103878-84-8
LAZABEMIDE
CAS: 103878-84-8
Molecular Formula: C8H10ClN3O
103878-84-8 - Names and Identifiers
103878-84-8 - Physico-chemical Properties
| Molecular Formula | C8H10ClN3O |
| Molar Mass | 199.64 |
| Density | 1.286±0.06 g/cm3(Predicted) |
| Boling Point | 397.4±37.0 °C(Predicted) |
| Solubility | DMSO: ≥22mg/mL |
| Appearance | powder |
| Color | white to tan |
| pKa | 12.90±0.46(Predicted) |
| Storage Condition | room temp |
| Physical and Chemical Properties | Lazabemide monohydrochloride (Lazabemide Monohydrochloride):C8Hl0ClN3O?HCl. [103878-83-7]. Crystallized from methanol-ether, melting point 193~195 ℃. Distribution coefficient (n-octanol vein): about 0.1. PKa 8.9. Acute toxic LD50 mice (mg/kg):1000~2000 oral administration. |
| In vitro study | 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 3 H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively. The IC 50 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 IC 50 of 6.9 nM and >10 nM, respectively. And it inhibits rat MAO-B and MAO-A with IC 50 of 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 not increase the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA. |
| In vivo study | 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. |
103878-84-8 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
103878-84-8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 5.009 ml | 25.045 ml | 50.091 ml |
| 5 mM | 1.002 ml | 5.009 ml | 10.018 ml |
| 10 mM | 0.501 ml | 2.505 ml | 5.009 ml |
| 5 mM | 0.1 ml | 0.501 ml | 1.002 ml |
Last Update：2024-01-02 23:10:35
103878-84-8 - Reference Information
| biological activity | Lazabemide (Ro 19-6327) is monoamine oxidase B (MAO-B) the selective reversible inhibitor (IC50=0.03 μm), but less active on MAO-A (IC50>100 μm). High concentrations of Lazabemide inhibited monoamine uptake with IC50 values of 86 μm, 123 μm and> 500 μm for norepinephrine, serotonin and dopamine uptake, respectively. Lazabemide can be used in the study of Parkinson's and Alzheimer's disease. |
| Target | IC50: 30 nM (MAO-B). |
| Use | Anti-Parkinson's disease drug. Is a selectively reversible monoamine oxidase B(MAO-B) inhibitor that acts on the brain and peripheral organs. |
| production method | 5-chloropyridine 2-carboxylic acid (I) and N-(2-aminoethyl) tert-butyl carbamate (II) is refluxed in tetrahydrofuran in the presence of carbonyldiimidazole (CDI) to give compound (II). Further hydrolysis with trifluoroacetic acid at reflux in dichloromethane followed by treatment with ethanolic hydrochloric acid gives lazabamine monohydrochloride. |
Last Update：2024-04-09 21:04:16
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