Results 81 to 90 of about 56,016 (216)

Gas Chromatography of Glucuronides.

Chemical and Pharmaceutical Bulletin, 1967
The applicability of gas chromatography to the analysis of various types of glucuronides including ether-, ester-, N-and S-glucuronides was studied by converting them to acetyl, methyl and trimethylsilyl derivatives.
T, Imanari, Z, Tamura
openaire   +3 more sources

Divergence in μ and δ opioid receptor pharmacology in neurons and antinociceptive efficacy in neuropathic pain: Insights from MP135 and CYM51010

British Journal of Pharmacology, EarlyView.
Background and purpose Opioids targeting the μ opioid receptor remain largely ineffective in neuropathic pain conditions, emphasizing the need for novel therapeutic strategies. MP135 was reported to reduce thermal nociception in naive animals by activating μ‐δ opioid receptor heteromers.
Perrine Inquimbert, Chantal Fitterer, Sylvain Hugel, Mila Jesic, Yannick Goumon, Virgine Andry, Severine Schneider, Francois Daubeuf, Abdelfattah Faouzi, Stephane Doridot, Susruta Majumdar, Frederic Bihel, Martine Schmitt, Dominique Massotte   +13 more
wiley   +1 more source

Characterization of CYPs and UGTs Involved in Human Liver Microsomal Metabolism of Osthenol

Pharmaceutics, 2018
Osthenol is a prenylated coumarin isolated from the root of Angelica koreana and Angelica dahurica, and is an O-demethylated metabolite of osthole in vivo. Its various pharmacological effects have been reported previously.
Pil Joung Cho, Sanjita Paudel, Doohyun Lee, Yun Ji Jin, GeunHyung Jo, Tae Cheon Jeong, Sangkyu Lee, Taeho Lee   +7 more
doaj   +1 more source

Influence of OATP1B1 Function on the Disposition of Sorafenib-β-D-Glucuronide [PDF]

, 2017
The oral multikinase inhibitor sorafenib undergoes extensive UGT1A9-mediated formation of sorafenib-β-D-glucuronide (SG). Using transporter-deficient mouse models, it was previously established that SG can be extruded into bile by ABCC2 or follow a liver-
Baker, S.D., Bins, S. (Sander), Bruijn, P.J. (Peter) de, Doorn, L. (Leni) van, Du, G., Eskens, F.A.L.M. (Ferry), Gibson, A.A., Hamberg, A.P. (Paul), Hu, S. (Shuiying), L. Li, Mathijssen, A.H.J. (Ron), Phelps, M.A., Sparreboom, A. (Alex), Vasilyeva, A.   +13 more
core   +1 more source

Randomised, phase 1 evaluation of the safety, tolerability, pharmacokinetics and pharmacodynamics of iptacopan in healthy volunteers

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Overactivation of the alternative pathway (AP) underlies several diseases. Iptacopan is an oral, first‐in‐class, highly potent specific inhibitor of factor B, a key AP protease. Experimental Approach The analysis included data from two phase 1 randomised, volunteer‐blinded, placebo‐controlled studies: Study 1, a single ...
Irina Baltcheva, Guido Junge, Kenneth Kulmatycki, Robert Schmouder, Anna Schubart, Marie‐Anne Valentin   +5 more
wiley   +1 more source

In Vitro Glucuronidation of Ochratoxin A by Rat Liver Microsomes

Toxins, 2013
Ochratoxin A (OTA), one of the most toxic mycotoxins, can contaminate a wide range of food and feedstuff. To date, the data on its conjugates via glucuronidation request clarification and consolidation.
Zheng Han, Emmanuel K. Tangni, José Diana Di Mavungu, Lynn Vanhaecke, Sarah De Saeger, Aibo Wu, Alfons Callebaut   +6 more
doaj   +1 more source

Rewiring Steroidal Metabolic Pathways for Diosgenin Production in Solanum nigrum

Plant Biotechnology Journal, EarlyView.
ABSTRACT Diosgenin is a key starting material for the synthesis of steroidal drugs, such as corticosteroids and sex hormones. While the primary commercial source of diosgenin is the tubers of Dioscorea spp., identifying alternative plant hosts capable of diosgenin biosynthesis could enhance its production.
Jongbu Lim, Keunhwa Kim, Jung Heo, Seung Mo Seo, Sungjun Choung, Hyeonjin Kim, Yuri Choi, Kyungsun Park, Hyejung Yun, Dongha Kim, Eun Song Lee, Junwoo Lee, Smita Mirsyad Warsadiharja, Saet Buyl Lee, Sunkyu Han, Soon Ju Park, Sang‐Gyu Kim   +16 more
wiley   +1 more source

Insights into the Metabolism, Disposition, and Quantitative Profile of mGlu5 NAM AE90015 with Metabolite Identification and a Novel Integration Method

Molecules
AE90015 is a highly specific and effective negative allosteric modulator (NAM) for the human mGlu5 receptor, showing significant promise for treating Parkinson’s disease.
Zhiyang Zack Zou, Ming-Jie Han, Yu Chang, Guiying Li   +3 more
doaj   +1 more source

Regulation of Hepatic UGT2B15 by Methylation in Adults of Asian Descent

Pharmaceutics, 2018
The hepatic uridine 5′-diphosphate-glucuronosyl transferases (UGTs) are critical for detoxifying endo- and xenobiotics. Since UGTs are also dynamically responsive to endogenous and exogenous stimuli, we examined whether epigenetic DNA methylation can ...
Steffen G. Oeser, Jon-Paul Bingham, Abby C. Collier   +2 more
doaj   +1 more source

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, Beresford, Borchard, Kobayashi, Mahmoudian, Mahmoudian, Mohri, Moldeus, Ramsch, Roden, Scherling, Scherling, Scherling, Stopher, Teramura, Van Zwieten   +15 more
core   +1 more source