Results 21 to 30 of about 2,998,144 (312)

Identification of a domain which affects kinetics and antagonistic potency of clozapine at 5-HT3 receptors. [PDF]

, 2009
The widely used atypical antipsychotic clozapine is a potent competitive antagonist at 5-HT(3) receptors which may contribute to its unique psychopharmacological profile. Clozapine binds to 5-HT(3) receptors of various species.
Gerhard Rammes, Caroline Nothdurfter, Tanasic, S., Rammes, G., Rupprecht, R., Eisensamer, Brigitte, Zieglgänsberger Walter, Christine Hosp, Tanasic, Sascha, Hosp Christine, Walter Zieglgänsberger, Rupprecht Rainer, Rammes, Gerhard, Sascha Tanasic, Hosp, C., Rammes Gerhard, Nothdurfter, C., Tanasic Sascha, Rupprecht, Rainer, Nothdurfter Caroline, Brigitte Eisensamer, Eisensamer, B., Zieglgänsberger, Walter, Zieglgänsberger, W., Hosp, Christine, Rainer Rupprecht, Nothdurfter, Caroline, Eisensamer Brigitte   +27 more
core   +2 more sources

GRK Mediates μ-Opioid Receptor Plasma Membrane Reorganization

Frontiers in Molecular Neuroscience, 2019
Differential regulation of the μ-opioid receptor (MOP) has been linked to the development of opioid tolerance and dependence which both limit the clinical use of opioid analgesics.
Arisbel B. Gondin, Arisbel B. Gondin, Arisbel B. Gondin, Michelle L. Halls, Meritxell Canals, Meritxell Canals, Meritxell Canals, Stephen J. Briddon, Stephen J. Briddon   +8 more
doaj   +1 more source

Distinct pharmacological and functional properties of NMDA receptors in mouse cortical astrocytes [PDF]

, 2011
Background and purpose Astrocytes of the mouse neocortex express functional NMDA receptors which are not blocked by Mg2+ions. However, study of the pharmacological profile of glial NMDARs and their subunit composition is far from complete ...
Lalo, Ulyana, Pankratov, Yuriy, Palygin, Oleg, Oleg Palygin, Ulyana Lalo, Yuriy Pankratov   +5 more
core   +1 more source

Visualizing Ligand Binding to a GPCR In Vivo Using NanoBRET

iScience, 2018
Summary: The therapeutic action of a drug depends on its ability to engage with its molecular target in vivo. However, current drug discovery strategies quantify drug levels within organs rather than determining the binding of drugs directly to their ...
Diana C. Alcobia, Alexandra I. Ziegler, Alexander Kondrashov, Eleonora Comeo, Sarah Mistry, Barrie Kellam, Aeson Chang, Jeanette Woolard, Stephen J. Hill, Erica K. Sloan   +9 more
doaj   +1 more source

Receptor-mediated targeted drug delivery systems for treatment of inflammatory bowel disease: Opportunities and emerging strategies

Acta Pharmaceutica Sinica B, 2021
Inflammatory bowel disease (IBD) is a chronic intestinal disease with painful clinical manifestations and high risks of cancerization. With no curative therapy for IBD at present, the development of effective therapeutics is highly advocated.
Peng Liu, Caifang Gao, Hongguo Chen, Chi Teng Vong, Xu Wu, Xudong Tang, Shengpeng Wang, Yitao Wang   +7 more
doaj   +1 more source

Anticancer drug delivery with transferrin targeted polymeric chitosan vesicles [PDF]

, 2004
The study reports the initial biological evaluation of targeted polymeric glycol chitosan vesicles as carrier systems for doxorubicin (Dox). Transferrin (Tf) was covalently bound to the Dox-loaded palmitoylated glycol chitosan (GCP) vesicles using ...
Dufès, Christine, Couet, William, Schätzlein, Andreas G., Uchegbu, I.F., Olivier, Jean-Christophe, Muller, Jean-Marc   +5 more
core   +4 more sources

Structure-Function Analyses of Human Bitter Taste Receptors—Where Do We Stand?

Molecules, 2020
The finding that bitter taste receptors are expressed in numerous tissues outside the oral cavity and fulfill important roles in metabolic regulation, innate immunity and respiratory control, have made these receptors important targets for drug discovery.
Maik Behrens, Florian Ziegler
doaj   +1 more source

Ganfule capsule alleviates AFB1-induced toxic liver injury via inhibiting oxidative stress, inflammatory response, and apoptosis

Ecotoxicology and Environmental Safety
Aflatoxins, particularly aflatoxin B1 (AFB1), are widely present in the environment and pose a significant risk to food safety. However, no specific drugs are available for AFB1-induced toxic liver injury. Ganfule (GFL) is a traditional Chinese medicine (
Pan Li, Yujia Cao, Yifan Hou, Jianhua Zhang, Linlin Zhang, Ziang Li, Hongtao Xu, Wenbo Zhang, Zhenhua Zhao, Xiaobo Nie, Junqing Hou   +10 more
doaj   +1 more source

Pregnane Xenobiotic Receptors and Their Effect on Drug Elimination from the Organism

Prague Medical Report, 2013
Nuclear receptors are intracellular proteins which, having been activated by their more or less specific ligands, regulate (usually increase) the transcription of target genes.
Martin Šíma, I. Netíková, O. Slanař
doaj   +1 more source

Molecular Simulations and Drug Discovery of Adenosine Receptors

Molecules, 2022
G protein-coupled receptors (GPCRs) represent the largest family of human membrane proteins. Four subtypes of adenosine receptors (ARs), the A1AR, A2AAR, A2BAR and A3AR, each with a unique pharmacological profile and distribution within the tissues in ...
Jinan Wang, Apurba Bhattarai, Hung N. Do, Sana Akhter, Yinglong Miao   +4 more
doaj   +1 more source