Name | (2E)-2-(fluoromethylidene)-4-(4-fluorophenyl)butan-1-amine,hydrochloride |
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Synonyms |
MOFEGILINE HYDROCHLORIDE
(E)-2-(p-fluorophenethyl)-3-fluoroallylamine hydrochloric acid (2Z)-2-(Fluoromethylene)-4-(4-fluorophenyl)-1-butanamine hydrochloride (1:1) (2Z)-3-Fluoro-2-[2-(4-fluorophenyl)ethyl]prop-2-en-1-amine Hydrochloride MDL 72974A Mofegiline hydrochloride (USAN) Benzenebutanamine, 4-fluoro-β-(fluoromethylene)-, (βZ)-, hydrochloride (1:1) Mofegiline HCl (E)-1-amino-2-(fluoromethylene)-4-(p-fluorophenyl)butane hydrochloride salt |
Description | Mofegiline Hcl (MDL72974A) is a potent and selective enzyme-activated irreversible inhibitor of MAO-B; shows marked selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A and MAO-B).IC50 value: 3.6 nM [1]Target: MAO-Bin vitro: MDL72974 inhibits rat brain mitochondrial MAO in a concentration and time-dependent fashion and shows marked selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A and MAO-B, respectively) [1]. is also capable of inhibiting semicarbazide-sensitive amine oxidases (SSAOs) obtained from vascular tissues and sera of different species. The inhibition of SSAO by MDL-72974A was irreversible and time dependent. It was competitive without preincubation of the enzyme with the inhibitor and demonstrated a mixed-type of inhibition when the enzyme was preincubated with the inhibitor. The IC50 values were estimated to be 2 x 10(-9) M, 5 x 10(-9) M, 8 x 10(-8) M and 2 x 10(-8) M for SSAO from dog aorta, rat aorta, bovine aorta and human umbilical artery, respectively [2]. in vivo: After oral administration to rats, the compound shows preferential inhibition of brain MAO-B with ED50 values of 8 and 0.18 mg/kg p.o. for the A and B forms, respectively. Selectivity is retained on repeat dosing. MDL 72,974 did not significantly potentiate the cardiovascular effects of intraduodenually-administered tyramine in anaesthetized rats and had only minor indirect sympathomimatic effects in the pithed rat [1]. Male beagle dogs were given single p.o. (20 mg/kg) and i.v. (5 mg/kg) doses of [14C]-Mofegiline. Total radioactivity excreted in urine and feces over 96 hr was, respectively, 75.5 +/- 3.8 and 6.3 +/- 3.4% of the dose after p.o. and 67.9 +/- 0.5 and 3.9 +/- 2.4% after i.v. administration. Unchanged drug in urine represented 3% of the dose after po and less than 1% after i.v. administration. Mofegiline was thus extensively metabolized in dogs, and urinary excretion was the major route of elimination of metabolites [3]. |
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Related Catalog | |
References |
Boiling Point | 322.7ºC at 760 mmHg |
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Molecular Formula | C11H14ClF2N |
Molecular Weight | 233.685 |
Flash Point | 149ºC |
Exact Mass | 233.078278 |
PSA | 26.02000 |
LogP | 4.07270 |
Vapour Pressure | 0.00232mmHg at 25°C |
Storage condition | 2-8℃ |
~% 120635-25-8 |
Literature: US5488188 A1, ; |