Results 11 to 20 of about 13,288 (170)

Noradrenergic inhibition of definitive POMC neurons through direct and indirect mechanisms. [PDF]

open access: yesJ Neuroendocrinol
Norepinephrine and the α2‐adrenoceptor agonist UK 14,304 robustly inhibit definitive arcuate POMC neurons. Direct inhibition is mediated by ADRA2A‐dependent activation of potassium conductances, while additional indirect mechanisms also contribute. In vivo, inducible POMC‐specific Adra2a deletion minimally affects energy balance and modestly impairs ...
Lavoie O   +6 more
europepmc   +2 more sources

Maternal-to-Infant Transfer of Medications for Type 2 Diabetes Mellitus Via Breastmilk: A Systematic Review of Available Evidence and Clinical Guidelines. [PDF]

open access: yesClin Pharmacol Ther
This review evaluates the available pharmacokinetic data on the plasma‐to‐breastmilk transfer of first‐ and second‐line T2DM drugs against available clinical guideline recommendations. A list of drug therapies for treating T2DM was generated from national and international clinical guidelines.
Richardson K   +4 more
europepmc   +2 more sources

Induction of cytochrome P450 2C9 and P-glycoprotein activity by antiseizure medications: A systematic review and network meta-analysis. [PDF]

open access: yesEpileptic Disord
Abstract Objectives Antiseizure medications (ASMs) can induce the activity of drug‐metabolizing enzymes and drug transporters, including cytochrome P450 (CYP)2C9 and P‐glycoprotein (P‐gp). Our objective was to comparatively assess the effects of ASMs on exposure to clinical CYP2C9 and P‐gp substrates.
Cohen H   +4 more
europepmc   +2 more sources

Development and Structural Characterization of UTE-156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase. [PDF]

open access: yesAdv Sci (Weinh)
The AAA+ ATPase Valosin‐containing protein (VCP/p97) regulates protein homeostasis by unfolding ubiquitinated substrates. Here, we describe UTE‐156, a novel irreversible covalent inhibitor that modifies Cys522 in the D2 ATPase motor domain. Although its pharmacochemical limitations preclude immediate therapeutic use, UTE‐156 serves as a valuable ...
Tamayo-Jaramillo D   +8 more
europepmc   +2 more sources

Quantitation of Diclofenac, Tolbutamide, and Warfarin as Typical CYP2C9 Substrates in Rat Plasma by UPLC-MS/MS and Its Application to Evaluate Linderane-Mediated Herb-Drug Interactions

open access: yesJournal of Analytical Methods in Chemistry, 2022
Linderane (LDR), the main active and distinctive component of L. aggregate, is a mechanism-based inactivator of CYP2C9 in vitro, indicating the occurrence of herb-drug interactions.
Tingting Zhang   +4 more
doaj   +1 more source

Cytochrome P450-Based Drug-Drug Interactions of Vonoprazan In Vitro and In Vivo

open access: yesFrontiers in Pharmacology, 2020
BackgroundVonoprazan fumarate is a potassium-competitive acid blocker that was developed as a novel acid-suppressing drug for multiple indications. As a potential alternative to proton-pump inhibitors, the determination of the drug-drug interactions is ...
Yiran Wang   +7 more
doaj   +1 more source

CHARACTERIZATION OF INSULIN SECRETION AFTER CONTINUOUS EXPOSURE OF NORMAL ISOLATED PERFUSED RAT PANCREAS FOR MORE THAN SIX HOURS TO GLUCOSE, THEOPHYLLINE AND TOLBUTAMIDE

open access: yesZagazig Journal of Pharmaceutical Sciences, 1997
A perfusion system was conducted for more than 6 hours in response to glucose (16.7mM), theophylline (5 mM ) and tolbutamide (100 µg/ml) to give an insight about the B-cell secretory capacity. Continuous exposure of the isolated pancreas to glucose (16.7
Hassan El-Fayoumi
doaj   +1 more source

Xiao chai hu tang for liver diseases: A literature review

open access: yesWorld Journal of Traditional Chinese Medicine, 2017
The objective of this study is to summarize the pharmacological effects and the mechanisms of action of Xiao Chai Hu Tang (XCHT, Minor Bupleurum Decoction) on liver diseases, so as to give relevant researchers a valuable insight and benefit patients with
Yi Wang   +3 more
doaj   +1 more source

Within-Sulfonylurea-Class Evaluation of Time to Intensification with Insulin (ZODIAC-43). [PDF]

open access: yesPLoS ONE, 2016
Previous studies have shown that many within-class differences exist between sulfonylureas (SUs), however, whether differences exist regarding the time it takes between initiating an SU and the need to intensify treatment with insulin is unclear. The aim
Dennis Schrijnders   +5 more
doaj   +1 more source

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