DC Chemicals Limited
China
Product Name: Lazabemide hydrochloride
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Purity: 98.0%
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103878-83-7

103878-83-7 structure

Name: Lazabemide hydrochloride
Chemical Name: N-(2-aminoethyl)-5-chloropyridine-2-carboxamide,hydrochloride
CAS Number: 103878-83-7
Molecular Formula: C₈H₁₁Cl₂N₃O
Molecular Weight: 236.09800
Catalog: Signaling Pathways Neuronal Signaling Monoamine Oxidase
Create Date: 2018-05-18 08:00:00
Modify Date: 2024-01-10 17:38:06
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].

Name	N-(2-aminoethyl)-5-chloropyridine-2-carboxamide,hydrochloride
Synonyms	Lazabemide hydrochloride Ro 19-6327/001 Huwentoxin IV Tempium Lazabemide monohydrochloride Lazabemide HCl Ro 19-6327

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].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase Research Areas >> Neurological Disease
Target	MAO-B:0.4 nM (IC50)
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].
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].
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.

Boiling Point	397.4ºC at 760mmHg
Molecular Formula	C₈H₁₁Cl₂N₃O
Molecular Weight	236.09800
Flash Point	194.2ºC
Exact Mass	235.02800
PSA	68.01000
LogP	2.31670
Vapour Pressure	1.59E-06mmHg at 25°C

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 DATA

ACUTE 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

Hazard Codes	Xi

103878-83-7	1406-14-0
6138-79-0	127228-87-9
143851-98-3	929-73-7
65546-09-0	1135280-78-2
56-99-5	1406-02-6
1158522-08-7	940364-43-2
113967-27-4	894213-73-1
260352-06-5	134104-43-1
131615-57-1	924102-12-5
919017-52-0	453568-45-1