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. Author manuscript; available in PMC: 2012 Aug 7.
Published in final edited form as: Biochem Pharmacol. 2004 May 1;67(9):1763–1770. doi: 10.1016/j.bcp.2004.01.011

Table 1.

Inhibition by aryl diisothiocyanate derivatives of the activation of PLC induced by P2Y receptor agonists

Compound (MRS number) graphic file with name nihms-31400-t0007.jpg Position of NCS Percent inhibitiona
hP2Y1 hP2Y2 hP2Y4 hP2Y6 hP2Y11
4 (2568) trans-CH=CH– 4 <5 <5 <5 <5 <5
5 (2567) –CH2–CH2– 4 <5 <5 <5 95 ± 7 <5
6 (2564) –NHCSNH(CH2)2NHCSNH– 4 <5 <5 <5 77 ± 4 62 ± 4
7 (2575) –NHCSNH(CH2)3NHCSNH– 4 <5 <5 <5 96 ± 6 <5
8 (2576) –NHCSNH(CH2)4NHCSNH– 4 90 ± 5 92 ± 4 77 ± 4 78 ± 2 <5
9 (2570) –NHCSNH(CH2)2NHCSNH– 3 80 ± 4 40 <5 71 ± 10 <5
10 (2577) –NHCSNH(CH2)3NHCSNH– 3 <5 <5 98 ± 2 86 ±6 <5
11 (2578) –NHCSNH(CH2)4NHCSNH– 3 20 ± 3 <5 <5 100 ± 6 <5
a

Concentration of antagonists was 10 μM. Specific subtypes of human P2Y receptors were expressed in 1321N astrocytoma cells (hP2Y1, hP2Y2, hP2Y4, and hP2Y6) or in CHO cells (hP2Y11) [13]. Agonists used were: P2Y1, 2-MeSADP (30 nM); hP2Y2, UTP (100 nM); hP2Y4, UTP (100 nM); hP2Y6, UDP (300 nM); hP2Y11, ATP (10 μM). The concentrations of agonists used were roughly equivalent to their EC50 values. The potency (IC50 values) of MRS2567, MRS2575 and MRS2578 at both human and rat P2Y6 receptors were listed in the text.