General
Preferred name
SAFINAMIDE
Synonyms
EMD 1195686 mesylate ()
FCE28073 mesylate ()
EMD1195686 ()
FCE26743 ()
FCE 26743 ()
EMD-1195686 ()
EMD 1195686 ()
FCE-26743 ()
SAFINAMIDE MESYLATE ()
Safinamide (mesylate) ()
FCE 26743 (mesylate) ()
EMD 1195686 (mesylate) ()
PNU-151774E,FCE28073 ()
EMD-1195686, PNU-15774E ()
Safinamide (mesylate) ()
Safinamida ()
Xadago ()
Safinamide ()
Safinamide methansulfonate ()
NW-1015 ()
Safinamide methanesulfonate ()
Safinamide mesilate ()
PNU-151774E ()
NW 1015 ()
PNU 151774E ()
Safinamide-d4 ()
P&D ID
PD012205
CAS
133865-89-1
202825-46-5
2748522-33-8
Tags
available
drug
Approved by
EMA
PMDA
FDA
First approval
2014
2015
Drug indication
Liver disease
Idiopathic parkinson disease
Parkinson disease
Drug Status
approved
investigational
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)
TOXICITY uncontrolled involuntary movement, falls, nausea, and trouble sleeping or falling asleep (insomnia); Patients who have an overdose may experience hypertension (high blood pressure), orthostatic hypotension, hallucinations, psychomotor agitation, nausea, vomiting, and dyskinesia.
METABOLISM The principal step is mediated by amidases which have not been identified, and produces safinamide acid. It is also metabolized to O-debenzylated safinamide and N-delkylated amine. The N-dealkylated amine is then oxidized to a carboxylic acid and finally glucuronidated. Dealkylation reactions are mediated by cytochrome P450s (CYPs), especially CYP3A4. Safinamide acid binds to organic anion transporter 3 (OAT3), but no clinical relevance of this interaction has been determined. Safinamide also binds to ABCG2 transiently. No other transporter affinities have been found in preliminary studies.
DESCRIPTION Safinamide is an alpha-aminoamide. The clinically administered formulation may be the mesylate salt (PubChem CID 3038502). (GtoPdb)
DESCRIPTION Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 ¦ÌM) over MAO-A (IC50=580 ¦ÌM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 ¦ÌM) than at resting (IC50=262 ¦ÌM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
PRICE 34
DESCRIPTION Safinamide (FCE-26743) is a reversible and selective monoamine oxidase B (IC50 0.098??M) inhibitor, reducing the degradation of dopamine, and a glutamate release inhibitor (IC50 8??M). It also inhibits dopamine reuptake. Safinamide also blocks sodium and calcium channels. Potential additional uses of Safinamide might be Parkinson's disease, restless leg syndrome and epilepsy.
DESCRIPTION Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 ¦ÌM) over MAO-A (IC50=580 nM)[1]. Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 ¦ÌM) than at resting (IC50=262 ¦ÌM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al[2][3].
PRICE 40
DESCRIPTION Safinamide (FCE-26743) is a reversible and selective monoamine oxidase B (IC50 0.098μM) inhibitor, reducing the degradation of dopamine, and a glutamate release inhibitor (IC50 8μM). It also inhibits dopamine reuptake. Safinamide also blocks sodium and calcium channels. Potential additional uses of Safinamide might be Parkinson's disease, restless leg syndrome and epilepsy. (TargetMol Bioactive Compound Library)
DESCRIPTION Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A. (TargetMol Bioactive Compound Library)
Compound Sets
24
Cayman Chemical Bioactives
21546
28490
ChEMBL Approved Drugs
CHEMBL396778
CHEMBL48582
ChEMBL Drugs
CHEMBL396778
CHEMBL48582
Concise Guide to Pharmacology 2017/18
8291
Concise Guide to Pharmacology 2019/20
8291
Concise Guide to Pharmacology 2021/22
8291
Concise Guide to Pharmacology 2023/24
8291
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB06654
DrugBank Approved Drugs
DB06654
DrugCentral
4921
DrugCentral Approved Drugs
4921
DrugMAP
DM0YWJC
DM0J2ZT
DrugMAP Approved Drugs
DM0YWJC
DM0J2ZT
EU-OPENSCREEN Bioactive Compound Library
EOS101156
Guide to Pharmacology
8291
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL396778
MedChem Express Bioactive Compound Library
HY-70057
HY-70057A
NCATS Inxight Approved Drugs
90ENL74SIG
ReFrame library
Selleckchem Bioactive Compound Library
safinamide
Safinamide-mesilate
TargetMol Bioactive Compound Library
T6651L
T6651
VGSC-DB
NA0106
NA0107
External IDs
62
Properties
(calculated by RDKit )
Molecular Weight
302.14
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
2
Aromatic Ring Count
2
cLogP
2.37
TPSA
64.35
Fraction CSP3
0.24
Chiral centers
1.0
Largest ring
6.0
QED
0.83
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Sodium Channel
MAO-B
MAOB
Monoamine Oxidase
Pathway
Metabolism
Neuroscience
Membrane Transporter/Ion Channel
Neuronal Signaling
MOA
MAO
dopamine reuptake inhibitor, glutamate inhibitor, monoamine oxidase inhibitor
Indication
Parkinson's Disease
VGSC Target
Nav1.7
Source data