• Publications
  • Influence
Prasugrel achieves greater and faster P2Y12receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite in aspirin-treated patients with coronary
TLDR
In aspirin-treated subjects with coronary artery disease, prasugrel 60/10 mg provides faster onset and greater inhibition of P2Y(12) receptor-mediated platelet aggregation than clopidogrel 600/75 mg, because of greater and more efficient generation of the active metabolite. Expand
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
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
Patients with poor responsiveness to thienopyridine treatment or with diabetes have lower levels of circulating active metabolite, but their platelets respond normally to active metabolite added ex
TLDR
The mechanism of incomplete platelet inhibition in clopidogrel poor-responder groups and in diabetic patients is lower plasma levels of its AM and not differences in platelet P2Y(12) receptor function. 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
Regulation of Functionally Active P2Y12 ADP Receptors by Thrombin in Human Smooth Muscle Cells and the Presence of P2Y12 in Carotid Artery Lesions*
TLDR
The data suggest that the P2Y12 receptor not only is central to ADP-induced platelet activation but also may mediate platelet-independent responses, specifically under conditions of enhanced thrombin formation, such as local vessel injury and atherosclerotic plaque rupture. 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
Impaired responsiveness to the platelet P2Y12 receptor antagonist clopidogrel in patients with type 2 diabetes and coronary artery disease.
TLDR
Among DM patients, impaired P2Y12 inhibition mediated by clopidogrel is largely attributable to attenuation of clopilator-stimulated phosphoprotein's PK profile, and this is characterized by lower plasma levels of Clop-AM over the sampling time course. 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
Relationship between degree of P2Y12 receptor blockade and inhibition of P2Y12-mediated platelet function.
TLDR
Different assays varied in their ability to discriminate particular ranges of P2Y12 blockade and 80% or greater P2y12 receptor blockade is required for consistently strong inhibition of several aspects of platelet function, which guides the interpretation of results from different assays used to monitor the effects of P 2Y12 receptor antagonists. Expand
...
1
2
3
4
5
...