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Identification of angiotensin II receptor subtypes.
TLDR
Two distinct subtypes of the angiotensin II receptor in the rat adrenal gland are demonstrated using radioligand binding and tissue section autoradiography and the discovery of two structurally dissimilar, nonpeptide compounds that show reciprocal selectivity for the two subtypes.
Apixaban Metabolism and Pharmacokinetics after Oral Administration to Humans
TLDR
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
TLDR
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.
Angiotensin II receptors and functional correlates.
TLDR
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).
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,
TLDR
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.
TLDR
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.
Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor
TLDR
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.
Nonpeptide angiotensin II receptor antagonists. XI. Pharmacology of EXP3174: an active metabolite of DuP 753, an orally active antihypertensive agent.
TLDR
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.
Functional studies of nonpeptide angiotensin II receptor subtype-specific ligands: DuP 753 (AII-1) and PD123177 (AII-2).
TLDR
A function of the PD123177-sensitive AII binding site (AII-2) has not yet been identified, however, the DuP 753-sensitive site appears to mediate the AII-induced responses such as adrenal aldosterone and catecholamine secretion, release from sympathetic ganglia, drinking and vasoconstriction.
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