Tissue distribution of the novel DPP-4 inhibitor BI 1356 is dominated by saturable binding to its target in rats

2009 ◽  
Vol 30 (5) ◽  
pp. 229-240 ◽  
Author(s):  
Holger Fuchs ◽  
Rudolf Binder ◽  
Andreas Greischel
Keyword(s):  
Tissue Distribution ◽  
The Novel ◽  
Saturable Binding

Identification and Tissue Distribution of the Novel Human Cytochrome P450 2S1 (CYP2S1)

2001 ◽  
Vol 281 (2) ◽  
pp. 529-535 ◽  
Author(s):  
Tove Rylander ◽  
Etienne P.A. Neve ◽  
Magnus Ingelman-Sundberg ◽  
Mikael Oscarson
Keyword(s):  
Cytochrome P450 ◽  
Tissue Distribution ◽  
The Novel ◽  
Human Cytochrome

Characterization, tissue distribution and biological activity of the novel neuropeptide secretoneurin

Neuropeptides ◽  
1994 ◽  
Vol 26 ◽  
pp. 22
Author(s):  
R. Fischer-Colbrie ◽  
R. Kirchmair ◽  
J. Marksteiner ◽  
A. Saria ◽  
N. Reinisch ◽  
...  
Keyword(s):  
Biological Activity ◽  
Tissue Distribution ◽  
The Novel

scholarly journals Tissue distribution and tumor concentrations of hydroxychloroquine and quinacrine analogs in mice

2018 ◽  
Author(s):  
Abigail R. Solitro ◽  
Jeffrey P. MacKeigan
Keyword(s):  
Tissue Distribution ◽  
Lupus Erythematosus ◽  
Degradation Process ◽  
The Novel ◽  
Multiple Cancer ◽  
Chromatography Tandem Mass Spectrometry ◽  
Tumor Tissues ◽  
Liquid Chromatography Tandem Mass ◽  
Autophagy Inhibition

ABSTRACTHydroxychloroquine (HCQ) is a 4-aminoquinoline molecule used for the treatment of malaria, and more recently to treat rheumatoid arthritis, systemic lupus erythematosus, and cancer. In cancer, HCQ is being used in multiple cancer clinical trials as an inhibitor of autophagy, a cytosolic degradation process employing the lysosome. Importantly, more potent lysosomotropic agents are being developed as autophagy inhibitors. Additional studies revealed that acridine-based compounds such as quinacrine (QN) increased potency over the 4-aminoquinoline HCQ. In line with these initial discoveries, we performed chemical synthesis of acridine-based compounds and screened for potent autophagy inhibition. The novel compound VATG-027 increased potency and cytotoxicity over HCQ in osteosarcoma and melanoma cell lines, supporting further investigation in vivo. Here, we developed a liquid chromatography tandem mass spectrometry (LC-MS/MS) method to investigate HCQ, QN, and VATG-027 compound concentrations across various tissue types in mice. This method detected compound concentrations in whole blood, lung, liver, kidney, and subcutaneous tumor tissues. Concentrations of HCQ, QN, and VATG-027 varied within and between tissue types, suggesting unique tissue distribution profiles for 4-aminoquinoline and acridine compounds.

TISSUE DISTRIBUTION OF THE NOVEL MACROLIDE IMMUNOSUPPRESSANT SDZ-RAD: INTERACTION WITH CYCLOSPORINE

1999 ◽  
Vol 21 (4) ◽  
pp. 445
Author(s):  
N. Serkova ◽  
B. Hausen ◽  
R. E. Morris ◽  
L. Z. Benet ◽  
U. Christians
Keyword(s):  
Tissue Distribution ◽  
The Novel

Profile of disposition, tissue distribution and excretion of the novel anti-human immunodeficiency virus (HIV) agent W-1 in rats

2016 ◽  
Vol 39 (7) ◽  
pp. 970-977 ◽  
Author(s):  
Ying-Yuan Lu ◽  
Xiao-Wei Wang ◽  
Xin Wang ◽  
Wen-Bing Dai ◽  
Qiang Zhang ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Tissue Distribution ◽  
The Novel ◽  
Immunodeficiency Virus

scholarly journals Bioavailability, tissue distribution, and excretion characteristics of the novel carbonic anhydrase inhibitor tolsultazolamide in rats

2013 ◽  
Vol 35 (2) ◽  
pp. 275-282 ◽  
Author(s):  
Jin-da Wang ◽  
Yong-ping Shi ◽  
Jing Yin ◽  
Zhi-yuan Pan ◽  
Wen-yu Cui ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Tissue Distribution ◽  
Carbonic Anhydrase Inhibitor ◽  
The Novel

scholarly journals A Novel Co-Crystal of Bexarotene and Ligustrazine Improves Pharmacokinetics and Tissue Distribution of Bexarotene in SD Rats

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 906
Author(s):  
Shuyue Ren ◽  
Lingtai Jiao ◽  
Shiying Yang ◽  
Li Zhang ◽  
Junke Song ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Neurological Disorders ◽  
Cell Lymphoma ◽  
Neurological Diseases ◽  
Absolute Bioavailability ◽  
The Novel ◽  
Pharmaceutical Ingredients ◽  
Sd Rats ◽  
Fda Approval ◽  
Enhanced Solubility

Bexarotene (BEX), a specific retinoic acid X receptor (RXR) agonist granted by Food and Drug Administration (FDA) approval for the clinical treatment of T cell lymphoma, has now been found to exert pharmacological effects in the nervous system, with low bioavailability and poor cerebral distribution limiting its application in treatment on neurological disorders. Pharmaceutical co-crystal was a helpful method to improve the bioavailability and tissue distribution of active pharmaceutical ingredients (APIs). Here, 2bexarotene-ligustrazine (2BEX-LIG), a novel co-crystal system of BEX and ligustrazine (LIG) of which with BEX is an API, was constructed with satisfactory stability and enhanced solubility. The pharmacokinetics characteristics of BEX were detected, and the results showed that the absolute bioavailability and the cerebral concentration of BEX in rats administrated with 2BEX-LIG were enhanced from 22.89% to 42.86% and increased by 3.4-fold, respectively, compared with those in rats administrated an equivalent of BEX. Hence, our present study indicated that the novel co-crystal of 2BEX-LIG contributed to improving BEX oral bioavailability and cerebral distribution, thereby providing significant advantages for clinical application of brain tumors and other neurological diseases.

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