Lazabemide hydrochloride  (Synonyms: Ro 19-6327 hydrochloride)

Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC₅₀=0.03 μM) but less active for MAO-A (IC₅₀>100 μM). Lazabemide  inhibits monoamine uptake at high concentrations, the IC₅₀ values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease^[1].

The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. K_D and B_max values for ³H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively^[1].
The IC₅₀ values for lazabemide are: 86 μM for NA uptake; 123 μM for 5HT uptake; > 500 μM for DA uptake, respectively^[1].
. Lazabemide (5 μM) inhibits human MAO-B and MAO-A with IC₅₀ of 6.9 nM and >10 nM, respectively. And it inhibits rat MAO-B and MAO-A with IC₅₀of 37 nM and >10 μM, respectively ina enzymatic assay^[2].
Lazabemide differs from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Lazabemide (500 μM) induces a greater 5 HT release than does L-deprenyl, but is less effective than L-deprenyl in releasing DA. On the contrary, lazabemide was almost completely inactive on either 5 HT and DA release^[2].
Lazabemide (250 nM) results in a clear inhibition of DOPAC formation, while does not increase the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lazabemide (3 mg/kg) attenuates ichemia reperfusion-induced hydroxyl radical generation and pretreatment with Lazabemide showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

236.10

C₈H₁₁Cl₂N₃O

103878-83-7

Solid

Brown to dark brown

O=C(C1=NC=C(Cl)C=C1)NCCN.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Saura J, et al. Quantitative enzyme radioautography with 3H-Ro 41-1049 and 3H-Ro 19-6327 in vitro: localization and abundance of MAO-A and MAO-B in rat CNS, peripheral organs, and human brain. J Neurosci. 1992 May;12(5):1977-99.  [Content Brief]

  [2]. Bondiolotti GP, et al. In vitro effects on monoamine uptake and release by the reversible monoamine oxidase-B inhibitors lazabemide and N-(2-aminoethyl)-p-chlorobenzamide: a comparison with L-deprenyl. Biochem Pharmacol. 1995 Jun 29;50(1):97-102.  [Content Brief]

  [3]. Guimaraes J, et al. The activity of MAO A and B in rat renal cells and tubules. Life Sci. 1998;62(8):727-37.  [Content Brief]

  [4]. Suzuki T, et al. MAO inhibitors, clorgyline and lazabemide, prevent hydroxyl radical generation caused by brain ischemia/reperfusion in mice. Pharmacology. 1995 Jun;50(6):357-62.  [Content Brief]