255896-07-2Relevant academic research and scientific papers
The discovery and synthesis of novel adenosine receptor (A2A) antagonists
Matasi, Julius J.,Caldwell, John P.,Hao, Jinsong,Neustadt, Bernard,Arik, Leyla,Foster, Carolyn J.,Lachowicz, Jean,Tulshian, Deen B.
, p. 1333 - 1336 (2005)
In high throughput screening of our file compounds, a novel structure 1 was identified as a potent A2A receptor antagonist with no selectivity over the A1 adenosine receptor. The structure-activity relationship investigation using 1 as a template lead to identification of a novel class of compounds as potent and selective antagonists of A2A adenosine receptor. Compound 26 was identified to be the most potent A2A receptor antagonist (Ki = 0.8 nM) with 100-fold selectivity over the A1 adenosine receptor.
Reevaluation of fenpropimorph as a σ receptor ligand: Structure-affinity relationship studies at human σ1 receptors
Sguazzini, Elena,Schmidt, Hayden R.,Iyer, Kavita A.,Kruse, Andrew C.,Dukat, Ma?gorzata
, p. 2912 - 2919 (2017/05/31)
Fenpropimorph (1) is considered a “super high-affinity” σ1 receptor ligand (Ki?=?0.005?nM for guinea pig σ1 receptors). Here, we examine the binding of 1 and several of its deconstructed analogs at human σ1 (hσ
Biaryl derived amide modulators of vanilloid VR1 receptor
-
Page/Page column 30, (2010/11/24)
The invention is directed to novel vanilloid receptor type 1 (VR1) ligands. More specifically, the invention relates to novel biaryl-derived amides that are potent antagonists or agonists of VR1. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
LIGANDS AND CATALYSTS FOR PRODUCING ELASTOMERIC PROPYLENE POLYMERS
-
, (2008/06/13)
A ligand useful to form a metallocene olefin polymerization catalyst comprises:wherein at least R3 and R4 are substituents having at least a bulk of a t-butyl group and, optionally, wherein R1 or R2 may be a bulky substituent group.
