199655-36-2 Usage
Uses
CP 465022 is an AMPA antagonist.
Biological Activity
cp 465022 hydrochloride is a potent and selective antagonist of ampa receptor with ic50 value of 25 nm [1].the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (ampa receptor) is an ionotropic transmembrane receptor for glutamate and mediates fast synaptic transmission in the central nervous system. ampa receptors are oligomeric assemblies of four protein subunits, glur1-4.cp 465022 hydrochloride is a noncompetitive and selective ampa receptor antagonist. in rat cortical neurons, cp-465022 inhibited currents induced by kainate (100 μm) with ic50 value of 25 nm and completely inhibited at concentration up to 3.2 μm. in hnt human teratocarcinoma cells, cp-465022 inhibited kainate-induced currents with ic50 value of 15 nm, which was mediated by ampa receptors. in cultured cortical neurons stimulated by kainate, cp-465022 dose-dependently inhibited kainate-induced responses by 54% and 88% at 10 nm and 100 nm, respectively [1]. in hek cells expressing the nav1.6 channel, cp465022 dose-dependently inhibited nav1.6-mediated persistent current [2].in rats after stimulation of schaeffer collateral/commissural pathway, cp-465022 reversibly inhibited the evoked population spike amplitude in the ca1 region. in pentylenetetrazole-induced seizure rats, cp-465022 dose-dependently reduced the incidence of tonic seizures, clonic seizures and lethality. cp-465022 inhibited vertical and horizontal locomotor activity with ed50 values of 6.6 and 11.9 mg/kg, respectively [3].
references
[1]. lazzaro jt, paternain av, lerma j, et al. functional characterization of cp-465,022, a selective, noncompetitive ampa receptor antagonist. neuropharmacology, 2002, 42(2): 143-153.[2]. welch nc, lin w, juranka pf, et al. traditional ampa receptor antagonists partially block na v1.6-mediated persistent current. neuropharmacology, 2008, 55(7): 1165-1171. [3]. menniti fs, buchan am, chenard bl, et al. cp-465,022, a selective noncompetitive ampa receptor antagonist, blocks ampa receptors but is not neuroprotective in vivo. stroke, 2003, 34(1): 171-176.
Check Digit Verification of cas no
The CAS Registry Mumber 199655-36-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,9,9,6,5 and 5 respectively; the second part has 2 digits, 3 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 199655-36:
(8*1)+(7*9)+(6*9)+(5*6)+(4*5)+(3*5)+(2*3)+(1*6)=202
202 % 10 = 2
So 199655-36-2 is a valid CAS Registry Number.
199655-36-2Relevant articles and documents
Measurement of atropisomer racemization kinetics using segmented flow technology
Davoren, Jennifer E.,Bundesmann, Mark W.,Yan, Qi T.,Collantes, Elizabeth M.,Mente, Scot,Nason, Deane M.,Gray, David L.
supporting information; experimental part, p. 433 - 435 (2012/07/14)
When stable atropisomers are encountered by drug discovery teams, they can have important implications due to potential differences in their biological activity, pharmacokinetics, and toxicity. Knowledge of an atropisomer's activation parameters for interconversion is required to facilitate informed decisions on how to proceed. Herein, we communicate the development of a new method for the rapid measurement of atropisomer racemization kinetics utilizing segmented flow technology. This method leverages the speed, accuracy, low sample requirement, safety, and semiautomated nature of flow instrumentation to facilitate the acquisition of kinetics data required for experimentally probing atropisomer activation parameters. Measured kinetics data obtained for the atropo isomerization of AMPA antagonist CP-465021 using segmented flow and traditional thermal methods were compared to validate the method.
