Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H27N3O2 |
Molecular Weight | 365.4687 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCN(CC)CCN1C(=O)C(CC2=CC=C(OC)C=C2)=NC3=C1C=CC=C3
InChI
InChIKey=MSPRUJDUTKRMLM-UHFFFAOYSA-N
InChI=1S/C22H27N3O2/c1-4-24(5-2)14-15-25-21-9-7-6-8-19(21)23-20(22(25)26)16-17-10-12-18(27-3)13-11-17/h6-13H,4-5,14-16H2,1-3H3
Molecular Formula | C22H27N3O2 |
Molecular Weight | 365.4687 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/25351499Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/caroverine.html | https://clinicaltrials.gov/ct2/show/NCT01174979 | https://www.ncbi.nlm.nih.gov/pubmed/15042481 | http://www.mims.com/india/drug/info/caroverine?type=full&mtype=generic | https://www.ncbi.nlm.nih.gov/pubmed/9297050
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25351499
Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/caroverine.html | https://clinicaltrials.gov/ct2/show/NCT01174979 | https://www.ncbi.nlm.nih.gov/pubmed/15042481 | http://www.mims.com/india/drug/info/caroverine?type=full&mtype=generic | https://www.ncbi.nlm.nih.gov/pubmed/9297050
Caroverine is a spasmolytic drug used in tinnitus treatment improves mechanosensitivity and mechanotransduction phenomenon and otoneuroprotective agent. Caroverine acts as an N-type calcium channel blocker, competitive AMPA receptor antagonist, and non-competitive NMDA receptor antagonist. When excessive glutamate binds to NMDA receptors, the receptor opens and allows calcium and sodium to enter the neuron, abnormal levels of calcium disturbs ionic balance causing spontaneous depolarization state. Pathological spontaneous depolarization state is reversed back to physiological polarization state by antagonistic property of Caroverine.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2094124 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12473379 |
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Target ID: CHEMBL2096670 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12473379 |
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Target ID: CHEMBL2363032 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12473379 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Spasmium Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Different action of memantine and caroverine on glutamatergic transmission in the mammalian cochlea. | 2002 |
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Clinical experience with caroverine in inner ear diseases. | 2002 |
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Caroverine, a multifunctional drug with antioxidant functions. | 2003 |
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Re-establishment of olfactory and taste functions. | 2005 |
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Therapy of hearing disorders - conservative procedures. | 2005 |
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[Changes of synaptoarchitecture of the retina after the light-induced damage and their correction by plant antioxidants]. | 2008 |
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Visual-procedural memory consolidation during sleep blocked by glutamatergic receptor antagonists. | 2008 May 21 |
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Changes in the synaptoarchitectonics of the retina after light-induced damage and their correction with antioxidants of plant origin. | 2009 Feb |
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Blocking AMPA receptor signalling by caroverine infusion does not affect counter-regulation of hypoglycaemia in healthy men. | 2009 Jun |
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Tinnitus: characteristics, causes, mechanisms, and treatments. | 2009 Mar |
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Analysis of 60 patients after tympanotomy and sealing of the round window membrane after acute unilateral sensorineural hearing loss. | 2009 May-Jun |
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Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
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Neuropharmacology of vestibular system disorders. | 2010 Mar |
Patents
Sample Use Guides
Adult: 20-40 mg 3-4 times daily. Max: 200 mg/day.
Max Dosage: 200 mg daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25351499
Cytotoxicity of caroverine in HNSCC cell lines was assessed using the Cell Counting Kit-8 (CCK-8, Dojindo Molecular Technologies Inc., Rockville, MD, USA). Briefly, 3 9 103 cells were seeded into 96 well plates and allowed to rest for 24 h. Caroverine was dissolved in dimethyl sulfoxide (DMSO) and diluted to concentrations ranging from 50 to 500 mkM. Cells were incubated with increasing doses of caroverine and after 72 h, cell viability was measured using the CCK-8 kit according to the manufacturer’s protocol.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:02:25 UTC 2023
by
admin
on
Fri Dec 15 16:02:25 UTC 2023
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Record UNII |
XJ73B0K6KB
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Record Status |
Validated (UNII)
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Record Version |
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WHO-ATC |
A03AX11
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WHO-VATC |
QA03AX11
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NCI_THESAURUS |
C333
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NCI_THESAURUS |
C29698
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65709
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3254
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DB13835
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CHEMBL1729803
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DTXSID6049010
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23465-76-1
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C73173
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CAROVERINE
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SUB06136MIG
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m3129
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100000081323
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |