119431-25-3 Usage
Description
N-Methyl-D-aspartate (NMDA) receptors are calcium permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents. It is selective for NR2B subunit-containing receptors (IC50 = 1 μM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits. Eliprodil also avidly binds σ1 and σ2 sites (Kis = 0.013 and 0.63 μM, respectively). It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion. Eliprodil can also have proarrhythmic actions in hearts under normal conditions.
Uses
Eliprodil is a noncardiac drug with neuroprotective properties. It is also a N-Methyl-D-aspartate receptor (NMDAR) antagonist.
Biological Activity
Different sources of media describe the Biological Activity of 119431-25-3 differently. You can refer to the following data:
1. Non-competitive NMDA receptor antagonist that acts at the polyamine modulatory site. Selective for NR2B- over NR2A- and NR2C-containing receptors (IC 50 values are 1, > 100 and > 100 μ M respectively). Also σ 1 ligand (K i = 0.013 μ M). Antagonizes neuronal voltage-gated Ca 2+ channels and selectively inhibits the rapid component of the delayed rectifier K + current (I Kr ). Neuroprotective.
2. Eliprodil (SL-820715) is a non-competitive, NR2B-selective NMDA antagonist with IC50 of 1 μM. Its IC50 is greater than 100 μM for receptors containing NR2A and NR2C.
Check Digit Verification of cas no
The CAS Registry Mumber 119431-25-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,9,4,3 and 1 respectively; the second part has 2 digits, 2 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 119431-25:
(8*1)+(7*1)+(6*9)+(5*4)+(4*3)+(3*1)+(2*2)+(1*5)=113
113 % 10 = 3
So 119431-25-3 is a valid CAS Registry Number.
InChI:InChI=1/C20H23ClFNO/c21-18-5-3-17(4-6-18)20(24)14-23-11-9-16(10-12-23)13-15-1-7-19(22)8-2-15/h1-8,16,20,24H,9-14H2
119431-25-3Relevant articles and documents
Synthesis and resolution of racemic eliprodil and evaluation of the enantiomers of eliprodil as NMDA receptor antagonists
Pabel, Joerg,Hoefner, Georg,Wanner, Klaus Th.
, p. 1377 - 1380 (2000)
A short synthesis of the NMDA receptor antagonist (rac)-Eliprodil (9) and its resolution into the enantiomers by chiral HPLC is described. The enantiomers (R)-9 and (S)-9 were found to exhibit markedly different affinities for NR2B subunit containing NMDA
Method for treating diseased-related or drug-induced dyskinesias
-
, (2008/06/13)
Dyskinesias in humans are treated by administering a therapeutically effective dose of an NR1A/2B site-selective NMDA receptor antagonist compound to a human suffering therefrom.
