General
Preferred name
FLUNARIZINE
Synonyms
FLUNARIZINE HYDROCHLORIDE ()
Flunarizine dihydrochloride ()
Flunarizine 2HCl ()
KW-3149 ()
R14950 ()
Flunarizine (dihydrochloride) ()
KW-3149, R14950 ()
Flunarizine dihydroch ()
NSC-757807 ()
R-14950 ()
Flunarizine HCl ()
Migarid-10 ()
Sibelium ()
Flunarizine (as hydrochloride) ()
Flurizin ()
R 14,950 ()
Flunarizine (hydrochloride) ()
P&D ID
PD009365
CAS
30484-77-6
52468-60-7
40218-96-0
27064-95-5
Tags
natural product
drug
available
Drug Status
approved
Drug indication
Vasodilator
Migraine
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
TOXICITY -Flunarizine should be used with care in patients with depression or those being prescribed other agents, such as phenothiazines, concurrently, which may cause extrapyramidal side-effects.; -Acute overdosage has been reported and the observed symptoms were sedation, agitation and tachycardia.; -Treatment of acute overdosage consists of charcoal administration, induction of emesis or gastric lavage, and supportive measures. No specific antidote is known.
DESCRIPTION Flunarizine has been demonstrated to exhibit multiple activities : calcium entry blocker with calmodulin binding properties, histamine H1 receptor antagonism, dopamine D2 receptor antagonism. It is a fluorine derivative of . Both of these compounds induce parkinsonism as an adverse effect , likely due to antagonism of D2 receptors by the parent molecules and/or some of their bioactive metabolites . (GtoPdb)
DESCRIPTION Dual Na+/Ca2+ channel (T-type) blocker (Tocriscreen Plus)
DESCRIPTION Ca2+/Na+ channel blocker; vasodilator (LOPAC library)
DESCRIPTION Dual Na+/Ca2+ channel (T-type) blocker (Tocriscreen Total)
DESCRIPTION Flunarizine is a selective calcium entry blocker, which has calmodulin binding properties and histamine H1 blocking activity. It may help to reduce the severity and duration of attacks of paralysis and is effective in rapid onset dystonia-parkinsonism. It is effective in the prophylaxis of migraine, vascular disease, occlusive peripheral, vertigo of central and peripheral origin. It is used as an adjuvant in the therapy of epilepsy. It has been shown to significantly reduce headache frequency and severity in both adults and children. It was discovered at Janssen Pharmaceutica in 1968. It has been listed. (BOC Sciences Bioactive Compounds)
Cell lines
0
Organisms
5
Compound Sets
25
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocriscreen Plus
Tocriscreen Total
External IDs
55
Properties
(calculated by RDKit )
Molecular Weight
404.21
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
0
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
3
cLogP
5.39
TPSA
6.48
Fraction CSP3
0.23
Chiral centers
0.0
Largest ring
6.0
QED
0.54
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Ion Channels
Selectivity
Na+/Ca2+ channel
Pathway
Membrane Transporter/Ion Channel
GPCR/G protein
Neuronal Signaling
Target
Calcium Channel
CACNA1G, CACNA1H, CACNA1I, CALM1, HRH1
Dopamine Receptor
Sodium Channel
Indication
migraine headache, vertigo, peripheral artery disease (PAD)
Disease Area
neurology/psychiatry, cardiology
MOA
calcium channel blocker
Therapeutic Class
Anticonvulsants
VGSC Target
Nav1.2
Solubility
Soluble in DMSO, not in water
Source data