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Details

Stereochemistry ACHIRAL
Molecular Formula C11H13F2N.ClH
Molecular Weight 233.685
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of MOFEGILINE HYDROCHLORIDE

SMILES

Cl.NC\C(CCC1=CC=C(F)C=C1)=C\F

InChI

InChIKey=QUCNNQHLIHGBIA-HCUGZAAXSA-N
InChI=1S/C11H13F2N.ClH/c12-7-10(8-14)2-1-9-3-5-11(13)6-4-9;/h3-7H,1-2,8,14H2;1H/b10-7+;

HIDE SMILES / InChI

Description

Mofegiline (MDL 72,974A or (E)-2-(4-fluorophenethyl)-3-fluoroallylamine, hydrochloride), is a selective and irreversible inhibitor of monoamine oxidase type B (MAO-B) both in vitro and in vivo. In addition, mofegiline inhibits semicarbazide-sensitive amine oxidase activity from human serum and saphenous vein. In phase II studies, MDL 72,974A is proving to be a useful adjunct to conventional therapy of Parkinson's disease. It seems mofegiline development was discontinued.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
28.0 nM [Ki]
3.6 nM [IC50]
10.0 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
27202 pg/mL
48 mg single, oral
MOFEGILINE plasma
Homo sapiens
14018 pg/mL
24 mg 1 times / day steady-state, oral
MOFEGILINE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
105170 pg × h/mL
48 mg single, oral
MOFEGILINE plasma
Homo sapiens
54359 pg × h/mL
24 mg 1 times / day steady-state, oral
MOFEGILINE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
3.02 h
48 mg single, oral
MOFEGILINE plasma
Homo sapiens
2.79 h
24 mg 1 times / day steady-state, oral
MOFEGILINE plasma
Homo sapiens

Doses

PubMed

Sample Use Guides

In Vivo Use Guide
In human volunteers, potent inhibition of platelet MAO-B activity was observed at submilligram doses (ED50 = 90 micrograms) following a single oral dose. Upon multiple oral doses of 100 micrograms, as much as 80% of MAO-B could be inhibited. In phase II studies, Mofegiline (MDL 72,974A) is proving to be a useful adjunct to conventional therapy. Patients (250) with Parkinson's disease, treated once daily with either 1 or 4 mg, together with L-Dopa and a decarboxylase inhibitor (MadoparR or SinemetR), saw significant improvements in symptoms compared with those on standard therapy without the inhibitor.
Route of Administration: Oral
In Vitro Use Guide
Unknown