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The in vivo pharmacological profile of CS‐747, a novel antiplatelet agent with platelet ADP receptor antagonist properties
TLDR
In vivo pharmacological profiles of CS‐747 show that it is an orally active and a potent antiplatelet and antithrombotic agent with a rapid onset and long duration of action, and warrants clinical evaluations of the agent. Expand
Antiplatelet action of R‐99224, an active metabolite of a novel thienopyridine‐type Gi‐linked P2T antagonist, CS‐747
TLDR
R‐99224 is a selective and irreversible antagonist of Gi‐linked P2T receptors and that R‐99 224 is a responsible molecule for in vivo actions of CS‐747 are suggested. Expand
The greater in vivo antiplatelet effects of prasugrel as compared to clopidogrel reflect more efficient generation of its active metabolite with similar antiplatelet activity to that of clopidogrel’s
TLDR
The greater in vivo antiplatelet potency of prasug Rel reflects more efficient in vivo generation of its AM, which demonstrates similar in vitro activity to clopidogrel AM. Expand
Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444.
TLDR
Antiplatelet effects of R-96544 and R-102444 were more potent than those of two other 5-HT(2A) receptor antagonists, sarpogrelate and its active metabolite (+/-)-1-[2-methoxyphenyl)ethyl]phenoxy]-3-(dimethylamino)-2-propanol hydrochloride (M-1). Expand
Exosite-mediated Substrate Recognition of Factor IX by Factor XIa
TLDR
The results support a model in which factor IX binds initially to exosites on the factor XIa heavy chain, followed by interaction at the active site with subsequent bond cleavage, and support a growing body of evidence that exosite interactions are critical determinants of substrate affinity and specificity in blood coagulation reactions. Expand
[2-(omega-phenylalkyl)phenoxy]alkylamines.II: Synthesis and selective serotonin-2 receptor binding.
TLDR
(S)-2-[2- [2-(3-methoxyphenyl)ethyl]phenoxy]ethyl]-1-methylpyrrolidine, (S)-27, exhibited the most potent and selective affinity for 5-HT2 receptors and was effective in inhibiting 5- HT2-induced vasoconstriction in vitro and platelet aggregation both in vivo and ex vivo. Expand
Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (prasugrel, LY640315), a novel P2Y12 receptor inhibitor.
TLDR
In vitro studies indicate that R- 138727 is an effective antagonist of P2Y12 and potent inhibitor of ADP-induced platelet aggregation, and that these antiplatelet activities of R-138727 are largely dependent on its (R, S)-isomer. Expand
Repeat oral dosing of prasugrel, a novel P2Y12 receptor inhibitor, results in cumulative and potent antiplatelet and antithrombotic activity in several animal species.
TLDR
Results show that in several species multiple oral administration of prasugrel results in more potent inhibition of platelet aggregation and thrombus formation than clopidogrel and ticlopidine, and that these effects are mediated by inhibition of Platelet ADP receptors. Expand
The influence of P2Y12 receptor deficiency on the platelet inhibitory activities of prasugrel in a mouse model: evidence for specific inhibition of P2Y12 receptors by prasugrel.
TLDR
In the present study, effects of prasugrel on ex vivo platelet aggregation were examined in wild type (WT) and P2Y(12)(-/-) mice and results clearly provide additional in vivo evidence that pr asugrel has selective P2y(12) antagonistic activity. Expand
A comparison of the pharmacological profiles of prasugrel and ticagrelor assessed by platelet aggregation, thrombus formation and haemostasis in rats
TLDR
Prasugrel is a third‐generation thienopyridine prodrug and ticagrelor is a non‐competitive P2Y12 receptor antagonist and both agents reduced rates of ischemic events relative to treatment with clopidogrel. Expand
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