Phenelzine sulfate
(Synonyms: 硫酸苯乙肼) 目录号 : GC30773An inhibitor of MAO
Cas No.:156-51-4
Sample solution is provided at 25 µL, 10mM.
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Phenelzine is an inhibitor of monoamine oxidase (MAO; IC50 = 0.9 μM using rat brain mitochondrial preparations).1 It potentiates the effects of tryptamine on isolated rat fundus (EC50 = 90 nM) and increases tryptamine toxicity in mice with LD50 values of 85 and 500 mg/kg in the presence and absence of phenelzine, respectively. Phenelzine (20 mg/kg) increases GABA, dopamine, serotonin , and norepinephrine levels in the hippocampus and cortex of socially isolated rats and rats treated with the NMDA receptor antagonist (+)-MK-801 .2 It also increases 5-HT levels in the ventral horn of the spinal cord, improves gross motor ability in a rotarod test, and increases locomotor activity in an open field test in mice with experimental autoimmune encephalomyelitis when administered at a dose of 30 mg/kg.3
1.Maxwell, D.R., Gray, W.R., and Taylor, E.M.Relative activity of some inhibitors of mono-amine oxidase in potentiating the action of tryptamine in vitro and in vivoBr. J. Pharmacol. Chemother.17(3)310-320(1961) 2.Simpson, S.M., Hickey, A.J., Baker, G.B., et al.The antidepressant phenelzine enhances memory in the double Y-maze and increases GABA levels in the hippocampus and frontal cortex of ratsPharmacol. Biochem. Behav.102(1)109-117(2012) 3.Musgrave, T., Benson, C., Wong, G., et al.The MAO inhibitor phenelzine improves functional outcomes in mice with experimental autoimmune encephalomyelitis (EAE)Brain Behav. Immun.25(8)1677-1688(2011)
Cas No. | 156-51-4 | SDF | |
别名 | 硫酸苯乙肼 | ||
Canonical SMILES | NNCCC1=CC=CC=C1.O=S(O)(O)=O | ||
分子式 | C8H14N2O4S | 分子量 | 234.27 |
溶解度 | DMSO : ≥ 41 mg/mL (175.01 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 4.2686 mL | 21.3429 mL | 42.6858 mL |
5 mM | 0.8537 mL | 4.2686 mL | 8.5372 mL |
10 mM | 0.4269 mL | 2.1343 mL | 4.2686 mL |
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Phenelzine and Morphine Drug-Drug Interaction? A Literature Review
The objectives of this manuscript are to describe a case report of a patient whose phenelzine maintenance therapy was discontinued due to concern for a phenelzine-morphine drug interaction, to review the available literature regarding the potential for this drug-drug interaction, and provide recommendations for this clinical scenario. A PubMed/MEDLINE literature search was conducted and all publications determined to be relevant to this case report were included. Literature describing in vitro data, case reports/human studies, and review articles concerning the interaction between morphine and monoamine oxidase inhibitors (MAOIs) were included. A total of 14 publications pertinent to the potential phenelzine-morphine interaction were included in this review including 5 in vitro studies, 4 human studies, and 6 review articles detailing the drug interaction profile between opioids and antidepressants. Of these publications, only a single case report of a potential drug interaction between morphine and phenelzine was identified. The literature suggesting a drug interaction between morphine and phenelzine is limited. The combination of phenelzine and morphine, with close monitoring for signs and symptoms of serotonin syndrome, is reasonable for patients with appropriate indications for both agents.
Phenelzine discontinuation: A bitter pill to swallow
Overview of the Neuroprotective Effects of the MAO-Inhibiting Antidepressant Phenelzine
Phenelzine (PLZ) is a monoamine oxidase (MAO)-inhibiting antidepressant with anxiolytic properties. This multifaceted drug has a number of pharmacological and neurochemical effects in addition to inhibition of MAO, and findings on these effects have contributed to a body of evidence indicating that PLZ also has neuroprotective/neurorescue properties. These attributes are reviewed in this paper and include catabolism to the active metabolite β-phenylethylidenehydrazine (PEH) and effects of PLZ and PEH on the GABA-glutamate balance in brain, sequestration of reactive aldehydes, and inhibition of primary amine oxidase. Also discussed are the encouraging findings of the effects of PLZ in animal models of stroke, spinal cord injury, traumatic brain injury, and multiple sclerosis, as well other actions such as reduction of nitrative stress, reduction of the effects of a toxin on dopaminergic neurons, potential anticonvulsant actions, and effects on brain-derived neurotrophic factor, neural cell adhesion molecules, an anti-apoptotic factor, and brain levels of ornithine and N-acetylamino acids.
Phenelzine-induced psychosis
Phenelzine poisoning
A 46-year-old female with severe phenelzine poisoning was managed successfully by alpha blockade and fluid loading, with the aid of invasive haemodynamic monitoring. The pathophysiology was documented, showing elevated plasma and urinary catecholamines, cardiovascular abnormalities and a contracted blood volume. Most of these changes were reversed following treatment.