N-(Dibenz[b,f]oxepin-10-ylmethyl)-N-Methyl-N-(2-propynyl)aminemaleate

Uses

Omigapil Maleate is a potent anti-apoptotic drug that protects against loss of dopaminergic neurons in laboratory models. It is currently being investigated for its use as a drug for the treatment of neurodegenerative disorders such as Parkinson''s disease and amyotrophic lateral sclerosis (ALS).

Biological Activity

r-(2)-deprenyl represents one of the drugs currently used for the treatment of parkinson’s disease. the mechanism of action of neuroprotection as well as inhibition of apoptosis remains elusive. cgp 3466 is a structurally related r-(2)-deprenyl analoge that exhibits virtually no monoamine oxidase type b inhibiting activity but is neuroprotective.

in vitro

cgp 3466b is structurally related to both classical monoamine oxidase inhibitors and tricyclic antidepressent agents but lacks the pharmacological properties relevant to their anti-depressant effects. cgp 3466b has been shown to rescue human neuroblastoma and pc-12 cells from apoptotic death and also cerebellar granule cells in vitro from death induced by cytosine arabinoside [1].

in vivo

in pmn/pmn mice, cgp 3466b was administered orally at the onset of the clinical symptoms (2 weeks after birth). cgp 3466b slowed disease progression as determined by a 57% life-span increase, preservation of body weight and motor performance. the data support evaluation of cgp 3466b as a potential motor neuron disease treatment [2].

storage

Store at +4°C

References

[1] kragten e, lalande i, zimmermann k, roggo s, schindler p, muller d, van oostrum j, waldmeier p, furst p. glyceraldehyde-3-phosphate dehydrogenase, the putative target of the antiapoptotic compounds cgp 3466 and r-(-)-deprenyl. j biol chem. 1998 mar 6;273(10):5821-8.
[2] sagot y, toni n, perrelet d, lurot s, king b, rixner h, mattenberger l, waldmeier pc, kato ac. an orally active anti-apoptotic molecule (cgp 3466b) preserves mitochondria and enhances survival in an animal model of motoneuron disease. br j pharmacol. 2000 oct;131(4):721-8.