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GIST Scholar College of Life Sciences and Medical Engineering Department of Life Sciences 1. Journal Articles

Structure-Activity Relationship Studies of Spinorphin as a Potent and Selective Human P2X3 Receptor Antagonist

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Author(s)
Jung, Kwan-Young; Moon, Hyoun Duk; Lee, Ga Eun; Lim, Hyun-Ho; Park, Chul-Seung; Kim, Yong-Chul
Type
Article
Citation
ACS National Meeting Book of Abstracts, v.50, no.18, pp.4543 - 4547
Issued Date
2007-09
Abstract
Spinorphin, an endogenous antinociceptive peptide (LVVYPWT), showed potent and non-competitive antagonism at the ATP-activated human P2X3 receptor (IC50 = 8.3 pM) in a two-electrode voltage clamp assay with recombinant human P2X3 receptors expressed in Xenopus oocytes. Single alanine substitutions from 1st to 4th amino acids and the cyclic form of LVVYPWT sustained antagonistic properties at the human P2X3 receptors, whereas the threonine to alanine substitution resulted in an enhancing effect of the agonistic activity.
회의초록: 190-MEDI
Publisher
AMER CHEMICAL SOC
ISSN
0022-2623
DOI
10.1021/jm070114m
URI
https://scholar.gist.ac.kr/handle/local/17579
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