Details
Stereochemistry | ACHIRAL |
Molecular Formula | C29H32N4 |
Molecular Weight | 436.5912 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4)N=C(N1)C5=CC=C(C)C=C5
InChI
InChIKey=HTDFEXRUDGWNHA-UHFFFAOYSA-N
InChI=1S/C29H32N4/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/h3-16,28H,17-21H2,1-2H3,(H,30,31)
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 |
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 |
---|---|---|
MR evaluation of calcium entry blockers with putative cerebroprotective effects in acute cerebral ischaemia. | 1990 |
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Neuroprotective efficacy of lifarizine (RS-87476) in a simplified rat survival model of 2 vessel occlusion. | 1995 Dec |
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Selectivity of the neuroprotective agent lifarizine. | 1995 Sep |
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Efficacy and tolerability of lifarizine in acute ischemic stroke. A pilot study. Lifarizine Study Group. | 1995 Sep 15 |
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Inhibition by lifarizine of intracellular Ca2+ rises and glutamate exocytosis in depolarized rat cerebrocortical synaptosomes and cultured neurones. | 1996 May |
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Focal cerebral ischemia in the mouse: hypothermia and rapid screening of drugs. | 1998 Feb |
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Frequency-independent blockade of cardiac Na+ channels by riluzole: comparison with established anticonvulsants and class I anti-arrhythmics. | 2000 Mar-Apr |
|
Reasons why stroke trials underestimate the neuroprotective effects of drugs. | 2002 Jan |
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
Fri Dec 15 16:12:25 UTC 2023
by
admin
on
Fri Dec 15 16:12:25 UTC 2023
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Record UNII |
C3705I245K
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Record Status |
Validated (UNII)
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Record Version |
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-
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NCI_THESAURUS |
C333
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6885
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C72816
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SUB08510MIG
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CC-82
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71336
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CHEMBL122079
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119514-66-8
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100000082292
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C3705I245K
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C067927
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |