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NO-independent regulatory site on soluble guanylate cyclase
TLDR
A pyrazolopyridine is presented that potently stimulates sGC through this site by a mechanism that is independent of NO, which results in antiplatelet activity, a strong decrease in blood pressure and an increase in survival in a low-NO rat model of hypertension, and may offer an approach for treating cardiovascular diseases.
NO‐ and haem‐independent activation of soluble guanylyl cyclase: molecular basis and cardiovascular implications of a new pharmacological principle
TLDR
A novel type of sGC activator which activates the enzyme even after it has been oxidized by the sGC inhibitor ODQ or rendered haem deficient is identified and may offer a new approach for treating cardiovascular diseases.
Finerenone, a Novel Selective Nonsteroidal Mineralocorticoid Receptor Antagonist Protects From Rat Cardiorenal Injury
TLDR
Investigation of the tissue distribution and chronic cardiorenal end-organ protection of finerenone in comparison to the steroidal MR antagonist, eplerenone, in 2 different preclinical rat disease models concludes that finerenones may offer end- Organ protection with a reduced risk of electrolyte disturbances.
BAY 1000394, a Novel Cyclin-Dependent Kinase Inhibitor, with Potent Antitumor Activity in Mono- and in Combination Treatment upon Oral Application
TLDR
BAY 1000394 is a potent pan-CDK inhibitor and a novel oral cytotoxic agent currently in phase I clinical trials and shows more than additive efficacy when combined with cisplatin and etoposide.
Artemisone--a highly active antimalarial drug of the artemisinin class.
TLDR
Efficacies of artemisone against the malaria parasite are substantially greater than those of the current artemisinin "gold standard", artesunate and it displays low lipophilicity and negligible neuro- and cytotoxicity in in vitro and in vivo assays.
Pharmacokinetics of miglitol. Absorption, distribution, metabolism, and excretion following administration to rats, dogs, and man.
TLDR
The absorption, distribution, metabolism, and excretion of miglitol have been studied following single and repeated administration of non-labelled and radiolabelled drug to rats, dogs, and human volunteers via different routes of administration and at various doses.
NO-independent regulatory site of direct sGC stimulators like YC-1 and BAY 41-2272
TLDR
The data demonstrate that the region surrounding the cysteines 238 and 243 in the α1-subunit of the sGC could play an important role in regulation of s GC activity and could be the target of this new type of sGC stimulators.
Biotransformation of cerivastatin in mice, rats, and dogs in vivo.
Biotransformation of cerivastatin was investigated in mice, rats, and dogs in vivo using the 14C-labeled drug. Marked species differences exist, both in pathways and extent of cerivastatin
Pharmacokinetics of BAY 59-7939 – an oral, direct Factor Xa inhibitor – in rats and dogs
TLDR
BAY 59-7939 had a favourable, predictable pharmacokinetic profile, with high oral bioavailability and a dual route of excretion, and was rapidly excreted in rats and dogs and was not irreversibly retained.
Pharmacokinetics of the 8-methoxyquinolone, moxifloxacin: tissue distribution in male rats.
TLDR
The results show a high tissue affinity and a rapid and homogeneous distribution of radioactivity from blood to organs or tissues and in melanin-containing structures located in the eye, meninges and hair follicles of pigmented skin.
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