Metabolism of the dihydropyridine calcium channel blockers mebudipine and dibudipine by isolated rat hepatocytes [PDF]
The prototype 1,4-dihydropyridine (1,4-DHP) nifedipine, indicated for the management of hypertension and angina pectoris, has drawbacks of rapid onset of vasodilating action and a short half-life.
Baarnhielm +15 more
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Pharmaceutics, 2020 The number of therapeutic peptides for human treatment is growing rapidly. However, their development faces two major issues: the poor yield of large peptides from conventional solid-phase synthesis, and the intrinsically short serum half-life of ...
Mijeong Bak +7 more
doaj +1 more source
A Peptide-Based HIV-1 Fusion Inhibitor with Two Tail-Anchors and Palmitic Acid Exhibits Substantially Improved In Vitro and Ex Vivo Anti-HIV-1 Activity and Prolonged In Vivo Half-Life [PDF]
Molecules, 2019 Enfuvirtide (T20) is the first U.S. FDA-approved HIV fusion inhibitor-based anti-HIV drug. Its clinical application is limited because of its low potency and short half-life. We previously reported that peptide HP23-E6-IDL, containing both N- and C-terminal anchor-tails, exhibited stronger potency and a better resistance profile than T20.
Shan Su +7 more
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Quinolones modulate ghrelin receptor signaling: potential for a novel small molecule scaffold in the treatment of cachexia [PDF]
, 2018 Cachexia is a metabolic wasting disorder characterized by progressive weight loss, muscle atrophy, fatigue, weakness, and appetite loss. Cachexia is associated with almost all major chronic illnesses including cancer, heart failure, obstructive ...
Cano, Rafael +8 more
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Drug Design, Development and Therapy, 2020 Mohamed W Attwa, Ali S Abdelhameed, Nasser S Al-Shakliah, Adnan A Kadi 1 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi ArabiaCorrespondence: Ali S AbdelhameedDepartment of Pharmaceutical Chemistry ...
Attwa MW +3 more
doaj
Rationale-Based Engineering of a Potent Long-Acting FGF21 Analog for the Treatment of Type 2 Diabetes. [PDF]
PLoS ONE, 2012 Fibroblast growth factor 21 (FGF21) is a promising drug candidate for the treatment of type 2 diabetes. However, the use of wild type native FGF21 is challenging due to several limitations.
Randy Hecht +20 more
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Pharmaceutics, 2021 Ferritin, one of the most investigated protein nanocages, is considered as a promising drug carrier because of its advantageous stability and safety.
Shuang Yin +8 more
doaj +1 more source
Tumor Growth Increases Neuroinflammation, Fatigue and Depressive-like Behavior Prior to Alterations in Muscle Function [PDF]
, 2015 Cancer patients frequently suffer from fatigue, a complex syndrome associated with loss of muscle mass, weakness, and depressed mood. Cancer-related fatigue (CRF) can be present at the time of diagnosis, during treatment, and persists for years after ...
Bicer, Sabahattin +8 more
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Novel ACE2-IgG1 fusions with improved in vitro and in vivo activity against SARS-CoV2
bioRxiv, 2020 SARS-CoV2, the etiologic agent of COVID-19, uses ACE2 as a cell entry receptor. Soluble ACE2 has been shown to have neutralizing antiviral activity but has a short half-life and no active transport mechanism from the circulation into the alveolar spaces ...
N. Iwanaga +7 more
semanticscholar +1 more source
In vivo and in vitro assessment of mirtazapine pharmacokinetics in cats with liver disease. [PDF]
, 2018 BackgroundLiver disease (LD) prolongs mirtazapine half-life in humans, but it is unknown if this occurs in cats with LD and healthy cats.Hypothesis/objectivesTo determine pharmacokinetics of administered orally mirtazapine in vivo and in vitro (liver ...
Benson, Kellyi K +6 more
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