《Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist for Use in Central Nervous System Disease Models》 was written by Amaradhi, Radhika; Banik, Avijit; Mohammed, Shabber; Patro, Vidyavathi; Rojas, Asheebo; Wang, Wenyi; Motati, Damoder Reddy; Dingledine, Ray; Ganesh, Thota. Recommanded Product: 2-Hydroxyphenylboronic acid And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
Activation of prostanoid EP2 receptor exacerbates neuroinflammatory and neurodegenerative pathol. in central nervous system diseases such as epilepsy, Alzheimer’s disease, and cerebral aneurysms. A selective and brain-permeable EP2 antagonist will be useful to attenuate the inflammatory consequences of EP2 activation and to reduce the severity of these chronic diseases. We recently developed a brain-permeable EP2 antagonist 1 (TG6-10-1), which displayed anti-inflammatory and neuroprotective actions in rodent models of status epilepticus. However, this compound exhibited moderate selectivity to EP2, a short plasma half-life in rodents (1.7 h) and low aqueous solubility (27μM), limiting its use in animal models of chronic disease. With lead-optimization studies, we have developed several novel EP2 antagonists with improved water solubility, brain penetration, high EP2 potency, and selectivity. These novel inhibitors suppress inflammatory gene expression induced by EP2 receptor activation in a microglial cell line, reinforcing the use of EP2 antagonists as anti-inflammatory agents. After reading the article, we found that the author used 2-Hydroxyphenylboronic acid(cas: 89466-08-0Recommanded Product: 2-Hydroxyphenylboronic acid)
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. Recommanded Product: 2-Hydroxyphenylboronic acid
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