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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
Platelet inhibitory activity and pharmacokinetics of prasugrel (CS-747) a novel thienopyridine P2Y12 inhibitor: A single ascending dose study in healthy humans
TLDR
Prasugrel 30 and 75 mg were well tolerated and achieved a consistently high level of platelet inhibition with a fast onset of action, suggesting irreversible inhibition by prasugrel and/or its metabolites. Expand
Pharmacology of CS-747 (prasugrel, LY640315), a novel, potent antiplatelet agent with in vivo P2Y12 receptor antagonist activity.
TLDR
Studies conducted to date indicate that CS-747 is a highly effective antiplatelet and antithrombotic agent and is anticipated to be effective in the treatment of atherothrombosis and other ischemic vascular diseases. Expand
A multiple dose study of prasugrel (CS-747), a novel thienopyridine P2Y12 inhibitor, compared with clopidogrel in healthy humans.
TLDR
Compared with clopidogrel 75 mg, prasugrel 10 mg and 20 mg daily for 10 days resulted in more rapid, more consistent, and higher levels of platelet inhibition. 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
Platelet inhibitory activity and pharmacokinetics of prasugrel (CS-747) a novel thienopyridine P2Y12 inhibitor: A multiple-dose study in healthy humans
TLDR
This study indicated that prasugrel 10 mg daily for 10 days was well tolerated and at steady-state provided sustained high levels of inhibition of platelet aggregation. Expand
Preparation of leustroducsin H and the structure-activity relationship of its derivatives.
TLDR
The hydrolysis to yield Id only indicated that all LSNs have the same absolute configuration, which was determined to be 4S, 5S9 SR, 9R, UR, 16R, 18S. Expand
Mechanism of cadmium-induced blockade of neuromuscular transmission.
TLDR
It is suggested that Cd 2+ reversibly inhibits neuromuscular transmission by reducing transmitter release from motor nerve terminals resulting from the inhibition of Ca 2+ influx at the membrane of axon terminals. 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
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