Angiotensin II receptors and angiotensin II receptor antagonists.
- P. Timmermans, P. Wong, R. Smith
- BiologyPharmacological Reviews
- 1 June 1993
Identification of angiotensin II receptor subtypes.
- A. Chiu, W. Herblin, A. Johnson
- Biology, ChemistryBiochemical and Biophysical Research…
- 30 November 1989
Apixaban Metabolism and Pharmacokinetics after Oral Administration to Humans
- Nirmala Raghavan, C. Frost, Donglu Zhang
- Biology, MedicineDrug Metabolism And Disposition
- 1 January 2009
Apixaban is an orally bioavailable inhibitor of factor Xa with elimination pathways that include metabolism and renal excretion with no serious adverse events or discontinuations due to adverse effects.
Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies
In vivo, apixaban was effective in the prevention of experimental thrombosis at doses that preserve hemostasis in rabbits and potent and selective, with a Ki of 0.08 nm for human FXa.
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious,…
- D. Pinto, M. J. Orwat, P. Lam
- Chemistry, BiologyJournal of Medicinal Chemistry
- 3 October 2007
Compound 40 exhibits a high degree of fXa potency, selectivity, and efficacy and has an improved pharmacokinetic profile relative to 4.
Angiotensin II receptor subtypes.
- P. Timmermans, A. Chiu, W. Herblin, P. Wong, R. Smith
- BiologyAmerican Journal of Hypertension
- 1 June 1992
The AT1 and AT2 receptor subtypes/binding sites identified so far appears widespread and the presence and proportion of these receptors vary significantly among different tissues/organs of the same species and within the same tissue/organ of different species.
Angiotensin II receptors and functional correlates.
- P. Timmermans, P. Benfield, A. Chiu, W. Herblin, P. Wong, R. Smith
- BiologyAmerican Journal of Hypertension
- 1 December 1992
The angiotensin receptor and its functional correlates have been redefined by the cloning of angiotENSin receptors and the discovery and widespread study of specific nonpeptide ANG II-receptor antagonists losartan (AT1 selective) and PD123177 (AT2 selective).
Nonpeptide angiotensin II receptor antagonists. XI. Pharmacology of EXP3174: an active metabolite of DuP 753, an orally active antihypertensive agent.
- P. Wong, W. Price, P. Timmermans
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 October 1990
The results demonstrate that EXP3174 is a selective and noncompetitive AII receptor antagonist and lacks agonistic effect and may be responsible for part of the antihypertensive effect of DuP 753 in rats.
Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor
- P. Wong, D. Pinto, Donglu Zhang
- BiologyJournal of Thrombosis and Thrombolysis
- 13 February 2011
Non-clinical findings have established the favorable pharmacological profile of apixaban, and support the potential use of Apixaban in the clinic for the prevention and treatment of various thromboembolic diseases.
Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding
- P. Wong, D. Seiffert, Jing Yang
- Biology, MedicineScience Translational Medicine
- 4 January 2017
Targeting PAR4 is an attractive antiplatelet strategy with the potential to treat patients at a high risk of atherothrombosis with superior safety compared with the current standard of care, and is defined as a biological role of PAR4 in mediating platelet aggregation.
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