From Wikipedia, the free encyclopedia
Mofegiline
Clinical data
Other namesMDL-72,974A
Routes of
administration		Oral [1]
ATC code
  • None
Legal status
Legal status
  • Development terminated
Pharmacokinetic data
Elimination half-life1–3 hours [1]
ExcretionUrine [2]
Identifiers
  • (2E)-2-(fluoromethylidene)-4-(4-fluorophenyl)butan-1-amine
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC11H13F2N
Molar mass197.229 g·mol−1
3D model ( JSmol)
  • Fc1ccc(cc1)CCC(=[C@H]F)CN
  • 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 inhibitor of monoamine 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]

See also

References

  1. ^ 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.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.
  5. ^ 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.
  6. ^ 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.
  7. ^ 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.
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