MDL-72274 HCl - CAS 85278-24-6
Catalog number: 85278-24-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C9H11Cl2N
Molecular Weight:
204.09
COA:
Inquire
Targets:
Others
Description:
MDL-72274 is a selective SSAO inhibitor. It is a potent (IC50 = 10(-9) M) inhibitor of both MAO-B and SSAO, with 190-fold lower affinity for MAO-A. MDL-72974 can be used for the treatment of Parkinson diseases.
Purity:
98%
Appearance:
Powder
Synonyms:
(E)-3-chloro-2-phenylprop-2-en-1-amine hydrochloride
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Parkinson diseases
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Canonical SMILES:
NC/C(C1=CC=CC=C1)=C/Cl.[H]Cl
1.Haloallylamine inhibitors of MAO and SSAO and their therapeutic potential.
Palfreyman MG;McDonald IA;Bey P;Danzin C;Zreika M;Cremer G J Neural Transm Suppl. 1994;41:407-14.
Based on mechanistic understandings, molecular modeling and extensive quantitative structure-activity relationships, appropriately substituted haloallylamine derivatives were designed as potential mechanism-based inhibitors of MAO and/or SSAO. Potent inhibition of MAO-B and SSAO occurred with fluoroallylamines whereas chloroallylamines, such as MDL 72274A ((E)-2-phenyl-3-chloroallylamine hydrochloride), were selective and potent inhibitors of SSAO. MDL 72974A (E)-2-(4-fluorophenethyl)-3-fluoroallylamine hydrochloride is a potent (IC50 = 10(-9) M) inhibitor of both MAO-B and SSAO, with 190-fold lower affinity for MAO-A. In clinical studies, oral doses as low as 100 micrograms produced substantial inhibition of platelet MAO-B. Essentially complete inhibition occurred at 1 mg with the effect lasting 6-10 days. One or 4 mg MDL 72974A given daily for 28 days to 40 Parkinson's patients treated with L-dopa produced statistically significant reductions in the Unified Parkinson's Disease Rating Scale. MAO-B inhibitors, such as MDL 72974A and L-deprenyl, offer the potential of being neuroprotective in Parkinson's Disease and other neurogenerative disorders. Concommitant inhibition of SSAO may provide additional, but as yet unproven, advantages over pure inhibitors of MAO-B.
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