|4-氯-N-(2-吗啉代乙基)苯甲酰胺|CsnPharm

CAS No.: 71320-77-9

Moclobemide/吗氯贝胺 Catalog No. CSN11456

Synonyms: Ro111163;brand name: Amira;Aurorix

Moclobemide is a reversible MAO-A inhibitor.

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描述Moclobemide is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A^[3]. Moclobemide is a reversible inhibitor of monoamine-oxidase-A (RIMA) and has been extensively evaluated in the treatment of a wide spectrum of depressive disorders. The effective therapeutic dose range for moclobemide in most acute phase trials was 300 to 600 mg, divided in 2 to 3 doses. Cases of refractory depression might improve with a combination of moclobemide with other antidepressants, such as clomipramine or a SSRI (selective serotonin reuptake inhibitors)^[4]. In humans, moclobemide is rapidly absorbed after a single oral administration and maximum concentration in plasma is reached within an hour. In the case of moclobemide, increase in the level of serotonin is the most pronounced. Moclobemide administration also leads to increased monoamine receptor stimulation, reversal of reserpine induced behavioral effects, selective depression of REM sleep, down regulation of beta-adrenoceptors and increases in plasma prolactin and growth hormone levels. It reduces scopolamine-induced performance decrement and alcohol induced performance deficit which suggest a neuroprotective role^[5]. Long-term treatment with moclobemide causes gynecomastia in rats, which is reversible^[6]. Morever, moclobemide overdose in combination with a serotonergic agent (even in normal therapeutic doses) can cause severe serotonin toxicity^[7].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02269540	Major Depressive Disorder	Early Phase 1	Recruiting	July 2018	Canada, Ontario ... more >> Research Imaging Centre, Centre for Addiction and Mental Health Recruiting Toronto, Ontario, Canada, M5T 1R8 Principal Investigator: Jeffrey H Meyer, MD, PhD Collapse <<
NCT01544309	Hypercholesterolemia With Conc... more >>omitant Type 2 Diabetes Collapse <<	Not Applicable	Completed	-	-
NCT00068224	-	-	Completed	-	United States, Maryland ... more >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7211 mL
- 18.6054 mL
- 37.2108 mL
- 5 mM
- 0.7442 mL
- 3.7211 mL
- 7.4422 mL
- 10 mM
- 0.3721 mL
- 1.8605 mL
- 3.7211 mL

技术信息

CAS号

71320-77-9

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H17ClN2O2

运输

蓝冰

分子量

268.74

别名

Ro111163;brand name: Amira;Aurorix;Clobemix;Depnil;Manerix;吗氯贝胺

溶解度

DMSO	100.0 mg/mL (372.1 mM)
Water	insoluble

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02269540	Major Depressive Disorder	Early Phase 1	Recruiting	July 2018	Canada, Ontario ... more >> Research Imaging Centre, Centre for Addiction and Mental Health Recruiting Toronto, Ontario, Canada, M5T 1R8 Principal Investigator: Jeffrey H Meyer, MD, PhD Collapse <<
NCT01544309	Hypercholesterolemia With Conc... more >>omitant Type 2 Diabetes Collapse <<	Not Applicable	Completed	-	-
NCT00068224	-	-	Completed	-	United States, Maryland ... more >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Collapse <<
NCT01544309	-	-	Completed	-	-
NCT01962753	Elderly Major... more >> Depression Collapse <<	Not Applicable	Unknown	May 2018	France ... more >> University Hospital of Besançon- Jean Minjoz Recruiting Besançon, France, 25030 Contact: Pierre VANDEL pierre.vandel@univ-fcomte.fr University Hospital of Caen Recruiting Caen, France, 14000 Contact: Sonia DOLLFUS dollfus-s@chu-caen.fr University Hospital of Lille Recruiting Lille, France, 59000 Contact: Jean ROCHE Jean.ROCHE@CHRU-LILLE.FR University Hospital of Nice Recruiting Nice, France, 06000 Contact: Philippe ROBERT robert.p@chu-nice.fr Sainte-Anne Hospital Recruiting Paris, France, 75014 Contact: Thierry GALLARDA T.GALLARDA@ch-sainte-anne.fr Le Rouvray Hospital Recruiting Sotteville lès Rouen, France, 76300 Contact: Marie DESBORDES marie.desbordes@ch-lerouvray.fr University Hospital of Strasbourg - HUS Recruiting Strasbourg, France, 67098 Contact: Frédéric BLANC frederic.blanc@chru-strasbourg.fr University Hospital of Toulouse - Purpan Recruiting Toulouse, France, 31059 Contact: Christophe ARBUS arbus.c@chu-toulouse.fr University Hospital of Tours Recruiting Tours, France, 37000 Contact: Vincent CAMUS vincent.camus@univ-tours.fr Collapse <<
NCT00704860	Major Depression	Phase 4	Completed	-	Canada, Ontario ... more >> University of Ottawa Institute of Mental Health Research Ottawa, Ontario, Canada, K1Z 7K4 Collapse <<
NCT02222220	Clozapine-induced Hypersalivat... more >>ion Collapse <<	Phase 3	Completed	-	Israel ... more >> Be'er Sheva Mental Health Center, Be'er Sheva, Israel, 8417000 Collapse <<
NCT03010761	Addiction	Phase 2	Terminated(all participants fi... more >>nished the trial) Collapse <<	-	-
NCT00534573	Clozapine-induced Hypersalivat... more >>ion Collapse <<	Phase 3	Completed	-	Israel ... more >> Be'er Sheva Mental Health Center, Tirat HaKarmel Mental Health Center Be'er Sheva, Haifa, Israel Collapse <<
NCT01926626	Nicotine Dependence	Phase 2	Completed	-	United States, North Carolina ... more >> Duke Center for Smoking Cessation Charlotte, North Carolina, United States, 28210 Duke Center forSmoking Cessation Durham, North Carolina, United States, 27705 Duke Center for Smoking Cessation Winston-Salem, North Carolina, United States, 27103 Collapse <<
NCT01926626	-	-	Completed	-	-
NCT02374567	Dementia Depr... more >>ession Schizophrenia Psychosomatic Disorders Anxiety Disorders Collapse <<	Phase 3	Terminated	-	Germany ... more >> Bezirkskrankenhaus Augsburg Augsburg, Germany Krankenhaus Hedwigshöhe Berlin, Germany Hannover Medical School Hannover, Germany, 30625 Asklepios Fachklinikum Lübben Lübben, Germany Asklepios Fachklinikum Teupitz Teupitz, Germany Collapse <<

Moclobemide/吗氯贝胺 Catalog No. CSN11456

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