FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2011052392> ?p ?o ?g. }

• W2011052392 endingPage "635" @default.
• W2011052392 startingPage "620" @default.
• W2011052392 abstract "1. SB-706375 potently inhibited [(125)I]hU-II binding to both mammalian recombinant and 'native' UT receptors (K(i) 4.7+/-1.5 to 20.7+/-3.6 nM at rodent, feline and primate recombinant UT receptors and K(i) 5.4+/-0.4 nM at the endogenous UT receptor in SJRH30 cells). 2. Prior exposure to SB-706375 (1 microM, 30 min) did not alter [(125)I]hU-II binding affinity or density in recombinant cells (K(D) 3.1+/-0.4 vs 5.8+/-0.9 nM and B(max) 3.1+/-1.0 vs 2.8+/-0.8 pmol mg(-1)) consistent with a reversible mode of action. 3. The novel, nonpeptidic radioligand [(3)H]SB-657510, a close analogue of SB-706375, bound to the monkey UT receptor (K(D) 2.6+/-0.4 nM, B(max) 0.86+/-0.12 pmol mg(-1)) in a manner that was inhibited by both U-II isopeptides and SB-706375 (K(i) 4.6+/-1.4 to 17.6+/-5.4 nM) consistent with the sulphonamides and native U-II ligands sharing a common UT receptor binding domain. 4. SB-706375 was a potent, competitive hU-II antagonist across species with pK(b) 7.29-8.00 in HEK293-UT receptor cells (inhibition of [Ca(2+)](i)-mobilization) and pK(b) 7.47 in rat isolated aorta (inhibition of contraction). SB-706375 also reversed tone established in the rat aorta by prior exposure to hU-II (K(app) approximately 20 nM). 5. SB-706375 was a selective U-II antagonist with >/=100-fold selectivity for the human UT receptor compared to 86 distinct receptors, ion channels, enzymes, transporters and nuclear hormones (K(i)/IC(50)>1 microM). Accordingly, the contractile responses induced in isolated aortae by KCl, phenylephrine, angiotensin II and endothelin-1 were unaltered by SB-706375 (1 microM). 6. In summary, SB-706375 is a high-affinity, surmountable, reversible and selective nonpeptide UT receptor antagonist with cross-species activity that will assist in delineating the pathophysiological actions of U-II in mammals." @default.
• W2011052392 created "2016-06-24" @default.
• W2011052392 creator A5001032088 @default.
• W2011052392 creator A5001512555 @default.
• W2011052392 creator A5007588400 @default.
• W2011052392 creator A5013412756 @default.
• W2011052392 creator A5018150065 @default.
• W2011052392 creator A5027525741 @default.
• W2011052392 creator A5035407065 @default.
• W2011052392 creator A5035411478 @default.
• W2011052392 creator A5035647861 @default.
• W2011052392 creator A5035875588 @default.
• W2011052392 creator A5038388236 @default.
• W2011052392 creator A5039193921 @default.
• W2011052392 creator A5042569093 @default.
• W2011052392 creator A5054882579 @default.
• W2011052392 creator A5058671887 @default.
• W2011052392 creator A5074268467 @default.
• W2011052392 creator A5076874505 @default.
• W2011052392 creator A5078464253 @default.
• W2011052392 creator A5080711925 @default.
• W2011052392 creator A5081760153 @default.
• W2011052392 creator A5081970999 @default.
• W2011052392 creator A5083223367 @default.
• W2011052392 creator A5090468389 @default.
• W2011052392 date "2005-07-01" @default.
• W2011052392 modified "2023-10-17" @default.
• W2011052392 title "Nonpeptidic urotensin-II receptor antagonists I: <i>in vitro</i> pharmacological characterization of SB-706375" @default.
• W2011052392 cites W1507859731 @default.
• W2011052392 cites W1597722293 @default.
• W2011052392 cites W1968724435 @default.
• W2011052392 cites W1974828530 @default.
• W2011052392 cites W1981391899 @default.
• W2011052392 cites W1983991419 @default.
• W2011052392 cites W1993826928 @default.
• W2011052392 cites W2006120517 @default.
• W2011052392 cites W2008284738 @default.
• W2011052392 cites W2014239850 @default.
• W2011052392 cites W2014696604 @default.
• W2011052392 cites W2020075835 @default.
• W2011052392 cites W2021207107 @default.
• W2011052392 cites W2027724929 @default.
• W2011052392 cites W2035641803 @default.
• W2011052392 cites W2040043565 @default.
• W2011052392 cites W2041083376 @default.
• W2011052392 cites W2041736813 @default.
• W2011052392 cites W2043040253 @default.
• W2011052392 cites W2045780777 @default.
• W2011052392 cites W2045988967 @default.
• W2011052392 cites W2046945670 @default.
• W2011052392 cites W2048231167 @default.
• W2011052392 cites W2049784193 @default.
• W2011052392 cites W2054867528 @default.
• W2011052392 cites W2056735945 @default.
• W2011052392 cites W2062412518 @default.
• W2011052392 cites W2063808488 @default.
• W2011052392 cites W2063891666 @default.
• W2011052392 cites W2071370565 @default.
• W2011052392 cites W2072551075 @default.
• W2011052392 cites W2074631079 @default.
• W2011052392 cites W2074745209 @default.
• W2011052392 cites W2075600010 @default.
• W2011052392 cites W2075733166 @default.
• W2011052392 cites W2082712185 @default.
• W2011052392 cites W2084029889 @default.
• W2011052392 cites W2085855801 @default.
• W2011052392 cites W2087111011 @default.
• W2011052392 cites W2089541370 @default.
• W2011052392 cites W2094592279 @default.
• W2011052392 cites W2097603877 @default.
• W2011052392 cites W2102970261 @default.
• W2011052392 cites W2110937370 @default.
• W2011052392 cites W2111985967 @default.
• W2011052392 cites W2123161719 @default.
• W2011052392 cites W2125361242 @default.
• W2011052392 cites W2130246742 @default.
• W2011052392 cites W2130943352 @default.
• W2011052392 cites W2135813820 @default.
• W2011052392 cites W2139136350 @default.
• W2011052392 cites W2140228755 @default.
• W2011052392 cites W2145043050 @default.
• W2011052392 cites W2145070360 @default.
• W2011052392 cites W2149322442 @default.
• W2011052392 cites W2150898245 @default.
• W2011052392 cites W2152996717 @default.
• W2011052392 cites W2157815513 @default.
• W2011052392 cites W2411430241 @default.
• W2011052392 cites W4240447811 @default.
• W2011052392 cites W4241616013 @default.
• W2011052392 doi "https://doi.org/10.1038/sj.bjp.0706229" @default.
• W2011052392 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1576177" @default.
• W2011052392 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15852036" @default.
• W2011052392 hasPublicationYear "2005" @default.
• W2011052392 type Work @default.
• W2011052392 sameAs 2011052392 @default.
• W2011052392 citedByCount "52" @default.
• W2011052392 countsByYear W20110523922012 @default.
• W2011052392 countsByYear W20110523922013 @default.

• next