Lazabemide hydrate - CAS 103878-84-8
Catalog number: 103878-84-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C8H10ClN3O
Molecular Weight:
199.64 (anhydrous basis)
COA:
Inquire
Targets:
Monoamine Oxidase
Description:
Lazabemide, a pyridine derivative, is a reversible and selective monoamine oxidase B inhibitor that has probable effect for Parkinson's disease. IC50: 30 nM. It could also influence the absorption of some monoamines like noradrenalin, serotonin and dopami
Purity:
95%
Appearance:
Powder
Synonyms:
N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrate, Ro 19-6327 hydrate
Solubility:
DMSO: > 34 mg/mL
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
Lazabemide is a reversible and selective monoamine oxidase B inhibitor that has probable effect against Parkinson's disease.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Boiling Point:
397.4ºC at 760mmHg
Density:
1.286g/cm3
InChIKey:
JZXRLKWWVNUZRB-UHFFFAOYSA-N
InChI:
InChI=1S/C8H10ClN3O/c9-6-1-2-7(12-5-6)8(13)11-4-3-10/h1-2,5H,3-4,10H2,(H,11,13)
Canonical SMILES:
C1=CC(=NC=C1Cl)C(=O)NCCN
1.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.
Bondiolotti GP;Galva MD;Villa F;Sciaba L;Picotti GB Biochem Pharmacol. 1995 Jun 29;50(1):97-102.
To investigate whether the reversible monoamine oxidase-B (MAO-B) inhibitors lazabemide and Ro 16-6491 have any additional effect on monoamine uptake and release, in vitro experiments were performed on rat forebrain synaptosomes and blood platelets. The effects of the two drugs were compared with those of L-deprenyl, the well-known irreversible MAO-B inhibitor which is reported to affect amine uptake. Both lazabemide and Ro 16-6491 behaved as weak inhibitors of [3H]monoamine uptake by synaptosomes, with a similar rank order of potency for amine uptake inhibition (noradrenaline (NA) > or = 5-hydroxytryptamine (5 HT) > dopamine (DA)). The IC50 values for lazabemide and Ro 16-6491, respectively, were: 86 microM and 90 microM for NA uptake; 123 microM and 90 microM for 5HT uptake; > 500 microM and > 1000 microM for DA uptake. L-Deprenyl (rank order of inhibitory potency: NA > DA > 5 HT) was four to 10 times more potent than either compound in inhibiting [3H]catecholamine uptake (IC50 = NA 23 microM, DA 109 microM), and two to three times less potent in inhibiting 5 HT uptake (IC50 233 microM). Lazabemide and Ro 16-6491 also differed from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes.
2.Symptomatic anti-parkinsonian effects of monoamine oxidase-B inhibition: comparison of selegiline and lazabemide.
LeWitt PA;Segel SA;Mistura KL;Schork MA Clin Neuropharmacol. 1993 Aug;16(4):332-7.
Selegiline (deprenyl) and lazabemide (Ro 19-6327) are inhibitors of monoamine oxidase-B but differ in several other pharmacological properties. We compared 4-week monotherapy trials of each to assess their actions against signs and disabilities of Parkinson's disease (PD). In a group of 20 mildly affected Parkinson patients treated with each drug, there were no statistically significant changes from the pretreatment baseline. There were no differences between the drugs. This work confirms that the symptomatic effects of selegiline against Parkinsonism are small and are likely due to its inhibition of monoamine oxidase-B.
3.Tyramine pharmacodynamics during combined administration of lazabemide and moclobemide.
Dingemanse J;Hussain Y;Korn A Int J Clin Pharmacol Ther. 1996 Apr;34(4):172-7.
The objective of this study was to assess the tyramine pressor sensitivity during combined administration of selective and reversible inhibitors of monoamine oxidase A and B, viz. moclobemide (300 mg b.i.d.) and lazabemide (100 mg b.i.d.), respectively. In part A, 5 healthy male subjects underwent i.v. tyramine pressor tests before (baseline) and during (day 7) combined treatment with both drugs. The tyramine dose was titrated until an increase in systolic blood pressure of 30 mmHg was attained. Subsequently, lazabemide treatment was discontinued and i.v. tyramine pressor tests were again conducted after 2 - 3 days of moclobemide monotreatment. The tyramine pressor sensitivity factor (mean + or - SD) during combined moclobemide and lazabemide treatment was 4.2 + or - 0.9 and during moclobemide monotreatment 3.1 + or - 1.1. In part B, a separate panel of 8 subjects received combined treatment with moclobemide and lazabemide for up to 10 days. Ascending oral doses of tyramine were administered on days 7 - 10 to determine the threshold dose eliciting a 30 mmHg increase in systolic blood pressure. In comparison to baseline the effects of oral tyramine were potentiated by a factor of 13.
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CAS 103878-84-8 Lazabemide hydrate

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