On May 13, 1994, Kulagowski, Janusz J.; Baker, Raymond; Curtis, Neil R.; Mawer, Ian M.; Moseley, Angela M.; Ridgill, Mark P.; Rowley, Michael; Stansfield, Ian; Leeson, Paul D. published an article.HPLC of Formula: 142327-44-4 The title of the article was 3′-(Arylmethyl)- and 3′-(Aryloxy)-3-phenyl-4-hydroxyquinolin- 2(1H)-ones: Orally Active Antagonists of the Glycine Site on the NMDA Receptor. And the article contained the following:
Antagonists acting at the glycine site of the N-methyl-D-aspartate (NMDA) receptor are expected to have considerable therapeutic potential in a variety of disorders of the central nervous system. However in vivo studies with currently available compounds are severely compromised by the poor activities observed following systemic administration. The authors have previously followed a strategy of carboxyl replacement in known antagonists to provide 7-chloro-4-hydroxy-3-phenylquinolin-2(1H)-one (I). The authors now show that optimization of I by substitution of the 3-Ph with selected hydrophobic 3′-substituents yields a 100-fold improvement of in vitro affinity (IC50 values for displacement of [3H]L-689,560 binding and Kb values in cortical slice), combined with potent systemic anticonvulsant activity in the DBA/2 mouse audiogenic seizure model (ED50 values obtained after i.p. (i.p.) and oral (p.o.) administration). The following 3′-derivatives of I were identified: 3′-(4-methoxybenzyl)- (L-703,717), IC50 4.5 nM, Kb 25 nM, ED50 0.7 mg/kg i.p. and 0.9 mg/kg p.o.; 3′-(4-(1-methoxy)methoxybenzyl)- (L-708,541), IC50 2.2 nM, Kb 3.2 nM, ED50 0.5 mg/kg i.p. and 0.9 mg/kg p.o.; 3′-phenoxy- (L-701,324), IC50 2.8 nM, Kb 28 nM, ED50 0.9 mg/kg i.p. and 0.9 mg/kg p.o.; and 3′-(3-thienyloxy)- (L-705,022), IC50 1.4 nM, Kb 5.0 nM< ED50 0.8 mg/kg i.p. and 0.8 mg/kg p.o. These new glycine antagonists are the most potent yet described, both in vitro and in vivo, and are the first with oral activity. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).HPLC of Formula: 142327-44-4
The Article related to nmda receptor glycine site antagonist hydroxyphenylquinolone, anticonvulsant phenylhydroxyquinolone preparation, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.HPLC of Formula: 142327-44-4
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