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Lazabemide (Ro 19-6327), a reversible and highly sensitive MAO-B inhibitor: preclinical and clinical findings.

作者信息

Henriot S, Kuhn C, Kettler R, Da Prada M

机构信息

Pharma Division, F. Hoffmann-La Roche Ltd, Basel, Switzerland.

出版信息

J Neural Transm Suppl. 1994;41:321-5. doi: 10.1007/978-3-7091-9324-2_42.

DOI:10.1007/978-3-7091-9324-2_42
PMID:7931245
Abstract

Ro 19-6327 (lazabemide, L), MDL 72974, selegiline, AGN 1135 and MDL 72145 were investigated for their MAO inhibitory effect in rat tissues in vitro. The selectivity of MAO-B inhibition of L, selegiline and MDL 72974 was also measured in vitro in human brain tissue as well as ex vivo in rat brain and liver after acute and subchronic administration. Of all compounds investigated L was the most selective for MAO-B inhibition under in vitro and ex vivo conditions. In volunteers, L completely but reversibly inhibited platelet MAO-B with a dose-dependent duration. Clinical trials with L are under way in both Alzheimer's and Parkinson's disease (PD).

摘要

相似文献

1
Lazabemide (Ro 19-6327), a reversible and highly sensitive MAO-B inhibitor: preclinical and clinical findings.
J Neural Transm Suppl. 1994;41:321-5. doi: 10.1007/978-3-7091-9324-2_42.
2
MAO-B inhibition in rabbit tissues and in human platelets by Ro 19-6327 shows similar time-course.Ro 19-6327对兔组织和人血小板中MAO-B的抑制作用呈现相似的时间进程。
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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.可逆性单胺氧化酶-B抑制剂拉扎贝胺和N-(2-氨基乙基)-对氯苯甲酰胺对单胺摄取和释放的体外作用:与L-司来吉兰的比较
Biochem Pharmacol. 1995 Jun 29;50(1):97-102. doi: 10.1016/0006-2952(95)00022-r.
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Measurement of human cerebral monoamine oxidase type B (MAO-B) activity with positron emission tomography (PET): a dose ranging study with the reversible inhibitor Ro 19-6327.用正电子发射断层扫描(PET)测量人脑中B型单胺氧化酶(MAO-B)活性:使用可逆抑制剂Ro 19-6327的剂量范围研究。
Eur J Clin Pharmacol. 1991;40(2):169-73. doi: 10.1007/BF00280072.
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Antioxidant activity of the monoamine oxidase B inhibitor lazabemide.
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Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B.雷沙吉兰[N-炔丙基-1R(+)-氨基茚],一种线粒体单胺氧化酶B的选择性强效抑制剂。
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[3H]Ro 19-6327: a reversible ligand and affinity labelling probe for monoamine oxidase-B.
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Combined treatment with MAO-A inhibitor and MAO-B inhibitor increases extracellular noradrenaline levels more than MAO-A inhibitor alone through increases in beta-phenylethylamine.MAO-A 抑制剂和 MAO-B 抑制剂联合治疗通过增加β-苯乙胺使细胞外去甲肾上腺素水平升高高于 MAO-A 抑制剂单独治疗。
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Pharmacodynamics of lazabemide, a reversible and selective inhibitor of monoamine oxidase B.拉扎贝胺的药效学,一种单胺氧化酶B的可逆性和选择性抑制剂。
Br J Clin Pharmacol. 1994 Jun;37(6):553-7. doi: 10.1111/j.1365-2125.1994.tb04303.x.
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Design and early clinical evaluation of selective inhibitors of monoamine oxidase.单胺氧化酶选择性抑制剂的设计与早期临床评估
Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):967-87. doi: 10.1016/0278-5846(88)90092-9.

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Sembragiline in Moderate Alzheimer's Disease: Results of a Randomized, Double-Blind, Placebo-Controlled Phase II Trial (MAyflOwer RoAD).司美吉林治疗中度阿尔茨海默病的随机、双盲、安慰剂对照 II 期试验(MAyflOwer RoAD)结果。
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3
Perseveration in a spatial-discrimination serial reversal learning task is differentially affected by MAO-A and MAO-B inhibition and associated with reduced anxiety and peripheral serotonin levels.
在空间辨别连续反转学习任务中的持续性受到单胺氧化酶A和单胺氧化酶B抑制的不同影响,并与焦虑和外周血清素水平降低有关。
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Recent developments in the drug treatment of Alzheimer's disease.阿尔茨海默病药物治疗的最新进展。
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Early detection of Parkinson's disease. Implications for treatment.
Drugs Aging. 1996 Sep;9(3):159-68. doi: 10.2165/00002512-199609030-00002.