Results 91 to 100 of about 2,283,209 (217)

Influence of Acupuncture at Zusanli point on Function of 5-HT and M Recepter in Rat's Brain and Spleen

针刺研究, 1994
5-HT and muscarine (M) recepters total binding capacities (Rt) in different brain areas and spleen were determined using recepter radioligand binding assay (RLBA) after needling zusanli of rats.
莫启忠, 宫斌, 方军, 李建萍, 黄巨涛, 陈坤华, 匡兴伟, 王菊美   +7 more
doaj   +2 more sources

Multitarget Drug Design for Cardiovascular Disease: Bridging Chemistry and Medicine

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
Many pathophysiological pathways associated with cardiovascular diseases involve multiple drug targets. This article reviews recent advances in the development of pharmacological compounds capable of simultaneously modulating multiple mechanisms. Multitarget drugs offer a promising therapeutic approach for complex cardiovascular disorders, including ...
Gyuzel Y. Mitronova, Vladimir N. Belov, Constanze Schmidt, Stephan E. Lehnart   +3 more
wiley   +1 more source

A Selectfluor‐based Polonovski Rearrangement Leading to Novel Entities for Synthetic and Medicinal Applications

Chemistry – A European Journal, Volume 32, Issue 38, 13 October 2026.
Starting from carboxylic acids and Selectfluor‐derivatives, functionalized diazabicyclooctanes can be obtained via a novel Polonovski‐type rearrangement proceeding under mild reaction conditions. Besides their use in organic synthesis the unique structure and reactivity of the rearrangement products enables applications in medicinal chemistry ...
Jakob Kuhn, Susanne Gradl, Vanessa Osterloh, Peter Gmeiner, Harald Hübner, Markus R. Heinrich   +5 more
wiley   +1 more source

Measuring substrate binding and affinity of purified membrane transport proteins using the scintillation proximity assay

, 2012
The scintillation proximity assay (SPA) is a rapid radioligand binding assay. Upon binding of radioactively labeled ligands (here L-[(3)H]arginine or D-[(3)H]glucose) to acceptor proteins immobilized on fluoromicrospheres (containing the scintillant), a ...
Harder, Daniel, Fotiadis, Dimitrios, Harder D, Fotiadis, Dimitrios José, Fotiadis D   +4 more
core   +1 more source

Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione- Based Compounds

Molecules, 2014
The anticonvulsant activity of several 1,2,4-triazole-3-thione derivatives on mouse maximal electroshock-induced seizures was tested in this study.
Tomasz Plech, Barbara Kaproń, Jarogniew J. Łuszczki, Monika Wujec, Agata Paneth, Agata Siwek, Marcin Kołaczkowski, Maria Żołnierek, Gabriel Nowak   +8 more
doaj   +1 more source

In Silico to In Cerebro—Development of the Orexin Receptor Antagonist “Photorexant” for Photomodulation In Vitro and in Mouse Brains

Angewandte Chemie International Edition, Volume 65, Issue 42, 12 October 2026.
Following a structure‐based design approach, photoswitchable derivatives of the FDA‐approved drug suvorexant were designed, docked, synthesized, and characterized pharmacologically at the orexin 1 and 2 receptors (OX1R and OX2R). Optimized “photorexant” showed up to an 11‐fold difference in IC50 between photoisomers, enabled dynamic and reversible ...
Marcus Angermann, Marie H. Deventer, Vicente Ledesma‐Martin, Nuno Martinho, Alix Flake, Silvia Mori, Angel Nuñez, Jaime Pignatelli, Rita C. Guedes, Christophe P. Stove, Michael Decker   +10 more
wiley   +1 more source

Intact Cell Binding for In Vitro Prediction of Sedative and Non-sedative Histamine H1–Receptor Antagonists Based on Receptor Internalization

Journal of Pharmacological Sciences, 2008
We evaluated changes in the binding properties of sedative and non-sedative histamine H1–receptor antagonists induced by internalization of H1 receptors in intact human U373 MG astrocytoma cells.
Shigeru Hishinuma, Yuko Sato, Yusuke Kobayashi, Hiroshi Komazaki, Masaki Saito   +4 more
doaj   +1 more source

Structural basis for saxitoxin congener binding and neutralization by anuran saxiphilins

Nature Communications
Dinoflagellates and cyanobacteria produce saxitoxin (STX) and ~50 congeners that disrupt bioelectrical signals by blocking voltage-gated sodium channels (NaVs). Consuming seafood carrying these toxins causes paralytic shellfish poisoning (PSP).
Sandra Zakrzewska, Samantha A. Nixon, Zhou Chen, Holly S. Hajare, Elizabeth R. Park, John V. Mulcahy, Kandis M. Arlinghaus, Eduard Neu, Kirill Konovalov, Davide Provasi, Tod A. Leighfield, Marta Filizola, J. Du Bois, Daniel L. Minor   +13 more
doaj   +1 more source

Development and In Vitro Characterization of [³H]GMC-058 as Radioligand for Imaging Parkinsonian-Related Proteinopathies

Cells
The molecular imaging of α-synuclein (α-syn) pathology in Parkinson’s disease (PD) and related movement disorders is a clinically unmet need. The aim of this study was to discover and characterize in vitro a radioligand for imaging α-syn pathology.
Andrea Varrone, Vasco C. Sousa, Manolo Mugnaini, Sandra Biesinger, Gunnar Nordvall, Lee Kingston, Ileana Guzzetti, Charles S. Elmore, Dan Sunnemark, Dinahlee Saturnino Guarino, Sjoerd J. Finnema, Magnus Schou   +11 more
doaj   +1 more source

Assessment of Novel Muscarinic Acetylcholine Receptors in Rat Cerebral Cortex by a Tissue Segment Binding Method

Journal of Pharmacological Sciences, 2010
Muscarinic acetylcholine receptors (mAChRs) of rat cerebral cortex were evaluated using a tissue segment radioligand binding assay. [3H]-Quinuclidinyl benzilate (QNB, a hydrophobic ligand) specifically bound to mAChRs in the cortex segments.
Kung-Shing Lee, Atsushi Nishimune, Hatsumi Yoshiki, Abu Syed Md Anisuzzaman, Fumiko Suzuki, Mao-Hsien Wang, Juei-Tang Cheng, Ikunobu Muramatsu   +7 more
doaj   +1 more source