General
Preferred name
PROPAFENONE
Synonyms
PROPAFENONE HYDROCHLORIDE ()
Propafenone (D7 hydrochloride) ()
SA-79 (D7 hydrochloride) ()
Propafenone HCl ()
Arythmol ()
SA-79 (hydrochloride) ()
Rytmonorm ()
Rythmol ()
Propafenonum ()
Propafenone (hydrochloride) ()
SA-79 ()
Propafenone (hydrochloride) ()
Rythmol Sr ()
NSC-758640 ()
Propafenona ()
Propafenon hexal ()
GNF-Pf-4594 ()
Propafenone-d5 (hydrochloride) ()
P&D ID
PD002872
CAS
34183-22-7
54063-53-5
107300-59-4
163858-56-8
1346605-05-7
Tags
available
drug
Approved by
FDA
First approval
1989
Drug indication
Tachyarrhythmias
Atrial fibrillation
Drug Status
approved
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE 29
DESCRIPTION Propafenone (hydrochloride) (SA-79 (hydrochloride)) is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.
PHARMACODYNAMICS Propafenone is a Class 1C antiarrhythmic drug with local anesthetic effects, and a direct stabilizing action on myocardial membranes. It is used in the treatment of atrial and ventricular arrhythmias. It acts by inhibiting sodium channels to restrict the entry of sodium into cardiac cells resulting in reduced excitation. Propafenone has local anesthetic activity approximately equal to procaine.
DESCRIPTION Marketed formulations may contain propafenone hydrochloride (PubChem CID 36708). (GtoPdb)
DESCRIPTION Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the ¦Â receptor (IC50=32 nM)[1]. Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 ¦Ìm and 8.6 ¦Ìm, respectively[2]. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis[3].
PRICE 29
DESCRIPTION Blocks hKv1.5 and ATP-sensitive K+ channels; beta-adrenoceptor antagonist (LOPAC library)
DESCRIPTION Propafenone HCl is an inhibitor of voltage-dependent sodium channels and potassium voltage-gated channel. It is a Class I antiarrhythmic drug. Propafenone HCl is used to treat cardiac arrhythmia. (Enamine Bioactive Compounds)
DESCRIPTION Propafenone hydrochloride (Arythmol8) is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias. (TargetMol Bioactive Compound Library)
DESCRIPTION Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy. (TargetMol Bioactive Compound Library)
Cell lines
4
Organisms
1
Compound Sets
30
Cayman Chemical Bioactives
ChEMBL Approved Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine Bioactive Compounds
Enamine BioReference Compounds
Guide to Pharmacology
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
NPC Screening Collection
Other bioactive compounds
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
External IDs
70
Properties
(calculated by RDKit )
Molecular Weight
341.2
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
11
Ring Count
2
Aromatic Ring Count
2
cLogP
3.24
TPSA
58.56
Fraction CSP3
0.38
Chiral centers
1.0
Largest ring
6.0
QED
0.49
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Selectivity
hKv1.5
Target
Sodium Channel
MRP1
Potassium Channel
Adrenergic Receptor
Adrenergic Receptor,Sodium Channel
Pathway
Membrane Transporter/Ion Channel
Immunology/Inflammation
GPCR/G protein
Neuronal Signaling
Therapeutic Class
Antiarrhythmic Agents
VGSC Target
Nav1.5
Source data