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
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
Molecular cloning and characterization of a nitrobenzylthioinosine-insensitive (ei) equilibrative nucleoside transporter from human placenta.
1997 Dec 15
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.
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