Chemical Name:N,N''-1,4-Butanediylbis[N'-(3-isothiocyanatophenyl)thio
urea
Biological Activity:
Selective
antagonist of P2Y6 nucleotide receptors; IC50 values are
37 and 98 nM at human and rat P2Y6 receptors respectively. Displays
no activity at P2Y1, P2Y2, P2Y4 and P2Y11
receptors (IC50 > 10 μM). Inhibits agonist-induced
cardiomyocyte contraction and UDP-induced phagocytosis.
Mamedovaet al (2004) Diisothiocyanate
derivatives as potent, insurmountable antagonists of P2Y6 nucleotide
receptors. Biochem.Pharmacol. 67 1763. Wihlborget
al (2006) Positive inotropic effects by uridine triphosphate (UTP) and
uridine diphosphate (UDP) via P2Y2 and P2Y6 receptors on
cardiomyocytes and release of UTP in man during myocardial infarction.
Circ.Res. 98 970. Koizumiet al (2007) UDP acting
at P2Y6 receptors is a mediator of microglial phagocytosis. Nature 446
1091.
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