Lazabemide
Names
[ CAS No. ]:
103878-84-8
[ Name ]:
Lazabemide
[Synonym ]:
N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide
2-Pyridinecarboxamide, N-(2-aminoethyl)-5-chloro-
N-(2-Aminoethyl)-5-chloropyridine-2-carboxamide
Lazabemide
Biological Activity
[Description]:
Lazabemide(Ro 19-6327/000) is selective, reversible monoamine oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 μM for MAO-B and MAO-A respectively).IC50 value: 30 nM [1]Target: MAO-B inhibitorin vitro: The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. KD and Bmax values for 3H-Ro 41-1049 in rat cerebral cortex were 10.7 nM and 7.38 pmol/mg protein, respectively, and for 3H-Ro 19-6327 were 18.4 nM and 3.45 pmol/mg protein, respectively [1]. The IC50 values for lazabemide and Ro 16-6491, respectively, were: 86 microM and 90 microM for NA uptake; 123 microM and 90 microM for 5HT uptake; > 500 microM and > 1000 microM for DA uptake. Lazabemide and Ro 16-6491 also differed from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Ro 16-6491 (500 microM) induced a greater 5 HT release than did L-deprenyl, but was less effective than L-deprenyl in releasing DA. On the contrary, lazabemide was almost completely inactive on either 5 HT and DA release [2]. a clear inhibition of DOPAC formation was observed with Ro 41-1049 (250 nM), while 250 nM lazabemide was found not to increase the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA [3].in vivo: The ischemia reperfusion-induced hydroxyl radical generation was attenuated by 3 mg/kg of clorgyline and lazabemide. Furthermore, mice pretreated with these MAO inhibitors showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups; recovery of the reduced DOPAC level was also delayed [4].
[Related Catalog]:
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Density]:
1.3±0.1 g/cm3
[ Boiling Point ]:
397.4±37.0 °C at 760 mmHg
[ Molecular Formula ]:
C8H10ClN3O
[ Molecular Weight ]:
199.637
[ Flash Point ]:
194.2±26.5 °C
[ Exact Mass ]:
199.051239
[ PSA ]:
68.01000
[ LogP ]:
-0.01
[ Vapour Pressure ]:
0.0±0.9 mmHg at 25°C
[ Index of Refraction ]:
1.572
[ Storage condition ]:
2-8℃