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Mofegiline

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Mofegiline

Clinical data

Other names

MDL-72,974A

Routes of
administration

Oral^[1]

ATC code

None

Legal status

Development terminated

Pharmacokinetic data

Elimination half-life

1–3 hours^[1]

Excretion

Urine^[2]

Identifiers

IUPAC name

(2E)-2-(fluoromethylidene)-4-(4-fluorophenyl)butan-1-amine

CAS Number

119386-96-8

PubChem CID

6437850

ChemSpider

4942371

UNII

1FMJ6D8Y1B

CompTox Dashboard (EPA)

DTXSID50869629

Chemical and physical data

Formula

C₁₁H₁₃F₂N

Molar mass

197.229 g·mol⁻¹

3D model (JSmol)

Interactive image

SMILES

Fc1ccc(cc1)CCC(=[C@H]F)CN

InChI

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

Key:VXLBSYHAEKDUSU-JXMROGBWSA-N

Mofegiline (MDL-72,974) is a selective, irreversible inhibitorofmonoamine oxidase B (MAO-B) and semicarbazide-sensitive amine oxidase (SSAO) which was under investigation for the treatment of Parkinson's disease and Alzheimer's disease,^[3]^[4]^[5]^[6] but was never marketed.^[7]

References[edit]

^ ^a ^b Stoltz M, Reynolds D, Elkins L, Salazar D, Weir S (September 1995). "Pharmacokinetics and pharmacodynamics of the monoamine oxidase B inhibitor mofegiline assessed during a phase I dose tolerance trial". Clinical Pharmacology and Therapeutics. 58 (3): 342–53. doi:10.1016/S0009-9236(96)90162-9. PMID 7554709. S2CID 21543441.

^ Dulery BD, Schoun J, Zreika M, et al. (March 1993). "Pharmacokinetics of and monoamine oxidase B inhibition by (E)-4-fluoro-beta-fluoromethylene benzene butanamine in man". Arzneimittel-Forschung. 43 (3): 297–302. PMID 8489556.

^ Palfreyman MG, McDonald IA, Bey P, Schechter PJ, Sjoerdsma A (1988). "Design and early clinical evaluation of selective inhibitors of monoamine oxidase". Progress in Neuro-psychopharmacology & Biological Psychiatry. 12 (6): 967–87. doi:10.1016/0278-5846(88)90092-9. PMID 3266532. S2CID 32734728.

^ Zreika M, Fozard JR, Dudley MW, Bey P, McDonald IA, Palfreyman MG (1989). "MDL 72,974: a potent and selective enzyme-activated irreversible inhibitor of monoamine oxidase type B with potential for use in Parkinson's disease". Journal of Neural Transmission. Parkinson's Disease and Dementia Section. 1 (4): 243–54. doi:10.1007/bf02263478. PMID 2597310. S2CID 26335432.

^ Palfreyman MG, McDonald IA, Bey P, Danzin C, Zreika M, Cremer G (1994). "Haloallylamine inhibitors of MAO and SSAO and their therapeutic potential". Amine Oxidases: Function and Dysfunction. Journal of Neural Transmission. Supplementum. Vol. 41. pp. 407–14. doi:10.1007/978-3-7091-9324-2_54. ISBN 978-3-211-82521-1. PMID 7931257.

^ Thiffault C, Quirion R, Poirier J (March 1998). "Effect of the MAO-B inhibitor, MDL72974, on superoxide dismutase activity and lipid peroxidation levels in the mouse brain". Synapse. 28 (3): 208–11. doi:10.1002/(SICI)1098-2396(199803)28:3<208::AID-SYN3>3.0.CO;2-E. PMID 9488505. S2CID 20976168.

^ Ganellin CR, Triggle DJ, Macdonald F (1997). Dictionary of pharmacological agents. CRC Press. p. 1370. ISBN 978-0-412-46630-4. Retrieved 25 November 2011.