Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Ralf Lotz"'
Publikováno v:
Pharmaceutics, Vol 11, Iss 11, p 595 (2019)
Movement of xenobiotic substances across the blood−brain barrier (BBB) is tightly regulated by various transporter proteins, especially the efflux transporters P-glycoprotein (P-gp/MDR1) and breast cancer resistance protein (BCRP). Avoiding drug ef
Externí odkaz:
https://doaj.org/article/84ea435ab49f49b6880b1423e43d1294
Autor:
Kota Toshimoto, Yuichi Sugiyama, Renato J. Scialis, Nora Lee, Ryota Kikuchi, Hiroyuki Kusuhara, Ralf Lotz, Wooin Lee, Naoki Ishiguro, Xiaoyan Chu, Albert P. Li, Kazuya Maeda, Kiyoe Morita, Aya Kiriake, Manthena V.S. Varma, Takashi Yoshikado, Emi Kimoto, Hong Shen
Publikováno v:
Journal of Pharmaceutical Sciences. 110:376-387
Hepatic uptake clearance has been measured in suspended human hepatocytes (SHH). Plated human hepatocytes (PHH) after short-term culturing are increasingly employed to study hepatic transport driven mainly by its higher throughput. To know pros/cons
Autor:
Claudia Dallinger, Kristell Marzin, Sven Wind, Ulrike Schmid, Ralf Lotz, Matthias Freiwald, Peter Stopfer, Thomas Ebner
Publikováno v:
Clinical Pharmacokinetics
Nintedanib is an oral, small-molecule tyrosine kinase inhibitor approved for the treatment of idiopathic pulmonary fibrosis and patients with advanced non-small cell cancer of adenocarcinoma tumour histology. Nintedanib competitively binds to the kin
Autor:
Kerstin Julia Schäfer, Georg Boeck, Tabea Bollmann, Ralf Lotz, Simone M. Blattner, Werner Weitschies, Michael Grimm, Mirko Koziolek
Publikováno v:
European Journal of Pharmaceutics and Biopharmaceutics. 136:221-230
In preclinical research, Beagle dogs are an important model for formulation development and for evaluation of food effects on drug absorption. In this study, the gastrointestinal transit conditions in Beagle dogs were studied with a telemetric motili
Autor:
Kazuya Maeda, Nora Lee, Hong Shen, Ralf Lotz, Satoshi Koyama, Yuichi Sugiyama, Hiroyuki Kusuhara, Ryota Kikuchi, Kiyoe Morita, Naoki Ishiguro, Renato J. Scialis, Wooin Lee, Xiaoyan Chu, Larry M. Tremaine, Emi Kimoto, Aya Kiriake
Publikováno v:
The AAPS Journal
Suspended human hepatocytes (SHH) have long been used in assessing hepatic drug uptake, while plated human hepatocytes in short-term monolayer culture (PHH) have gained use in recent years. This study aimed to cross-evaluate SHH and PHH in measuring
Publikováno v:
Pharmaceutics, Vol 11, Iss 11, p 595 (2019)
Pharmaceutics
Volume 11
Issue 11
Pharmaceutics
Volume 11
Issue 11
Movement of xenobiotic substances across the blood&ndash
brain barrier (BBB) is tightly regulated by various transporter proteins, especially the efflux transporters P-glycoprotein (P-gp/MDR1) and breast cancer resistance protein (BCRP). Avoidin
brain barrier (BBB) is tightly regulated by various transporter proteins, especially the efflux transporters P-glycoprotein (P-gp/MDR1) and breast cancer resistance protein (BCRP). Avoidin
Autor:
Frank Himmelsbach, Ralf Lotz, Moh Tadayyon, Elke Langkopf, Herbert Nar, Norbert Hauel, Leo Thomas, Matthias Eckhardt, Michael Mark, Brian Guth
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3158-3162
Systematic variations of the xanthine scaffold in close analogs of development compound BI 1356 led to the class of 3,5-dihydro-imidazo[4,5-d]pyridazin-4-ones which provided, after substituent screening, a series of highly potent DPP-4 inhibitors.
Autor:
Thorsten Lehmann, Ralf Lotz, Thorsten Oost, Mueller Stephan Georg, Klaus Rudolf, Dirk Stenkamp, Armin Heckel, Ralph Budzinski, Jörg Kley, Gerd-Michael Maier, Gerald Juergen Roth, Leo Thomas, Martin Lenter, Kirsten Arndt, Michael Markert
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(16)
Although overweight and obesity are highly prevalent conditions, options to treat them are still very limited. As part of our search for safe and effective MCH-R1 antagonists for the treatment of obesity, two series of pyridones and pyridazinones wer
Autor:
Gerd-Michael Maier, Thorsten Lehmann, Ralf Lotz, Jörg Kley, Martin Lenter, Michael Markert, Mueller Stephan Georg, Kirsten Arndt, Philipp Lustenberger, Klaus Rudolf, Thorsten Oost, Armin Heckel, Marcus Schindler, Gerald Juergen Roth, Dirk Stenkamp
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(16)
Despite recent approvals of anti-obesity drugs there is still a high therapeutic need for alternative options with higher efficacy in humans. As part of our MCH-R1 antagonist program for the treatment of obesity, a series of biphenylacetamide HTS hit
Autor:
Kirsten Arndt, Ralf Lotz, Klaus Rudolf, Thorsten Lehmann, Mueller Stephan Georg, Ralph Budzinski, Gerald Juergen Roth, Leo Thomas, Martin Lenter, Dirk Stenkamp, Armin Heckel, Thorsten Oost, Marcus Schindler, Jörg Kley
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(16)
Despite recent success there remains a high therapeutic need for the development of drugs targeting diseases associated with the metabolic syndrome. As part of our search for safe and effective MCH-R1 antagonists for the treatment of obesity, a serie