LAZABEMIDE

SKU: orb1220941

Description

LAZABEMIDE(Ro 19-6327) is selective reversible monoamine oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 μM for MAO-B and MAO-A respectively).

Key Properties

• CAS Number: 103878-84-8
• MW: 199.64
• Purity: >98% (HPLC)
• Formula: C₈H₁₀ClN₃O
• SMILES: NCCNC(=O)c1ccc(Cl)cn1
• Target: MAO
• Solubility: DMSO:34 mg/mL (170.31 mM)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. KD and Bmaxvalues for 3H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively. The IC50 values for lazabemide are: 86 μM for NA uptake; 123 μM for 5HT uptake; > 500 μM for DA uptake, respectively.. 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. 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. Lazabemide (250 nM) results in a clear inhibition of DOPAC formation, while does notincrease the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ro 19-6327

Quick Database Links

Gene Symbol

MAO