Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C29H32N4.CH4O3S |
| Molecular Weight | 532.697 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(O)(=O)=O.CC1=C(CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4)N=C(N1)C5=CC=C(C)C=C5
InChI
InChIKey=CGPIUYHUELMXMK-UHFFFAOYSA-N
InChI=1S/C29H32N4.CH4O3S/c1-22-13-15-26(16-14-22)29-30-23(2)27(31-29)21-32-17-19-33(20-18-32)28(24-9-5-3-6-10-24)25-11-7-4-8-12-25;1-5(2,3)4/h3-16,28H,17-21H2,1-2H3,(H,30,31);1H3,(H,2,3,4)
| Molecular Formula | C29H32N4 |
| Molecular Weight | 436.5912 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | CH4O3S |
| Molecular Weight | 96.106 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Lifarizine is a use- and voltage-dependent antagonist of human voltage sensitive sodium currents. Lifarizine inhibited both the plateau and the spike phases of the Ca2+ increases suggesting that, in addition to its known sodium channel blocking properties, it may also inhibit more than one class of calcium channel in the synaptosomes. Lifarizine reduced both infarct area and volume in the mouse with middle cerebral artery occlusion. Lifarizine was in phase II for the treatment of stroke but this investigation was discontinued.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Reasons why stroke trials underestimate the neuroprotective effects of drugs. | 2002-01 |
|
| Frequency-independent blockade of cardiac Na+ channels by riluzole: comparison with established anticonvulsants and class I anti-arrhythmics. | 2000-05-05 |
|
| Focal cerebral ischemia in the mouse: hypothermia and rapid screening of drugs. | 1998-02 |
|
| Inhibition by lifarizine of intracellular Ca2+ rises and glutamate exocytosis in depolarized rat cerebrocortical synaptosomes and cultured neurones. | 1996-05 |
|
| Neuroprotective efficacy of lifarizine (RS-87476) in a simplified rat survival model of 2 vessel occlusion. | 1995-12 |
|
| Efficacy and tolerability of lifarizine in acute ischemic stroke. A pilot study. Lifarizine Study Group. | 1995-09-15 |
|
| Selectivity of the neuroprotective agent lifarizine. | 1995-09 |
|
| MR evaluation of calcium entry blockers with putative cerebroprotective effects in acute cerebral ischaemia. | 1990 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9502174
Single dose 100 mg/kg
Route of Administration:
Other
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:25:34 GMT 2025
by
admin
on
Mon Mar 31 21:25:34 GMT 2025
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| Record UNII |
AKZ5B7DOP6
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| Record Status |
Validated (UNII)
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| Record Version |
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AKZ5B7DOP6
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130565-83-2
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PARENT -> SALT/SOLVATE |