Introduction：Basic information about CAS 103878-83-7|Lazabemide hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Lazabemide hydrochloride |
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| CAS Number | 103878-83-7 | Molecular Weight | 236.09800 |
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| Density | / | Boiling Point | 397.4ºC at 760mmHg |
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| Molecular Formula | C8H11Cl2N3O | Melting Point | / |
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| MSDS | / | Flash Point | 194.2ºC |
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Names
| Name | N-(2-aminoethyl)-5-chloropyridine-2-carboxamide,hydrochloride |
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| Synonym | More Synonyms |
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Lazabemide hydrochloride BiologicalActivity
| Description | 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]. |
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| Related Catalog | Signaling Pathways >>Neuronal Signaling >>Monoamine OxidaseResearch Areas >>Neurological Disease |
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| Target | MAO-B:0.4 nM (IC50) |
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| 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 Bmax 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]. |
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| 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[4]. |
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| References | [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. [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. [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. [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. |
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Chemical & Physical Properties
| Boiling Point | 397.4ºC at 760mmHg |
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| Molecular Formula | C8H11Cl2N3O |
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| Molecular Weight | 236.09800 |
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| Flash Point | 194.2ºC |
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| Exact Mass | 235.02800 |
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| PSA | 68.01000 |
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| LogP | 2.31670 |
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| Vapour Pressure | 1.59E-06mmHg at 25°C |
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| InChIKey | JMFKTFLARGGXCC-UHFFFAOYSA-N |
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| SMILES | Cl.NCCNC(=O)c1ccc(Cl)cn1 |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- US4551100
- CHEMICAL NAME :
- 2-Pyridinecarboxamide, N-(2-aminoethyl)-5-chloro-, hydrochloride
- CAS REGISTRY NUMBER :
- 103878-83-7
- LAST UPDATED :
- 199509
- DATA ITEMS CITED :
- 1
- MOLECULAR FORMULA :
- C8-H10-Cl-N3-O.Cl-H
- MOLECULAR WEIGHT :
- 236.12
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 30 gm/kg
- SEX/DURATION :
- male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22(suppl 11),S2785,199
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Safety Information
Synonyms
| Lazabemide hydrochloride |
| Ro 19-6327/001 |
| Huwentoxin IV |
| Tempium |
| Lazabemide monohydrochloride |
| Lazabemide HCl |
| Ro 19-6327 |
