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Small-molecule WNK inhibition regulates cardiovascular and renal function.
In rodent models of hypertension, WNK463 affects blood pressure and body fluid and electro-lyte homeostasis, consistent with WNK-kinase-associated physiology and pathophysiology.
Pharmacodynamic and Pharmacokinetic Characterization of the Aldosterone Synthase Inhibitor FAD286 in Two Rodent Models of Hyperaldosteronism: Comparison with the 11β-Hydroxylase Inhibitor Metyrapone
- D. Rigel, F. Fu, M. Beil, Chii-Whei Hu, Guiqing Liang, A. Jeng
- Biology, MedicineJournal of Pharmacology and Experimental…
- 1 July 2010
FAD is a potent, orally active, and relatively selective ASI in two rat models of hyperaldosteronism and metyrapone is an order of magnitude less selective than FAD but is, nevertheless, more potent as an ASI than as an 11β-hydroxylase inhibitor.
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
Compound 7n was found to be a potent inhibitor of 11β-hydroxylase (CYP11B1), which is responsible for cortisol production, and is being evaluated in the clinic for potential treatment of hypercortisol diseases such as Cushing's syndrome.
Drug effects on the CVS in conscious rats: separating cardiac output into heart rate and stroke volume using PKPD modelling
The present investigation aims to extend the previously developed model by parsing CO into heart rate (HR) and stroke volume (SV) and evaluate if the mechanism of action (MoA) of new compounds can be elucidated using only HR and MAP measurements.
PKPD modelling of the interrelationship between mean arterial BP, cardiac output and total peripheral resistance in conscious rats
A mechanism‐based pharmacokinetic‐pharmacodynamic (PKPD) model in rats is developed that could be used to characterize the effects of cardiovascular drugs with different mechanisms of action (MoA) on the interrelationship between BP, CO and TPR.
Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects
These results provide new insights into the cardiac and renal effects of inhibiting aldosterone synthase in experimental models and translation of the hormonal effects to humans.
Design and synthesis of a potent and selective endothelin-converting enzyme inhibitor, CGS 35066.
CGS 35066 and CGS 35339 represent novel compounds for assessing the pathogenic role of ET-1 overproduction in various disease states and exhibited a potent and sustained ECE-1 inhibitory activity in vivo.
CGS 35601 and its Orally Active Prodrug CGS 37808 as Triple Inhibitors of Endothelin-converting Enzyme-1, Neutral Endopeptidase 24.11, and Angiotensin-converting Enzyme
- A. Trapani, M. Beil, C. Bruseo, P. Savage, F. Firooznia, A. Jeng
- Biology, MedicineJournal of cardiovascular pharmacology
- 1 November 2004
By suppressing the biosyntheses of endothelin-1 and angiotensin II, two potent vasoconstrictors, while simultaneously potentiating the circulating levels of ANP, a vasorelaxant and diuretic, CGS 35601 and CGS 37808 may represent novel agents for the treatment of cardiovascular and renal diseases.
Evaluation of the cardiovascular effects of arecoline in the anesthetized dog
The data indicate that the continuous administration of a low dose of arecoline may minimize the undesired cardiovascular effects and suggest that a greater therapeutic ratio may be achieved in the presence of a peripheral muscarinic blocking agent.