In 2019,ACS Chemical Neuroscience included an article by Jorg, Manuela; van der Westhuizen, Emma T.; Khajehali, Elham; Burger, Wessel A. C.; White, Jonathan M.; Choy, Kwok H. C.; Tobin, Andrew B.; Sexton, Patrick M.; Valant, Celine; Capuano, Ben; Christopoulos, Arthur; Scammells, Peter J.. SDS of cas: 89466-08-0. The article was titled 《6-phenylpyrimidin-4-ones as positive allosteric modulators at the M1 mAChR: the determinants of allosteric activity》. The information in the text is summarized as follows:
Targeting allosteric sites of the M1 muscarinic acetylcholine receptor (mAChR) is an enticing approach to overcome the lack of receptor subtype selectivity observed with orthosteric ligands. This is a promising strategy for obtaining novel therapeutics to treat cognitive deficits observed in Alzheimer’s disease and schizophrenia, while reducing the peripheral side effects such as seen in the current treatment regimes, which are non-subtype selective. We previously described compound I, the first pos. allosteric modulator (PAM) of the M1 mAChR based on a 6-phenylpyrimidin-4-one scaffold, which has been further developed in this study. Herein, we present the synthesis, characterization, and pharmacol. evaluation of a series of 6-phenylpyrimidin-4-ones with modifications to the 4-(1-methylpyrazol-4-yl)benzyl pendant. Selected compounds were further profiled in terms of their allosteric affinity, cooperativity with acetylcholine (ACh), and intrinsic efficacy. Addnl., I and II were tested in mouse primary cortical neurons, displaying various degrees of intrinsic agonism and potentiation of the acetylcholine response. Overall, the results suggest that the pendant moiety is important for allosteric binding affinity and the direct agonistic efficacy of the 6-phenylpyrimidin-4-one based M1 mAChR PAMs. In the experimental materials used by the author, we found 2-Hydroxyphenylboronic acid(cas: 89466-08-0SDS of cas: 89466-08-0)
2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. SDS of cas: 89466-08-0
Referemce:
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