%0 Journal Article
%A Jung, Kwan-Young
%A Moon, Hyoun Duk
%A Lee, Ga Eun
%A Lim, Hyun-Ho
%A Park, Chul-Seung
%A Kim, Yong-Chul
%D 2007
%T Structure−Activity Relationship Studies of Spinorphin as a Potent and Selective Human P2X3
Receptor Antagonist
%U https://acs.figshare.com/articles/journal_contribution/Structure_Activity_Relationship_Studies_of_Spinorphin_as_a_Potent_and_Selective_Human_P2X_sub_3_sub_Receptor_Antagonist/2986693
%R 10.1021/jm070114m.s001
%2 https://acs.figshare.com/ndownloader/files/4687375
%K Single alanine substitutions
%K alanine substitution
%K agonistic activity
%K cyclic form
%K 8.3 pM
%K Selective Human P 2X Receptor AntagonistSpinorphin
%K P 2X receptors
%K LVVYPWT
%K P 2X receptor
%K 1 st
%K IC 50
%K Xenopus oocytes
%K antinociceptive peptide
%X 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.
%I ACS Publications