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Details

Stereochemistry RACEMIC
Molecular Formula C21H27N3O3
Molecular Weight 369.4574
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of NICAINOPROL

SMILES

CC(C)NCC(O)COC1=CC=CC2=C1N(CCC2)C(=O)C3=CC=CN=C3

InChI

InChIKey=AUIHHZBJBKRDIE-UHFFFAOYSA-N
InChI=1S/C21H27N3O3/c1-15(2)23-13-18(25)14-27-19-9-3-6-16-8-5-11-24(20(16)19)21(26)17-7-4-10-22-12-17/h3-4,6-7,9-10,12,15,18,23,25H,5,8,11,13-14H2,1-2H3

HIDE SMILES / InChI

Description

Nicainoprol, also known as RU-42924, is calcium channel antagonist and a putative class I antiarrhythmic agent. Nicainoprol was shown to be useful in the prevention and treatment of arrhythmias associated with acute myocardial infarction. Nicainoprol had been in phase II clinical trials for the treatment of arrhythmia. However, this research has been discontinued.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
1672 ng/mL
100 mg single, oral
NICAINOPROL plasma
Homo sapiens
2450 ng/mL
100 mg single, intravenous
NICAINOPROL plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
10205 ng × h/mL
100 mg single, oral
NICAINOPROL plasma
Homo sapiens
7388 ng × h/mL
100 mg single, intravenous
NICAINOPROL plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
104.2 min
100 mg single, oral
NICAINOPROL plasma
Homo sapiens
106.6 min
100 mg single, intravenous
NICAINOPROL plasma
Homo sapiens

PubMed

Sample Use Guides

In Vivo Use Guide
Ventricular arrhythmia: doses of 200, 400, 600 mg three times daily in randomized order
Route of Administration: Oral
In Vitro Use Guide
The effects of nicainoprol (1-50 uM) on the transmembrane action potentials in isolated papillary muscles of the guinea pig was examined. Nicainoprol (greater than or equal to 5 uM) produced dose-dependent decreases in the maximal upstroke velocity (Vmax) of the action potential. Only the highest concentration (50 uM) decreased the amplitude and the overshoot of the action potential and shortened its duration at 50 or 90% repolarization levels (APD50, APD90). The potential at rest was not affected by any concentration tested (1-50 uM).