Formula: C9H9BrO2, With the volume and accessibility of scientific research increasing across the world, it has never been more important to continue building the reputation for quality and ethical publishing we’ve spent the past two centuries establishing. Type is Article, and a compound is mentioned, 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, introducing its new discovery.
beta-Adrenoceptor antagonists boast a 50-year use for symptomatic control in numerous cardiovascular diseases. One might expect highly selective antagonists are available for the human beta-adrenoceptor subtype involved in these diseases, yet few truly beta1-selective molecules exist. To address this clinical need, we re-evaluated LK 204-545 (1),(1) a selective beta1-adrenoceptor antagonist, and discovered it possessed significant partial agonism. Removal of 1’s aromatic nitrile afforded 19, a ligand with similar beta1-adrenoceptor selectivity and partial agonism (log KD of -7.75 and -5.15 as an antagonist of functional beta1- and beta2-mediated responses, respectively, and 34% of the maximal response of isoprenaline (beta1)). In vitro beta-adrenoceptor selectivity and partial agonism of 19 were mirrored in vivo. We designed analogues of 19 to improve affinity, selectivity, and partial agonism. Although partial agonism could not be fully attenuated, SAR suggests that an extended alkoxyalkoxy side chain, alongside substituents at the meta- or para-positions of the phenylurea, increases ligand affinity and beta1-selectivity.
The catalyzed pathway has a lower Ea, but the net change in energy that results from the reaction is not affected by the presence of a catalyst. In my other articles, you can also check out more blogs about 214894-89-0