Results 21 to 30 of about 18,066 (161)

Analytical and Pharmacological Characterization of 1‐(Furan‐2‐Carbonyl)‐LSD (1F‐LSD) and Comparison With 1‐(Thiophene‐2‐Carbonyl)‐LSD (1T‐LSD)

open access: yesDrug Testing and Analysis, EarlyView.
The novel lysergamide 1‐(furan‐2‐carbonyl)‐LSD (1F‐LSD) was analytically characterized. 1F‐LSD showed LSD‐like activity in vivo similar to 1‐(thiophene‐2‐carbonyl)‐LSD (1T‐LSD) used for comparison. Administration studies in mice and LC–MS analysis revealed that 1F‐LSD served as a prodrug.
Simon D. Brandt   +5 more
wiley   +1 more source

Population Pharmacokinetics of Fruquintinib, a Selective Oral Inhibitor of VEGFR ‐1, ‐2, and ‐3, in Patients with Refractory Metastatic Colorectal Cancer

open access: yesThe Journal of Clinical Pharmacology, EarlyView.
Abstract Fruquintinib is a selective, oral tyrosine kinase inhibitor of all three vascular endothelial growth factor receptors 1, 2, and 3, which is approved for patients with previously treated metastatic colorectal cancer regardless of biomarker status. This population pharmacokinetic (PK) analysis characterized sources of interpatient variability on
Xiaofei Zhou   +10 more
wiley   +1 more source

An infant with Kawasaki disease having gastrointestinal bleeding due to multiple gastric ulcers

open access: yesJournal of General and Family Medicine, EarlyView.
Abstract Kawasaki disease (KD) is an acute systemic vasculitis managed mainly through intravenous immunoglobulin (IVIG), aspirin, and steroids. Although gastrointestinal symptoms are common, gastrointestinal bleeding is rare. We present the case of an 11‐month‐old girl with incomplete KD who developed severe gastrointestinal bleeding due to multiple ...
Takeru Kanazawa   +3 more
wiley   +1 more source

Palmitoylation of the canine histamine H2 receptor occurs at Cys305 and is important for cell surface targeting [PDF]

open access: yes, 2001
To determine the presence and functional role of the histamine H2 receptor (H2R) palmitoylation, a receptor with a Cys305 to Ala (A305 receptor) mutation was generated. Wild-type (WT) and A305 receptors were tagged at their N-termini with a hemagglutinin
Anai, Motonobu   +14 more
core   +1 more source

Proteomic Profiling Informs Mechanisms of Esophageal Adenocarcinoma Inhibition by Cranberry Proanthocyanidins

open access: yesMolecular Nutrition &Food Research, EarlyView.
In this study we utilized proteomic profiling to investigate mechanisms linked to the cancer‐inhibitory effect of cranberry proanthocyanidins (CPACs) on reflux‐induced esophageal adenocarcinoma in a rat model. The results indicate that CPAC inhibits cancer through targeting multiple hallmarks of cancer known to be dysregulated in progression to ...
Yun Zhang   +7 more
wiley   +1 more source

Influence of mirtazapine on salivary cortisol in depressed patients [PDF]

open access: yes, 2003
Unlike other antidepressants, mirtazapine does not inhibit the reuptake of norepinephrine or serotonin but acts as an antagonist at presynaptic alpha(2)-receptors, at postsynaptic 5-HT2 and 5-HT3 receptors, and at histaminergic H1 receptors. Furthermore,
Baghai, Thomas C.   +3 more
core   +1 more source

Is Deuterium Sequestering by Reactive Carbon Atoms an Important Mechanism to Reduce Deuterium Content in Biological Water?

open access: yesFASEB BioAdvances, EarlyView.
Deuterium, a heavy isotope of hydrogen, is universal in nature, but it disrupts the mitochondrial ATPase pumps. One mechanism that biological organisms may use to reduce deuterium levels in the mitochondria is to sequester deuterium bound to carbon atoms in a small set of organic molecules that have a unique configuration to support such trapping ...
Stephanie Seneff   +2 more
wiley   +1 more source

Histamine and Histamine H4 Receptor Promotes Osteoclastogenesis in Rheumatoid Arthritis. [PDF]

open access: yes, 2017
Histamine H4 receptor (H4R) has immune-modulatory and chemotaxic effects in various immune cells. This study aimed to determine the osteoclastogenic role of H4R in rheumatoid arthritis (RA).
Firestein, Gary S   +5 more
core   +1 more source

Progress on the development of Class A GPCR‐biased ligands

open access: yesBritish Journal of Pharmacology, EarlyView.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales   +20 more
wiley   +1 more source

First description of a histamine receptor of class 2 (HRH2) in a protochordate: expression during blastogenesis and role in regulation of ciliary beat frequency [PDF]

open access: yes, 2016
Histaminergic receptors belong to the family of seven-transmembrane \u3b1-helix domain receptors classified in mammals into four distinct classes. Despite being widely studied in vertebrates, few data are available on the invertebrate receptors, with ...
Cima, Francesca
core  

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