What question did this study set out to answer?

To assess the pharmacological potency and receptor selectivity of the novel ATP analogue FPL 66096 against human platelet P2T-purinoceptors and other purinoceptor subtypes.

November 1, 1994British Journal of PharmacologyOpen Access

FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T‐purinoceptors

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Authors

RHRobert G. HumphriesAstraZeneca (Brazil)WTWendy TomlinsonPharmaceutical Product Development (United States)AIAnthony H. IngallLoughborough University

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Implication

In vitro evaluation demonstrates that FPL 66096 selectively inhibits ADP-induced aggregation in human platelets, indicating its value as a selective tool for purinoceptor research.

Key Points

To assess the pharmacological potency and receptor selectivity of the novel ATP analogue FPL 66096 against human platelet P2T-purinoceptors and other purinoceptor subtypes.
Measured ADP-dependent and ADP-independent aggregation in suspensions of human washed platelets exposed to FPL 66096 (1–1000 nM).
Evaluated P2X- and P2Y-purinoceptor activity using isolated rabbit ear artery and guinea-pig aorta preparations.
FPL 66096 caused a concentration-dependent, competitive inhibition of ADP-induced human platelet aggregation with a pKB value of 8.66, having no effect on ADP-independent aggregation.
The compound acted as a weak P2X agonist (pA2 3.68) and weak P2Y antagonist (apparent pKB 4.71), demonstrating at least a 9,000-fold selectivity for the P2T subtype.

Cite This Study

Humphries et al. (1994) studied this question.

synapsesocial.com/papers/6a1c55fcbc71fb1015a96d11 https://doi.org/10.1111/j.1476-5381.1994.tb17100.x

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Implication

In vitro evaluation demonstrates that FPL 66096 selectively inhibits ADP-induced aggregation in human platelets, indicating its value as a selective tool for purinoceptor research.

FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T‐purinoceptors

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Implication

Key Points

Cite This Study

FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T‐purinoceptors

Discussion

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Implication

Key Points

Cite This Study

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