U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C30H35F2N3O
Molecular Weight 491.6152
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LIDOFLAZINE

SMILES

CC1=CC=CC(C)=C1NC(=O)CN2CCN(CCCC(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC2

InChI

InChIKey=ZBIAKUMOEKILTF-UHFFFAOYSA-N
InChI=1S/C30H35F2N3O/c1-22-5-3-6-23(2)30(22)33-29(36)21-35-19-17-34(18-20-35)16-4-7-28(24-8-12-26(31)13-9-24)25-10-14-27(32)15-11-25/h3,5-6,8-15,28H,4,7,16-21H2,1-2H3,(H,33,36)

HIDE SMILES / InChI

Molecular Formula C30H35F2N3O
Molecular Weight 491.6152
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Lidoflazine is a vasodilator used for the treatment of angina pectoris. Lidoflazine is a high-affinity blocker of the HERG K(+)channel.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
16.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CLINIUM

Approved Use

Angina pectoris resulting from ischaemic heart disease. Prophylaxis and after-treatment (after the acute phase) of myocardial infarcation.
PubMed

PubMed

TitleDatePubMed
Ventricular tachyarrhythmias induced by disopyramide and other similar anti-arrhythmic drugs.
1981 Jun 6
Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs.
2006 Mar
Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting.
2010 Dec

Sample Use Guides

The dosage ranges between 2 and 4 tablets daily. Dosage should be adapted individually and started gradually as follows: first week –1 tablet daily. second week –1 tablet every morning and evening. third week –1 tablet three times per day. An appreciable beneficial effect may sometimes be manifest after a few days or weeks of treatment but the full therapeutic result can usually only be assessed after 6 months of treatment. If no marked improvement is noticeable after 3 months then the dosage may gradually be increased to 6 tablets per day using as guidelines the therapeutic response, possible non-transient side-effects and ECG controls. Tablets are preferably taken during meals. Gastrointestinal disturbances can be avoided by taking an antacid con-currently. Clinical findings indicate that uninterrupted therapy, at the optimum dosage level, must be maintained indefinitely to consolidate the favourable results.
Route of Administration: Oral
In Vitro Use Guide
The neuronal cell degeneration was Ca+(+)-dependent because, in the absence of extracellular Ca++, 16 hr of exposure to 30 microM veratridine failed to produce release of LDH. Ca++ antagonists, nonselective for slow Ca++ channels (flunarizine, cinnarizine, lidoflazine, prenylamine and bepridil) inhibited veratridine-induced release of LDH with IC50 values between 0.11 and 0.47 microM.
Substance Class Chemical
Created
by admin
on Sat Dec 16 16:44:44 GMT 2023
Edited
by admin
on Sat Dec 16 16:44:44 GMT 2023
Record UNII
J4ZHN3HBTE
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LIDOFLAZINE
INN   MART.   MI   USAN   WHO-DD  
INN   USAN  
Official Name English
Lidoflazine [WHO-DD]
Common Name English
1-PIPERAZINEACETAMIDE, 4-(4,4-BIS(4-FLUOROPHENYL)BUTYL)-N-(2,6-DIMETHYLPHENYL)-
Systematic Name English
MCN-JR-7904
Code English
4-(4,4-BIS(P-FLUOROPHENYL)BUTYL)-1-PIPERAZINEACETO-2',6'-XYLIDIDE
Common Name English
R 7904
Code English
ANGEX
Brand Name English
lidoflazine [INN]
Common Name English
LIDOFLAZINE [MI]
Common Name English
LIDOFLAZINE [USAN]
Common Name English
LIDOFLAZINE [MART.]
Common Name English
R-7904
Code English
Classification Tree Code System Code
WHO-VATC QC08EX01
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
WHO-ATC C08EX01
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
NCI_THESAURUS C333
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
Code System Code Type Description
PUBCHEM
3926
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
ChEMBL
CHEMBL92870
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
RXCUI
6390
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY RxNorm
DRUG BANK
DB13766
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
EPA CompTox
DTXSID6045377
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
CAS
3416-26-0
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
DRUG CENTRAL
1580
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
MESH
D008013
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
EVMPD
SUB08509MIG
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
FDA UNII
J4ZHN3HBTE
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
NCI_THESAURUS
C81685
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
WIKIPEDIA
LIDOFLAZINE
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
MERCK INDEX
m6807
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY Merck Index
INN
1925
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
ECHA (EC/EINECS)
222-312-8
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
SMS_ID
100000082311
Created by admin on Sat Dec 16 16:44:44 GMT 2023 , Edited by admin on Sat Dec 16 16:44:44 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY