Table 1.
In Vitro Pharmacological Data for Antagonism of Turkey Erythrocyte P2Y1 Receptors, Indicated by the Inhibition of PLC Stimulation Elicited by 30 nM 2-MeSADP, for at Least Three Separate Determinations. “P” = Phosphate
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Compound | R = | R′ = | Antagonist Effect,a % of max. | IC50, μM (n = 3, unless noted) |
5 |
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Cl | 100 | 4.56 ± 1.38 |
6 |
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H | 100 | 1.09 ± 0.51 |
7 |
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Cl | 100 | 0.48 ±0.13 |
8 |
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Cl | 68 ±7 | 22.6+ 14.6 |
9 |
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Cl | 78 ±7 | 31 + 11 |
10 |
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Cl | 65 ±8 | 37.6 + 12.6 |
11 |
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Cl | 100 | 0.23 ±0.10 |
3 |
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H | 100 | 1.60 ± 0.47 |
4 |
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Cl | 99 ± 1 | 0.84 ±0.13 |
12 |
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Cl | 100 | 2.04 ± 0.94 (4) |
13 |
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Cl | 100 | 7.86 ±3.13 |
14 |
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Cl | 100 | 1.47 ± 0.43 |
15 |
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Cl | 100 | 2.10 ±0.97 |
16 |
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Cl | 100 | 1.74 ± 0.80 |
17 |
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Cl | 100 | 2.17 ±0.85 |
18 |
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Cl | 100 | 2.70 ± 0.66 |
19 |
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Cl | 100 | 2.36 ± 0.63 |
20 |
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Cl | 100 | 1.90 ±0.24 |
At 100 μM, none of the acyclic adenosine bisphosphate nucleotide analogues displayed agonist activity at the P2Y1 receptor in turkey erythrocyte membranes.