Results 91 to 100 of about 3,259,253 (212)

Tuning the Triazolotriazine Scaffold Toward Selective A3 Adenosine Receptor Antagonists: From Molecular Recognition to Neuroprotection

ChemMedChem, Volume 21, Issue 20, 28 October 2026.
Structure‐based optimization of the triazolo‐triazine scaffold afforded highly potent and selective adenosine A3 receptor antagonists. Replacement of the classical 2‐furyl group with phenyl‐based substituents markedly improved A3 receptor affinity and selectivity.
Veronika Kost, Filippo Prencipe, Federica Panozzi, Veronica Salmaso, Sonja Kachler, Karl‐Norbert Klotz, Elisabetta Coppi, Simone Adorinni, Stefano Moro, Anna Maria Pugliese, Stephanie Federico, Giampiero Spalluto, Tatiana Da Ros   +12 more
wiley   +1 more source

The measurement of testosterone and oestradiol-17[beta] using iodinated tracers and incorporating an affinity chromatography extraction procedure [PDF]

, 1985
The development of sensitive radioimmunoassays (RIA) for testosterone and oestradiol-17[beta], utilising 125I-radioligands, is described. Use of an homologous bridge at the same site of attachment, for both the radioligand and the steroid-carrier protein
Baxter, G., McBride, D., Shaw, M. P. K., Webb, R., Nordblom, Gerald D.   +4 more
core   +1 more source

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

On the kinetic features of orexin receptor antagonists at orexin receptors, transduction systems and receptor binding

Medicine in Drug Discovery
Orexin receptor antagonists are on the market or under development for the treatment of insomnia and a number of other neuropsychiatric disorders. Currently, suvorexant, lemborexant and daridorexant, three dual orexin receptor antagonists (DORAs) have ...
Daniel Hoyer, Laura H. Jacobson
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

Dopamine D2-like receptors on human peripheral blood lymphocytes: a radioligand binding assay and immunocytochemical study

, 1999
1. Peripheral blood lymphocytes express dopamine D1-like and D2-like receptors which were investigated using radioligand binding assay and molecular biology techniques.
AMENTA, Francesco, E. BRONZETTI, L. FELICI, A. RICCI, TAYEBATI, Seyed Khosrow   +4 more
core  

Establishing a Receptor Binding Assay for Ciguatoxins: Challenges, Assay Performance and Application

Toxins
Ciguatera, a global issue, lacks adequate capacity for ciguatoxin analysis in most affected countries. The Caribbean region, known for its endemic ciguatera and being home to a majority of the global small island developing states, particularly needs ...
Lisbet Díaz-Asencio, Donaida Chamero-Lago, Gabriel L. Rojas-Abrahantes, Carlos M. Alonso-Hernández, Marie-Yasmine Dechraoui Bottein   +4 more
doaj   +1 more source

Synthesis and in vitro evaluation of novel compounds and discovery of a promising iodine-125 radioligand for purinergic P2X7 receptor (P2X7R)

The purinergic P2X ligand-gated ion channel 7 receptor (P2X7R) plays a critical role in various inflammatory processes and other diseases. Fast determination of compounds P2X7R binding potency and discovery of a promise PET radiotracer for imaging P2X7R ...
Qiu, Lin, Tu, Zhude, Egan, Terrance M, Perlmutter, Joel S, Wang, Jinzhi, Tewari, Manju, Rensing, Derek T   +6 more
core   +1 more source

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