Lazabemide

• CAT Number: I000228
• CAS Number: 103878-84-8
• Molecular Formula: C8H10ClN3O
• Molecular Weight: 199.6
• Purity: ≥95%
• Target: MAO-B inhibitor
• Solubility: DMSO: ≥ 34 mg/mL
• Storage: -20°C
• IC50: 30 nM [1]
• InChIKey: JZXRLKWWVNUZRB-UHFFFAOYSA-N

Lazabemide(Ro 19-6327/000) is selective, reversible monoamine oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 μM for MAO-B and MAO-A respectively).IC50 value: 30 nM [1]Target: MAO-B inhibitorin 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 41-1049 in rat cerebral cortex were 10.7 nM and 7.38 pmol/mg protein, respectively, and for 3H-Ro 19-6327 were 18.4 nM and 3.45 pmol/mg protein, respectively [1]. 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. Lazabemide and Ro 16-6491 also differed from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Ro 16-6491 (500 microM) induced a greater 5 HT release than did L-deprenyl, but was less effective than L-deprenyl in releasing DA. On the contrary, lazabemide was almost completely inactive on either 5 HT and DA release [2]. a clear inhibition of DOPAC formation was observed with Ro 41-1049 (250 nM), while 250 nM lazabemide was found not to increase the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA [3].in vivo: The ischemia reperfusion-induced hydroxyl radical generation was attenuated by 3 mg/kg of clorgyline and lazabemide. Furthermore, mice pretreated with these MAO inhibitors showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups; recovery of the reduced DOPAC level was also delayed [4].

Reference

1:Specific binding of [3H]Ro 19-6327 (lazabemide) to monoamine oxidase B is increased in frontal cortex of suicide victims after controlling for age at death. Ballesteros J, Maeztu AI, Callado LF, Meana JJ, Gutiérrez M.Eur Neuropsychopharmacol. 2008 Jan;18(1):55-61. Epub 2007 Jun 13. PMID: 17570647 2:Lazabemide, a selective, reversible monoamine oxidase B inhibitor, as an aid to smoking cessation. Berlin I, Aubin HJ, Pedarriosse AM, Rames A, Lancrenon S, Lagrue G; Lazabemide in Smoking Cessation Study Investigators..Addiction. 2002 Oct;97(10):1347-54. PMID: 12359039 3:MAO-B inhibition by a single dose of l-deprenyl or lazabemide does not prevent neuronal damage following focal cerebral ischaemia in rats. Jolkkonen J, Kauppinen R, Nyman L, Haapalinna A, Sivenius J.Pharmacol Toxicol. 2000 Nov;87(5):242-5. PMID: 11129505 4:Antioxidant activity of the monoamine oxidase B inhibitor lazabemide. Mason RP, Olmstead EG, Jacob RF.Biochem Pharmacol. 2000 Sep 1;60(5):709-16. PMID: 10927030 5:Safety study of lazabemide (Ro19-6327), a new MAO-B inhibitor, on cardiac arrhythmias and blood pressure of patients with Parkinson/’s disease. Narabayashi H, Yamaguchi T, Sugi K, Mitamura H, Mizuno Y, Nakashima M.Clin Neuropharmacol. 1999 Nov-Dec;22(6):340-6. PMID: 10626094 6:Lazabemide for the treatment of Alzheimer/’s disease: rationale and therapeutic perspectives. Cesura AM, Borroni E, Gottowik J, Kuhn C, Malherbe P, Martin J, Richards JG.Adv Neurol. 1999;80:521-8. Review. No abstract available. PMID: 10410766 7:Pharmacokinetics and pharmacodynamics of single and multiple doses of the MAO-B inhibitor lazabemide in healthy subjects. Dingemanse J, Wood N, Jorga K, Kettler R.Br J Clin Pharmacol. 1997 Jan;43(1):41-7. PMID: 9056051 Free Article8:Effect of lazabemide on the progression of disability in early Parkinson/’s disease. The Parkinson Study Group. [No authors listed]Ann Neurol. 1996 Jul;40(1):99-107. PMID: 8687199 9: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. PMID: 8861736 10:Investigation on the structure of the active site of monoamine oxidase-B by affinity labeling with the selective inhibitor lazabemide and by site-directed mutagenesis. Cesura AM, Gottowik J, Lahm HW, Lang G, Imhof R, Malherbe P, Röthlisberger U, Da Prada M.Eur J Biochem. 1996 Mar 15;236(3):996-1002. PMID: 8665924 Free Article