One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, SDS of cas: 90806-60-3, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 90806-60-3, Name is 5-Methoxyisoquinoline-1-carbonitrile, molecular formula is C11H8N2O
Structure-activity study of 2,3-benzodiazepin-4-ones noncompetitive AMPAR antagonists: Identification of the 1-(4-amino-3-methylphenyl)-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-one as neuroprotective agent
In the search for AMPA receptor (AMPAR) antagonists, 2,3-benzodiazepines represent a family of specific noncompetitive antagonists with anticonvulsant and neuroprotective properties. We have previously shown that 2,3-benzodiazepin-4-ones possess marked anticonvulsant properties and high affinity for the noncompetitive binding site of the AMPAR complex. In this paper, we report the synthesis and pharmacological characterization of a full set of 2,3-benzodiazepin-4-ones in order to better define the structure-activity relationship (SAR) of this class of compounds. Binding assays and functional tests were performed to evaluate the antagonistic activity at the AMPARs. Through these results we have identified a potent AMPAR antagonist, 1-(4-amino-3-methylphenyl)-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-one (5c). This compound noncompetitively inhibited AMPAR-mediated toxicity in primary mouse hippocampal cultures with an IC50 of 1.6 muM and blocked kainate-induced calcium influx in rat cerebellar granule cells with an IC50 of 6.4 muM. Thus, 5c has the in vitro potential as therapeutic drug in the treatment of various neurological disorders.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. SDS of cas: 90806-60-3, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 90806-60-3, in my other articles.
Reference£º
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem