Results 61 to 70 of about 27,101 (273)

Metabolic Profiling of the Uncaria Hook Alkaloid Geissoschizine Methyl Ether in Rat and Human Liver Microsomes Using High-Performance Liquid Chromatography with Tandem Mass Spectrometry

Molecules, 2015
Geissoschizine methyl ether (GM) is an indole alkaloid found in Uncaria hook, which is a galenical constituent of yokukansan, a traditional Japanese medicine. GM has been identified as the active component responsible for anti-aggressive effects. In this
Hirotaka Kushida, Takashi Matsumoto, Yasushi Igarashi, Hiroaki Nishimura, Junko Watanabe, Kazuya Maemura, Yoshio Kase   +6 more
doaj   +1 more source

Comparative Metabolism of Cinobufagin in Liver Microsomes from Mouse, Rat, Dog, Minipig, Monkey, and Human

, 2011
Comparative Metabolism of Cinobufagin in Liver Microsomes from Mouse, Rat, Dog, Minipig, Monkey, and HumanCinobufagin (CB), a major bioactive component of the traditional Chinese medicine Chansu, has been reported to have potent antitumor activity.
Ning, Jing, Liang, Si-Cheng, Li, Jing-Kui, 杨凌, Huang, Shan-Shan, Ge, Guang-Bo, Wang, Xiu-Li, Yang, Ling, Ma, Xiao-Chi, Zhang, Bao-Jing   +9 more
core   +1 more source

First‐in‐human, phase I, randomized, safety, pharmacokinetic, food‐effect and pharmacodynamic study of a tyrosine kinase 2/Janus kinase 1 inhibitor, SDC‐1801

British Journal of Clinical Pharmacology, EarlyView.
Aim The purpose of this study is to evaluate safety, tolerability, pharmacokinetics (PK), food‐effect (FE) and pharmacodynamics (PD) of an oral tyrosine kinase‐2 (TYK2)/Janus kinase‐1 (JAK1) inhibitor, SDC‐1801, in healthy adult participants. Methods This first‐in‐human study randomized 95 male and female participants.
Chris Brearley, Sam Francis, John Reader, Judi Proctor   +3 more
wiley   +1 more source

Inhibition of in vitro metabolism of testosterone in human, dog and horse liver microsomes to investigate species differences.

, 2015
Testosterone hydroxylation was investigated in human, canine and equine liver microsomes and in human and canine single CYPs. The contribution of the CYP families 1, 2 and 3 was studied using chemical inhibitors. Testosterone metabolites were analyzed by
Mevissen, Meike, Zielinski, Jana
core   +1 more source

Tetrazine Ligation in Living Systems: Beyond Fast Kinetics to Effective Bioorthogonality

Chemistry – A European Journal, EarlyView.
Rapid reaction kinetics (k2) alone do not ensure successful tetrazine ligation in living systems. This review introduces ‘effective orthogonality’—focusing on chemical survival, availability, and encounter—as a practical framework. We highlight how bottlenecks shift from cellular sinks to in vivo delivery limits, offering design strategies for reliable
Junhyeong Yim, Junyoung Park, Youngjun Lee, Jongmin Park   +3 more
wiley   +1 more source

PharmVar GeneFocus: CYP1A2—Clinical Impact, Genetic Variation, and Updated Nomenclature

Clinical Pharmacology &Therapeutics, EarlyView.
The Pharmacogene Variation Consortium (PharmVar) provides nomenclature for the highly polymorphic human CYP1A2 gene. CYP1A2 plays a crucial role in the biotransformation of several commonly used drugs, including antipsychotics, antidepressants, anxiolytics, and methylxanthines.
Katalin Monostory, Gonzalo Villapalos Garcia, Dora Koller, Solomon Adams, Chad A. Bousman, Evangelia Eirini Tsermpini, Michelle Whirl‐Carrillo, Amy J. Turner, Volker M. Lauschke, Mohamed Nagy, Erin C. Boone, Teri E. Klein, Pablo Zubiaur, Andrea Gaedigk   +13 more
wiley   +1 more source

Preclinical metabolism and metabolic drug–drug interaction profile of pedunculoside and rotundic acid

Clinical and Translational Science
Pedunculoside and rotundic acid, the most abundant components in plants of the genus Ilex L. (Aquifoliaceae), exhibit biological and pharmacological significance in the treatment of cardiovascular diseases.
Liang Wu, Linling Dong, Zhu Zhou, Xin Wang, Yujie Lin, Xuesong Shi, Peijing Wang, Suocheng Xu, Zhiyi Fang   +8 more
doaj   +1 more source

Repurposing Drugs for Malaria through a Human Dose Prediction: A Case Study with Berzosertib

Clinical Pharmacology &Therapeutics, EarlyView.
Repurposing drugs whose clinical safety has been established offers a valuable approach to reduce the cost and time associated with the development of new drugs for malaria. Here, we investigate the potential to repurpose the anticancer kinase inhibitor berzosertib for the treatment of malaria, by assessing whether a predicted efficacious human dose ...
Devasha Redhi, Mwila Mulubwa, Mmakwena M. Mmonwa, Mathew Njoroge, Liezl Krugmann, Kelly Chibale   +5 more
wiley   +1 more source

In Vitro Inhibitory Effects of Scutellarin on Six Human/Rat Cytochrome P450 Enzymes and P-glycoprotein

Molecules, 2014
Inhibition of cytochrome P450 (CYP) and P-glycoprotein (P-gp) are regarded as the most frequent and clinically important pharmacokinetic causes among the various possible factors for drug-drug interactions. Scutellarin is a flavonoid which is widely used
Yong-Long Han, Dan Li, Quan-Jun Yang, Zhi-Yong Zhou, Li-Ya Liu, Bin Li, Jin Lu, Cheng Guo   +7 more
doaj   +1 more source

Decavanadate displaces inositol 1,4,5-trisphosphate (IP3) from its receptor and inhibits IP3 induced Ca2+ release in permeabilized pancreatic acinar cells [PDF]

, 1991
Inositol 1,4,5-trisphosphate (IP3) induced Ca2+ release in digitonin permeabilized rat pancreatic acinar cells is specifically inhibited by decavanadate.
M. Gratzl, Föhr, K. J., T.P. Kemmer, Wahl, Y., K.J. Föhr, R. Engling, Engling, R., Gratzl, Manfred, Y. Wahl, Kemmer, T. P.   +9 more
core   +1 more source