Moclobemide: Evolution, Pharmacodynamic, and Pharmacokinetic Properties

Bonnet, Udo

doi:10.1111/j.1527-3458.2002.tb00229.x

Cited by 42 publications

(22 citation statements)

References 152 publications

(169 reference statements)

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“…The concentration of several drugs in vitreous humor and in cerebrospinal fluid have previously been reported to be closely related to the unbound fraction in plasma. The CSF to whole blood ratio is 0.76, a value which is in the same range as the value of the bound fraction of moclobemide in plasma (Fb ¼ 0:5) [1,4]. A high concentration of moclobemide was detected in the bile.…”

Section: Resultsmentioning

confidence: 97%

“…In the human brain, about three-fourth of MAO belongs to the B type [1]. MAO-A is mainly localised in noradrenergic neurons in the locus coeruleus [1]. Recently, the effects of moclobemide on MAO-A inhibition have been studied with positron emission tomography.…”

Section: Introductionmentioning

confidence: 99%

“…As a consequence of MAO-A inhibition, moclobemide increased the levels of brain neurotransmitter amines and in parallel decreased their main deaminated metabolites. In depressed patients, therapeutic administration of moclobemide reduced blood concentrations of metabolites of amine neurotransmitters and induced long-term up-and down-regulation of adrenoreceptors [1].…”

Section: Introductionmentioning

confidence: 99%

“…The distribution of MAO activity varies with tissues. In the human brain, about three-fourth of MAO belongs to the B type [1]. MAO-A is mainly localised in noradrenergic neurons in the locus coeruleus [1].…”

Section: Introductionmentioning

confidence: 99%

“…1) is a short acting selective and reversible inhibitor of monoamine-oxidase A (MAO-A) used as an anti-depressant and for the treatment of social phobia [1]. In human brain, serotonin, norepinephrine and epinephrine are preferentially deaminated by MAO-A, whereas dopamine and 2-phenylethylamine are favoured substrates of MAO-B [1,2].…”

Section: Introductionmentioning

confidence: 99%

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Death following acute poisoning by moclobemide

Giroud¹,

Horisberger²,

Eap

et al. 2004

Forensic Science International

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Section: Resultsmentioning

confidence: 97%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Death following acute poisoning by moclobemide

Giroud¹,

Horisberger²,

Eap

et al. 2004

Forensic Science International

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Mesoporous Niobium Oxide Spheres as an Effective Catalyst for the Transamidation of Primary Amides with Amines

Ghosh

Zeng

et al. 2014

Adv Synth Catal

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Mesoporous niobium oxide spheres (MNOS), conveniently prepared by a novel antisolvent precipitation approach, have been shown to be an effective catalyst for the transamidation of primary amides with amines. This novel transamidation can be efficiently carried out under solvent-free conditions and is applicable to a wide range of primary amides and amines to provide N-alkyl amides in good to excellent yields. The catalyst is highly stable and reusable. The application of this transamidation reaction has been demonstrated in the synthesis of antidepressant drug moclobemide and other druglike compounds.

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Synthesis and Biological Evaluation of Dantrolene‐Like Hydrazide and Hydrazone Analogues as Multitarget Agents for Neurodegenerative Diseases

et al. 2021

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Dantrolene, a drug used for the management of malignant hyperthermia, had been recently evaluated for prospective repurposing as multitarget agent for neurodegenerative syndromes, including Alzheimer's disease (AD). Herein, twenty-one dantrolene-like hydrazide and hydrazone analogues were synthesized with the aim of exploring structure-activity relationships (SARs) for the inhibition of human monoamine oxidases (MAOs) and acetylcholinesterase (AChE), two well-established target enzymes for anti-AD drugs. With few exceptions, the newly synthesized compounds exhibited selectivity toward MAO B over either MAO A or AChE, with the secondary aldimine 9 and phenylhydrazone 20 attaining IC 50 values of 0.68 and 0.81 μM, respectively. While no general SAR trend was observed with lipophilicity descriptors, a molecular simplification strategy allowed the main pharmacophore features to be identified, which are responsible for the inhibitory activity toward MAO B. Finally, further in vitro investigations revealed cell protection from oxidative insult and activation of carnitine/ acylcarnitine carrier as concomitant biological activities responsible for neuroprotection by hits 9 and 20 and other promising compounds in the examined series.

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Moclobemide: Evolution, Pharmacodynamic, and Pharmacokinetic Properties

Cited by 42 publications

References 152 publications

Death following acute poisoning by moclobemide

Death following acute poisoning by moclobemide

Mesoporous Niobium Oxide Spheres as an Effective Catalyst for the Transamidation of Primary Amides with Amines

Synthesis and Biological Evaluation of Dantrolene‐Like Hydrazide and Hydrazone Analogues as Multitarget Agents for Neurodegenerative Diseases

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