. 3, pp. 291 - 318
Keywords
capsaicintransient receptor potentialTRPV1TRPV1 antagonistvanilloidVR1VR1 antagonist
Publisher
INFORMA HEALTHCARE
Indexed
SCIE; SCOPUS WOS scopus
Abstract
Introduction: Transient receptor potential vanilloid type 1 (TRPV1) is a nonselective cation channel that can be activated by noxious heat, low pH and vanilloid compounds such as capsaicin. Since TRPV1 acts as an integrator of painful stimuli, TRPV1 antagonists can be used as promising therapeutics for new types of analgesics. Areas covered: This review article covers the patents that claim TRPV1 antagonists and were published during 2011 - 2014. The patent evaluation is organized according to the applicant companies, and the representative chemical entities with important in vitro and in vivo data are summarized. Expert opinion: Many pharmaceutical companies showed promising results in the discovery of potent small molecule TRPV1 antagonists, and recently, a number of small molecule TRPV1 antagonists have been advanced into clinical trials. Unfortunately, several candidate molecules showed critical side effects such as hyperthermia and impaired noxious heat sensation in humans, leading to their withdrawal from clinical trials. Some TRPV1 antagonists patented in recent years (2011 - 2014) overcame these undesirable side effects, making the development of TRPV1 antagonists much more promising.
DOI
10.1517/13543776.2015.1008449
Appears in Collections:
약학대학 > 약학과 > Journal papers
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