Monoamine Oxidase Inhibitors
Selegiline
A selective, irreversible inhibitor of Type B monoamine oxidase. It is used in newly diagnosed patients with Parkinson's disease. It may slow progression of the clinical disease and delay the requirement for levodopa therapy. It also may be given with levodopa upon onset of disability. (From AMA Drug Evaluations Annual, 1994, p385) The compound without isomeric designation is Deprenyl.
Monoamine Oxidase
An enzyme that catalyzes the oxidative deamination of naturally occurring monoamines. It is a flavin-containing enzyme that is localized in mitochondrial membranes, whether in nerve terminals, the liver, or other organs. Monoamine oxidase is important in regulating the metabolic degradation of catecholamines and serotonin in neural or target tissues. Hepatic monoamine oxidase has a crucial defensive role in inactivating circulating monoamines or those, such as tyramine, that originate in the gut and are absorbed into the portal circulation. (From Goodman and Gilman's, The Pharmacological Basis of Therapeutics, 8th ed, p415) EC 1.4.3.4.
Dioxanes
Tranylcypromine
A propylamine formed from the cyclization of the side chain of amphetamine. This monoamine oxidase inhibitor is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in panic and phobic disorders. (From AMA Drug Evaluations Annual, 1994, p311)
Phenethylamines
Tyramine
An indirect sympathomimetic. Tyramine does not directly activate adrenergic receptors, but it can serve as a substrate for adrenergic uptake systems and monoamine oxidase so it prolongs the actions of adrenergic transmitters. It also provokes transmitter release from adrenergic terminals. Tyramine may be a neurotransmitter in some invertebrate nervous systems.
Isocarboxazid
Imidazoline Receptors
Desipramine
A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.
Adrenergic Uptake Inhibitors
Drugs that block the transport of adrenergic transmitters into axon terminals or into storage vesicles within terminals. The tricyclic antidepressants (ANTIDEPRESSIVE AGENTS, TRICYCLIC) and amphetamines are among the therapeutically important drugs that may act via inhibition of adrenergic transport. Many of these drugs also block transport of serotonin.
Psychotropic Drugs
Autoradiography
Biogenic Monoamines
Moclobemide
Magnaporthe
Oryza sativa
Aspergillus oryzae
Immunotherapy
Macrophages
The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.)
Phenelzine
Administration, Rectal
Prescription Drug Misuse
Suppositories
Medicated dosage forms that are designed to be inserted into the rectal, vaginal, or urethral orifice of the body for absorption. Generally, the active ingredients are packaged in dosage forms containing fatty bases such as cocoa butter, hydrogenated oil, or glycerogelatin that are solid at room temperature but melt or dissolve at body temperature.
Protective Devices
Tranquilizing Agents
A traditional grouping of drugs said to have a soothing or calming effect on mood, thought, or behavior. Included here are the ANTI-ANXIETY AGENTS (minor tranquilizers), ANTIMANIC AGENTS, and the ANTIPSYCHOTIC AGENTS (major tranquilizers). These drugs act by different mechanisms and are used for different therapeutic purposes.
Obsessive-Compulsive Disorder
An anxiety disorder characterized by recurrent, persistent obsessions or compulsions. Obsessions are the intrusive ideas, thoughts, or images that are experienced as senseless or repugnant. Compulsions are repetitive and seemingly purposeful behavior which the individual generally recognizes as senseless and from which the individual does not derive pleasure although it may provide a release from tension.
Sleep
Compulsive Behavior
The behavior of performing an act persistently and repetitively without it leading to reward or pleasure. The act is usually a small, circumscribed behavior, almost ritualistic, yet not pathologically disturbing. Examples of compulsive behavior include twirling of hair, checking something constantly, not wanting pennies in change, straightening tilted pictures, etc.
Sleep, REM
Polysomnography
Simultaneous and continuous monitoring of several parameters during sleep to study normal and abnormal sleep. The study includes monitoring of brain waves, to assess sleep stages, and other physiological variables such as breathing, eye movements, and blood oxygen levels which exhibit a disrupted pattern with sleep disturbances.
Electroencephalography
Sleep Stages
Norepinephrine
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
Species-dependent differences in monoamine oxidase A and B-catalyzed oxidation of various C4 substituted 1-methyl-4-phenyl-1,2,3, 6-tetrahydropyridinyl derivatives. (1/92)
In an attempt to provide a better understanding of the scope and limitations of animal models used in some drug development programs and to further our understanding of potential metabolic bioactivation reactions, we have undertaken studies to profile the monoamine oxidase A and B (MAO-A and -B, respectively) activities in liver and brain mitochondrial preparations obtained from a variety of species using a series of 1-methyl-4-aryl-1,2,3, 6-tetrahydropyridinyl substrates. Mitochondrial preparations were incubated with substrates at 37 degrees C in the presence or absence of clorgyline, (R)-deprenyl, or a mixture of these two propargylamines to inhibit MAO-A, MAO-B, or both enzymes. The rates of formation of the corresponding dihydropyridinium metabolites were estimated spectrophotometrically. MAO-B was found to be the principal enzyme present in all tissues. Human liver displayed more MAO-A activity than the liver of any other species studied; subhuman primates displayed little or no detectable MAO-A activity. The properties of the preparations from rat liver were most similar to those from human liver with respect to the MAO-A/MAO-B ratios and the kinetic parameters of the four substrates used to profile enzymatic activity. The kinetic properties of mitochondrial preparations from bovine liver, a commonly used source of purified MAO-B preparations, were consistently different from all of the other species studied. The mitochondrial preparations from rabbit brain and liver also were unusual in that they displayed relatively low MAO activities. Additionally, these enzyme activities were considerably less susceptible to inhibition by clorgyline and (R)-deprenyl. Finally, an exceptionally low MAO-B liver/brain V(max)/K(m) ratio was observed with the mitochondria obtained from the C57BL/6 mouse, an effect that may contribute to the susceptibility of this strain to the toxic effects of the parkinsonian-inducing neurotoxin 1-methyl-4-phenyl-1,2,3, 6-tetrahydropyridine. (+info)FA-70, a novel selective and irreversible monoamine oxidase-A inhibitor: effect on monoamine metabolism in mouse cerebral cortex. (2/92)
A series of indolealkylamine derivatives has been previously designed and evaluated with the aim of finding the most potent and selective novel monoamine oxidase (MAO) inhibitors to be used in the therapy of neurological and affective disorders. Among them, FA70, a 5-hydroxy-indolealkylamine derivative, has been characterized in vitro as a potent, irreversible, and mechanism-based inhibitor of the MAO-A isoform. The comparison with clorgyline, analyzed under the same experimental conditions, confirmed FA70 as the most potent MAO-A inhibitor. The ex vivo effect of FA70 on MAO activity in mouse cerebral cortex was similar to that observed in vitro, showing more efficacy than in peripheral tissues. The ex vivo effect of FA70 on amine metabolism also was evaluated after acute and chronic treatment, and the results showed that between both MAO isoforms, MAO-A is the only one responsible for monoamine metabolism in this region of the brain. The ex vivo effect of FA70 on dopamine content was correlated with the activation effect on tyrosine hydroxylase activity, the enzyme responsible for the regulation of the limiting step in catecholamine synthesis. (+info)Selective monoamine oxidase subtype inhibition and striatal extracellular dopamine in the guinea-pig. (3/92)
Striatal microdialysate levels of dopamine (DA) in conscious guinea-pigs were measured following acute (1 day) and chronic (21 days) treatment with deprenyl (2 and 0.25 mg kg(-1) s.c., respectively) or clorgyline (4 and 1 mg kg(-1) s.c., respectively), as well as by combination treatment using the same doses of the two inhibitors. These treatments caused selective inhibition of monoamine oxidase type B (MAO-B) or monoamine oxidase type A (MAO-A) respectively. Neither acute nor chronic treatments with deprenyl or clorgyline increased basal or KCl-induced DA levels. Acute and chronic clorgyline treatments were accompanied by significant reductions in striatal microdialysate 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA). On the other hand, both acute and chronic deprenyl treatments were accompanied by significant increases in microdialysate HVA with no effect on DOPAC levels. Acute or chronic combined treatment with clorgyline and deprenyl increased tissue but not microdialysate DA levels. The combination treatment given chronically also reduced KCl-induced DA release but enhanced amphetamine-induced DA release. Microdialysate DA levels increased to a smaller extent in guinea-pig than in rat following local striatal infusion of GBR-12909 (100 microM). The difference between guinea-pigs and rats in the response to GBR-12909, could be the result of a lower dopaminergic innervation and/or density of DA transporter. This difference may explain why striatal microdialysate DA levels increased following chronic deprenyl treatment in the rat but not in the guinea-pig. (+info)Phentolamine inhibits exocytosis of glucagon by Gi2 protein-dependent activation of calcineurin in rat pancreatic alpha -cells. (4/92)
Capacitance measurements were used to investigate the molecular mechanisms by which imidazoline compounds inhibit glucagon release in rat pancreatic alpha-cells. The imidazoline compound phentolamine reversibly decreased depolarization-evoked exocytosis >80% without affecting the whole-cell Ca(2+) current. During intracellular application through the recording pipette, phentolamine produced a concentration-dependent decrease in the rate of exocytosis (IC(50) = 9.7 microm). Another imidazoline compound, RX871024, exhibited similar effects on exocytosis (IC(50) = 13 microm). These actions were dependent on activation of pertussis toxin-sensitive G(i2) proteins but were not associated with stimulation of ATP-sensitive K(+) channels or adenylate cyclase activity. The inhibitory effect of phentolamine on exocytosis resulted from activation of the protein phosphatase calcineurin and was abolished by cyclosporin A and deltamethrin. Exocytosis was not affected by intracellular application of specific alpha(2), I(1), and I(2) ligands. Phentolamine reduced glucagon release (IC(50) = 1.2 microm) from intact islets by 40%, an effect abolished by pertussis toxin, cyclosporin A, and deltamethrin. These data suggest that imidazoline compounds inhibit glucagon secretion via G(i2)-dependent activation of calcineurin in the pancreatic alpha-cell. The imidazoline binding site is likely to be localized intracellularly and probably closely associated with the secretory granules. (+info)Substrate and inhibitor specificities for human monoamine oxidase A and B are influenced by a single amino acid. (5/92)
Monoamine oxidase (MAO) is responsible for the oxidation of biogenic and dietary amines. It exists as two isoforms, A and B, which have a 70% amino acid identity and different substrate and inhibitor specificities. This study reports the identification of residues responsible for conferring this specificity in human MAO A and B. Using site-directed mutagenesis we reciprocally interchanged three pairs of corresponding nonconserved amino acids within the central portion of human MAO. Mutant MAO A-I335Y became like MAO B, which exhibits a higher preference for beta-phenylethylamine than for the MAO A preferred substrate serotonin (5-hydroxytryptamine), and became more sensitive to deprenyl (MAO B-specific inhibitor) than to clorgyline (MAO A-specific inhibitor). The reciprocal mutant MAO B-Y326I exhibited an increased preference for 5-hydroxytryptamine, a decreased preference for beta-phenylethylamine, and, similar to MAO A, was more sensitive to clorgyline than to deprenyl. These mutants also showed a distinct shift in sensitivity for the MAO A- and B-selective inhibitors Ro 41-1049 and Ro 16-6491. Mutant pair MAO A-T245I and MAO B-I236T and mutant pair MAO A-D328G and MAO B-G319D reduced catalytic activity but did not alter specificity. Our results indicate that Ile-335 in MAO A and Tyr-326 in MAO B play a critical role in determining substrate and inhibitor specificities in human MAO A and B. (+info)Acute and chronic effects of desipramine and clorgyline on alpha(2)-adrenoceptors regulating noradrenergic transmission in the rat brain: a dual-probe microdialysis study. (6/92)
1. The effects of desipramine (3 mg kg(-1) i.p.) and clorgyline (1 mg kg(-1) i.p.) on extracellular noradrenaline (NA) in the locus coeruleus (LC) and cingulate cortex were assessed in freely-moving rats by dual-probe microdialysis. Functional activities of alpha(2)-adrenoceptors regulating NA release in the LC and cingulate cortex were determined by systemic (0.3 mg kg(-1) i.p.) or local (0.1 - 100 microM) clonidine administration. 2. Extracellular NA was increased in the LC and cingulate cortex following acute desipramine but not clorgyline treatment. Systemic clonidine decreased NA similarly in desipramine-, clorgyline-, and saline-treated animals, in both brain areas. 3. Long-term (twice daily, 14 days) but not short-term (twice daily, 7 days) desipramine, and long-term clorgyline (once daily, 21 days) treatments increased NA (3 fold) in cingulate cortex but not in the LC. Following long-term treatments, responses of NA to systemic clonidine were attenuated in the LC and cingulate cortex. 4. Clonidine perfusion by reverse dialysis into the cingulate cortex decreased local NA (-55 +/- 9%). The effect was attenuated by long-term desipramine (-31 +/- 9%) and clorgyline (-10 +/- 2%) treatments. 5. Clonidine perfusion by reverse dialysis into the LC decreased NA in the LC (-89 +/- 2%) and in cingulate cortex (-52 +/- 12%). This effect was attenuated in the LC following long-term desipramine (-72 +/- 4%) and clorgyline (-62 +/- 12%) treatments but it was not modified in the cingulate cortex (-57 +/- 10% and -68 +/- 6%, respectively). 6. These findings demonstrate that chronic desipramine or clorgyline treatments increase NA in noradrenergic terminal areas and desensitize alpha(2)-adrenoceptors modulating local NA release at somatodendritic and terminal levels. However, somatodendritic alpha(2)-adrenoceptors that control LC firing activity are not desensitized. (+info)Norepinephrine metabolism in neuron: dissociation between 3,4-dihydroxyphenylglycol and 3,4-dihydroxymandelic acid pathways. (7/92)
AIM: To investigate the pre-synaptic metabolism of norepinephrine (NE), judged by variations in plasma concentration of 3,4-dihydroxyphenylglycol (DHPG) and 3,4-dihydroxymandelic acid (DOMA). METHODS: Pithed and electrically stimulated (2.5 Hz) rats were given intravenous infusion of exogenous NE (6 nmol . kg-1 . min-1). Plasma NE, DHPG, DOMA, and the activities of mono- amine oxidases (MAO) were measured with the radio-enzymatic assay. RESULTS: Exogenous NE induces an about 100-fold increase in plasma NE concentration while blood pressure remained within normal limits. A 12-fold increase in plasma DHPG and 1.2-fold increase for DOMA were observed. When NE transportation across the pre-synaptic membrane was inhibited by desipramine (2 mg/kg, iv), a great reduction in plasma DHPG concentration (about 25 % of control) was observed while DOMA remained unchanged. When MAO-A activity was inhibited to 25 % of control by clorgyline (2 mg/kg, iv) and MAO-B to 30 % by deprenyl, the plasma DHPG and DOMA concentrations were reduced to 15 % and 70 % of controls, and to 26 % and 76 % of controls, respectively. When clorgyline and deprenyl were combined, plasma DHPG was vanished (less than 2 % of control) while plasma DOMA remained in the same range (72 % of control). CONCLUSION: The metabolizing system of NE in pre-synapse, associating with the pre-synaptic reuptake plus oxidative deamination on the external membrane of mitochondria, is predominant for the reduction to DHPG. (+info)Effects of monoamine oxidase inhibition by clorgyline, deprenil or tranylcypromine on 5-hydroxytryptamine concentrations in rat brain and hyperactivity following subsequent tryptophan administration. (8/92)
1 The effect of various doses of tranylcypromine on the degree of inhibition of rat brain monoamine oxidase (MAO) using 5-hydroxytryptamine (5-HT), dopamine and phenylethylamine as substrates has been examined 120 min after injection of the inhibitor. The concentration of brain 5-HT was also examined both after tranylcypromine alone and also when L-tryptophan (100 mg/kg) had been given 30 min after the tranylcypromine. 2 All doses of tranylcypromine greater than 2.5 mg/kg totally inhibited MAO oxidation of 5-HT, phenylethylamine and dopamine as measured in vitro and produced a similar rise of brain 5-HT in vivo. When tryptophan was also given, there was a further rise of brain 5-HT, which was comparable after all doses of tranylcypromine above 2.5 mg/kg and the characteristic syndrome of hyperactivity made is appearance. 3 Clorgyline (a "Type A" MAO inhibitor), in doses up to 10 mg/kg, did not totally inhibit MAO activity towards phenylethylamine although it did inhibit 5-HT oxidation by 100%. Deprenil (a "Type B" MAO inhibitor) at doses up to 10 mg/kg did not fully inhibit 5-HT oxidation although phenylethylamine oxidation was inhibited almost completely. Administration of either compound alone did not produce as great an accumulation of brain 5-HT as that seen after tranylcypromine (2.5 mg/kg) and subsequent administration of tryptophan did not cause hyperactivity or the rise of brain 5-HT seen after tranylcypromine (2.5 mg/kg) plus tryptophan. 4 Administration of clorgyline plus deprenil (2.5 mg/kg of each) almost totally inhibited oxidation of both 5-HT and phenylethylamine; subsequent tryptophan administration resulted in a rise of brain 5-HT nearly as great as that seen following tranylcypromine (2.5 mg/kg) plus tryptophan and the animals became hyperactive. 5 No evidence was found pointing to the formation of any other 5-substituted indole in the brain following tranylcypromine plus L-tryptophan administration as suggested by others. 6 It is concluded that while 5-HT may normally be metabolized in the brain by "Tye A" MAO in vivo, when this form is inhibited, 5-HT can still be metabolized by "Type B" enzyme. It is only when both forms are almost totally inhibited that the largest rise of brain 5-HT is seen and subsequent tryptophan administration produces the hyperactivity syndrome. (+info)
Quantitative distribution of rat brain monoamine oxidase A by [ 14 C]clorgyline autoradiography | SpringerLink
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most interesting drug for case study - Molecular Biology
Adelaide Research & Scholarship: An evaluation of potential mechanism-based inactivation of human drug metabolizing cytochromes...
RCSB PDB
- 2C72: Functional Role of the Aromatic Cage in Human Monoamine Oxidase B: Structures and Catalytic...
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Iproclozide - DrugBank
MAO Inhibitors - Food & Drug Interactions Medication InfoShare
Monoamine Oxidase | Article about Monoamine Oxidase by The Free Dictionary
CERI Q&A: Increased Deprenyl Mortality?
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Monoamine Oxidase A抗体|Abcam中国|Anti-Monoamine Oxidase A抗体(ab40835)
Anti-Monoamine Oxidase A/MAO-A antibody (ab232845) | Abcam
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Visualization of brain monoamine oxidase B (MAO-B) in dementia of Alzheimers type by means of large cryosection...
wikitox:2.1.11.9.2.2 monoamine oxidase inhibitors [WikiTox]
A Comprehensive Review of Monoamine Oxidase-A Inhibitors in their Syntheses and Potencies | Bentham Science
Monoamine oxidase type a in fibroblasts from patients with bipolar depressive illness<...
Serval - Inhibition of monoamine oxidase-B by condensed pyridazines and pyrimidines: effects of lipophilicity and structure...
Deprenyl reduces delayed neuronal death of hippocampal pyramidal cells<...
RCSB PDB
- 2BK5: Human Monoamine Oxidase B: I199F mutant in complex with isatin Structure Summary Page
Tranylcypromine - The Full Wiki
TB5 | MAO-B inhibitor | TB-5 | CAS [948841-07-4] | Axon 2629 | Axon Ligand™ with |100% purity available from stock from...
Psycho-Babble Alternative Thread 1096138
Patent US4861800 - Method for administering the drug deprenyl so as to minimize the danger of ... - Google Patents
Fighting The Blues With Greens? MAO Inhibitors In Plants | Care2 Healthy Living
Protriptyline (Vivactil) uses and side effects
Deprenyl Controversy - Life Extension
Types A and B monoamine oxidase contribute to the metabolism of norepinephrine in perfused lungs of rats - UQ eSpace
Monoamine Oxidase A peptide (141-154) (ab45814) | Abcam
DMOZ - Health: Pharmacy: Drugs and Medications: S: Selegiline
Tranylcypromine Dosing
Monoamine oxidase B - Wikipedia
Phenelzine - Wikipedia
nonselective inhibition of monoamine oxidase (MAO) enzymes (ie, isoforms A and - Small molecule epigenetic inhibitors targeted...
My mom (75 years old but biologically younger) has early parkinsons. Any downside to mao-b inhibitor instead of levodopa if...
pub H-BRS | Search
Monoamine oxidase B inhibitor, selegiline, reduces 18F-THK5351 uptake in the human brain | Alzheimers Research & Therapy |...
Which medications in the drug class MAO-B inhibitors are used in the treatment of Parkinson Disease?
Nardil Side Effects, Uses & Dosage
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Deprenyl in Parkinsons disease: a two-year study in the different evolutive stages. | CureHunter
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Azilect (Rasagiline)
Shaving - 2
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What about Deprenyl for Dopamine Decline?
Parnate (Tranylcypromine) Patient Information | HealthyPlace
Pargyline
1998). "Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (clorgyline) or MAO-B ( ... Clorgyline Rasagiline Selegiline Fisar Z, Hroudová J, Raboch J (2010). "Inhibition of monoamine oxidase activity by ...
Monoamine oxidase A
Clorgyline, an MAO-A enzyme inhibitor, prevents apoptosis in melanoma cells, in vitro. Cholangiocarcinoma suppresses MAO-A ... Cimoxatone Clorgyline (irreversible) Methylene Blue Minaprine (Cantor) Moclobemide (Aurorix, Manerix) Phenelzine (Nardil) ...
Clorgiline
... (INN), or clorgyline (BAN), is a monoamine oxidase inhibitor (MAOI) structurally related to pargyline which is ... 1998). "Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (clorgyline) or MAO-B ( ...
N-Acetylserotonin
The SSRI fluoxetine and the MAO-A inhibitor clorgyline upregulate AANAT indirectly through serotonergic mechanisms and thereby ... abolishes the hypotensive effects of clorgyline. NAS is produced from serotonin by the enzyme aralkylamine N-acetyltransferase ...
Idazoxan
... (INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor.[1][2] Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia. ...
Clorgyline | Profiles RNS
"Clorgyline" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... This graph shows the total number of publications written about "Clorgyline" by people in this website by year, and whether " ... Below are the most recent publications written about "Clorgyline" by people in Profiles. ...
Quantitative distribution of rat brain monoamine oxidase A by [ 14 C]clorgyline autoradiography | SpringerLink
... clorgyline in normal, conscious rat brain. [14C]clorgyline was synthesized by the methylation reaction of N-desmethylclorgyline ... Kondoh, Y., Murakami, M., Yin, W. et al. Quantitative distribution of rat brain monoamine oxidase A by [14C]clorgyline ... Quantitative distribution of rat brain monoamine oxidase A by [14C]clorgyline autoradiography. *Yasushi Kondoh1. , ... Salach JI, Detmer K (1979) The reaction of bovine and rat liver monoamine oxidase with [14C]-clorgyline and [14C]-deprenyl. Mol ...
Inactivation of cytochrome P4502B1 by the monoamine oxidase inhibitors R-(-)-deprenyl and clorgyline. | Drug Metabolism &...
... was 0.23 min-1 for deprenyl and 0.28 min-1 for clorgyline. The partition ratio for deprenyl and clorgyline was between 2 and 3 ... Inactivation of cytochrome P4502B1 by the monoamine oxidase inhibitors R-(-)-deprenyl and clorgyline.. U Sharma, E S Roberts ... Inactivation of cytochrome P4502B1 by the monoamine oxidase inhibitors R-(-)-deprenyl and clorgyline.. U Sharma, E S Roberts ... Inactivation of cytochrome P4502B1 by the monoamine oxidase inhibitors R-(-)-deprenyl and clorgyline.. U Sharma, E S Roberts ...
The Inhibition of Rat Heart Type A Monoamine Oxidase by Clorgyline as a Method for the Estimation of Enzyme Active Centers |...
The Inhibition of Rat Heart Type A Monoamine Oxidase by Clorgyline as a Method for the Estimation of Enzyme Active Centers. ... The Inhibition of Rat Heart Type A Monoamine Oxidase by Clorgyline as a Method for the Estimation of Enzyme Active Centers. ... The Inhibition of Rat Heart Type A Monoamine Oxidase by Clorgyline as a Method for the Estimation of Enzyme Active Centers. ... The interaction between clorgyline and the Type-A monoamine oxidase (MAO-A) in homogenates and mitochondrial fractions of the ...
Clorgyline-mediated reversal of neurological deficits in a Complexin 2 knockout mouse : Human Molecular Genetics - oi
Clorgyline-mediated reversal of neurological deficits in a Complexin 2 knockout mouse - Sheffield Hallam University Research...
For example, clorgyline-treated Cplx2-/- mice spent significantly more time interacting with a novel visitor mouse compared to ... Chronic treatment with clorgyline, an irreversible inhibitor of monoamine oxidase A, restored hippocampal noradrenaline to ... Clorgyline-mediated reversal of neurological deficits in a Complexin 2 knockout mouse ... Clorgyline-mediated reversal of neurological deficits in a Complexin 2 knockout mouse. Human Molecular Genetics, 19 (17), 3402- ...
Frontiers | Accumulation of Azole Drugs in the Fungal Plant Pathogen Magnaporthe oryzae Is the Result of Facilitated Diffusion...
In addition, we found that co-treatment of M. oryzae with repurposed clorgyline and radio-labeled fluconazole prevented ... Efflux Inhibition by Clorgyline. To test the effect of Clorgyline as a possible inhibitor of energy-dependent efflux in M. ... Clorgyline has recently been identified in a screen as an inhibitor of two C. albicans ABC efflux pumps, CaCdr1p and CaCdr2p, ... Clorgyline as a Potential Efflux Inhibitor. Development of a new drug structure and a new mechanism of action would be a ...
Anti-oncogenic and pro-differentiation effects of clorgyline, a monoamine oxidase A inhibitor, on high grade prostate cancer...
Clorgyline induces genes suppressed by oncogenic pathways. The 156 genes identified by SAM as upregulated by clorgyline in E-CA ... Validation of the effects of clorgyline using E-CA-90 cells. To validate the effects of clorgyline on E-CA cells, we treated E- ... Clorgyline upregulates AR and modulates expression of androgen-regulated genes. We previously reported that clorgyline induces ... Because clorgyline induced a subset of androgen-regulated genes while repressing others, it is possible that clorgyline ...
Beyond descriptive accuracy: The central dogma of molecular biology - Klotho (Biochemical Compounds Declarative Database)
Targeting monoamine oxidase A-regulated tumor-associated macrophage polarization for cancer immunotherapy | Nature...
5d, e). Notably, the MAOIs that we tested include phenelzine, clorgyline, moclobemide, and pirlindole, covering the major ... MAOIs studied were phenelzine (Phe, 20 μM) (Sigma-Aldrich), clorgyline (Clo, 20 μM) (Sigma-Aldrich), moclobemide (Moc, 200 μM ... MAOIs (monoamine oxidase inhibitors) studied were phenelzine (Phe; 20 μM), clorgyline (Clo; 20 μM), moclobemide (Moc; 200 μM), ... In our studies, we tested multiple clinically approved MAOIs (phenelzine, clorgyline, moclobemide, and pirlindole) and ...
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Carbamazepine (Intravenous Route) Description and Brand Names - Mayo Clinic
Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. If you think you have become pregnant while using the medicine, tell your doctor right away. Do not use carbamazepine together with a monoamine oxidase inhibitor (MAOI) or during the first 14 days after you stop taking a MAOI. MAOIs are used for depression and some examples are isocarboxazid (Marplan®), phenelzine (Nardil®), selegiline (Eldepryl®), or tranylcypromine (Parnate®). Do not use this medicine together with boceprevir (Victrelis®), delavirdine (Rescriptor®), and nefazodone (Serzone®). Serious skin reactions can occur with this medicine. Check with your doctor right away if you have blistering, peeling, or loose skin, red skin lesions, severe acne or skin rash, sores or ulcers on the skin, a fever, or chills while you are using this medicine. Check with your doctor right away if a fever, sore throat, rash, ulcers in the mouth, nosebleeds, ...
Phenothiazine (Oral Route, Parenteral Route, Rectal Route) Proper Use - Mayo Clinic
Do not take this medicine within 2 hours of taking antacids or medicine for diarrhea. Taking these products too close together may make this medicine less effective.. This medicine will add to the effects of alcohol and other central nervous system (CNS) depressants (medicines that slow down the nervous system, possibly causing drowsiness). Some examples of CNS depressants are antihistamines or medicine for hay fever, other allergies, or colds; sedatives, tranquilizers, or sleeping medicine; prescription pain medicine or narcotics; barbiturates; medicine for seizures; muscle relaxants; or anesthetics, including some dental anesthetics. Check with your doctor before taking any of the above while you are using this medicine.. Before using any prescription or over-the-counter (OTC) medicine for colds or allergies, check with your doctor. These medicines may increase the chance of developing heatstroke or other unwanted effects, such as dizziness, dry mouth, blurred vision, and constipation, while ...
Ceramic oxyanion emitter (Patent) | DOepatents
Monoamine Oxidase (MAO) Inhibitors - Biochemicals - Neuroscience - Products
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HDM Inhibitors
BioVision develops and offers a wide variety of products including assay kits, antibodies, recombinant proteins & enzymes, and other innovative research tools for studying Apoptosis, Metabolism, Cell Proliferation, Cellular Stress, Cell Damage and Repair, Diabetes, Obesity and Metabolic Syndrome, Stem Cell Biology, Gene Regulation, Signal Transduction, etc. BioVisions products are currently being sold in more than 60 countries worldwide.
N-Methyl-N-propargyl-3-(2,4-dichlorophenoxy)propylamine hydrochloride ≥97% (GC) | Sigma-Aldrich
Influence of monoamine oxidase inhibitors on striatonigral dynorphin system: a study with deprenyl and clorgyline<...
... a study with deprenyl and clorgyline. Together they form a unique fingerprint. * Clorgyline Medicine & Life Sciences ... Deprenyl, a MAO-B selective inhibitor (0.25, 0.5, 5, 10 or 20 mg/kg/day, subcutaneously (s.c.) for 4 d) and clorgyline, a MAO-A ... Deprenyl, a MAO-B selective inhibitor (0.25, 0.5, 5, 10 or 20 mg/kg/day, subcutaneously (s.c.) for 4 d) and clorgyline, a MAO-A ... Deprenyl, a MAO-B selective inhibitor (0.25, 0.5, 5, 10 or 20 mg/kg/day, subcutaneously (s.c.) for 4 d) and clorgyline, a MAO-A ...
Amine oxidases : function and dysfunction : proceedings of the 5th International Amine Oxidase Workshop, Galway, Ireland,...
Clorgyline effect on pineal melatonin biosynthesis in roman high- and low-avoidance rats.- Reboxetine prevents the ... Clorgyline effect on pineal melatonin biosynthesis in adrenalectomized rats pretreated with 6-hydroxydopamine.- Synergistic ... Inhibition of monoamine oxidase by clorgyline analogues.- Kinetics of inhibition of MAO-B by N-(2-aminoethyl)-p-chlorobenzamide ...
METHODS FOR TREATING VISCERAL PAIN - Porreca, Frank
Sleep EEG of patients with obsessive-compulsive disorder | SpringerLink
Tranylcypromine - The Full Wiki
Nefazodone : Wikis (The Full Wiki)
Search - NeL.edu
MAO-A was inhibited by the following drugs: pargyline > clorgyline > iproniazid > fluoxetine > desipramine > amitriptyline > ... MAO-B was inhibited by the following drugs: pargyline > clorgyline > iproniazid > fluoxetine > venlafaxine > amitriptyline > ... and clorgyline.. RESULTS: In general, the effect of tested drugs was found to be inhibitory. The half maximal inhibitory ... Clorgyline:pharmacology, Cocaine:pharmacology, Cy. OBJECTIVE: Monoamine oxidase (MAO), the enzyme responsible for metabolism of ...
Frontiers | New Insights into the Potential Roles of 3-Iodothyronamine (T1AM) and Newly Developed Thyronamine-Like TAAR1...
... and whether these effects are modified under conditions of MAO inhibition by clorgyline. Our results revealed that when i.p. ... and whether these effects are modified under conditions of MAO inhibition by clorgyline. Our results revealed that when i.p. ... kg-1 T1AM or SG-2 was lost with clorgyline pretreatment (Figure 3B). Notably, in control mice i.p. injected with clorgyline an ... FIGURE 3. SG-2 and T1AM reduce nociceptive threshold in mice and the effect is blunted by clorgyline pretreatment. (A) Mice ...
Citalopram | Encyclopedia.com
N-acetylserotonin activates TrkB receptor in a circadian rhythm | PNAS
5B Left). Clorgyline increases both melatonin and NAS levels in rat pineal glands (24). To explore which of the 5-HT ... B) The MAO-A inhibitor clorgyline but not MAO-B inhibitor deprenyl promotes TrkB activation in the dark in C3H mice. Phospho- ... 5B ). Interestingly, in C3H mice treated at night, clorgyline strongly activated TrkB in the dark; in contrast, it lost the ... Further, the finding that TrkB activation by clorgyline in C3H but not C57BL/6J mice is prevented by light exposure, which ...
Morphine (Injection route)
It is very important that your doctor check the progress or you or your child while you are receiving this medicine. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to use it. This medicine will add to the effects of alcohol and other CNS depressants (medicines that can make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for allergies or colds; sedatives, tranquilizers, or sleeping medicine; other prescription pain medicine or narcotics; medicine for seizures or barbiturates; muscle relaxants; or anesthetics, including some dental anesthetics. Check with your doctor before you or your child take any of the medicines listed above while you are using this medicine. This medicine may be habit-forming. If you or your child feel that the medicine is not working as well, do not use more than your prescribed dose. Call your doctor for instructions. Using narcotics for a long time can cause severe ...
Narcotic analgesics
... will add to the effects of alcohol and other central nervous system (CNS) depressants (medicines that slow down the nervous system, possibly causing drowsiness). Some examples of CNS depressants are antihistamines or medicine for hay fever, other allergies, or colds; sedatives, tranquilizers, or sleeping medicine; other prescription pain medicines including other narcotics; barbiturates; medicine for seizures; muscle relaxants; or anesthetics, including some dental anesthetics. Do not drink alcoholic beverages, and check with your medical doctor or dentist before taking any of the medicines listed above, while you are using this medicine. This medicine may cause some people to become drowsy, dizzy, or lightheaded, or to feel a false sense of well-being. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous if you are dizzy or are not alert and clearheaded. Dizziness, light-headedness, or fainting may ...
PargylineInhibitor clorgylineInhibitionInhibitorsDeprenyl and clorgylineMoclobemideIrreversibleMAOASelegilinePreferentially inhibitedInhibitsInactivationEnzymeChronicSignificantly increasedIneffectiveAminesMiceSecretoryDrugsRatsVivoConcentrationSpecificProteinEffectsDoseAdministrationStudiesEffectCellsGroupSignificantTopicPublications
Pargyline7
- Campbell IC, Robinson DS, Lovenberg W, Murphy DL (1979) The effects of chronic regimens of clorgyline and pargyline on monoamine metabolism in the rat brain. (springer.com)
- The several antidepressants and mood stabilizers were compared with effects of well known MAO inhibitors such as moclobemide, iproniazid, pargyline, and clorgyline. (nel.edu)
- The results from single point time dependent inhibition and shift assays suggest that clorgyline, pargyline, phenelzine, and selegiline were metabolism based inhibitors of CYP2B6. (sigmaaldrich.com)
- In IC50 shift assays, clorgyline, pargyline, phenelzine and selegiline are metabolism based inhibitors of CYP2B6 with fold shit of 3.0-, 3.7-, 2.9-, and 11.4-fold respectively. (sigmaaldrich.com)
- Persistent stimulation of dopamine receptors pargyline amoxapine phenelzine buspirone selegiline clozapine tranylcypromine droperidol haloperidol inhibit dopamine metabolismmaois metoclopramide clorgyline phenytoin isocarboxazid linezolid dopamine antagonism moclobemide block dopamine receptors. (childbirthsolutions.com)
- The results obtained were compared with the effects of the less-selective MAO-B inhibitor pargyline and the MAO-A inhibitor clorgyline. (lenus.ie)
- Clorgyline showed a smaller protective effect of normal cells, whereas pargyline had no effect. (lenus.ie)
Inhibitor clorgyline6
- To understand the mechanisms of specific substrate and inhibitor recognitions of MAOA and MAOB, we have determined the crystal structure of rat MAOA complexed with the specific inhibitor, clorgyline, at 3.2A resolution. (rcsb.org)
- Recently, the monoamine oxidase A (MAO-A) inhibitor clorgyline was shown to inhibit the azole efflux pumps, leading to increased azole susceptibility i. (medworm.com)
- The effects of chronic treatment with desimipramine (a tricyclic antidepressant), fluoxetine [a specific 5-hydroxytryptamine (5-HT) uptake inhibitor], clorgyline (a specific monoamine oxydase inhibitor of A type), ipsapirone (a specific 5-HT1A receptor agonist) as well as electroconvulsive shock treatment were investigated on rat hippocampal 5-HT1A receptors negatively coupled to adenylyl cyclase. (aspetjournals.org)
- Animal experiments were performed on normal Wistar rats and on rats pretreated with the monoamine oxidase (MAO) inhibitor clorgyline. (ugent.be)
- All of these in vitro changes occur, in part, independently from - and β-adrenergic receptor-operated signaling and are inhibited by the specific MAO-A inhibitor clorgyline. (scialert.net)
- The contractile response was assessed using phenylephrine (0,01-1 microM) in the presence vs. absence of a MAO-A inhibitor, clorgyline (10 microM). (ovid.com)
Inhibition6
- After an initial reversible interaction, the inhibition of enzyme activity becomes irreversible in the presence of concentrations of clorgyline of the same order as that of the enzyme. (aspetjournals.org)
- As the rats grew older, both the specific activity of MAO-A, and the concentration of clorgyline/(mg protein) required to cause inhibition of the enzyme activity increased in a parallel fashion. (aspetjournals.org)
- To assess potential neuroprotection by TAAR1 agonists, in the present work, we initially investigated whether T1AM and its corresponding 3-methylbiaryl-methane analog SG-2 can improve learning and memory when systemically administered to mice at submicromolar doses, and whether these effects are modified under conditions of MAO inhibition by clorgyline. (frontiersin.org)
- The prototype inhibitors ("suicide inactivators", which engender covalent bonds with the active site of the enzyme and induce irreversible inhibition) used in PET studies are [ 11 C]deprenyl and [ 11 C]clorgyline (Fowler et al. (aspetjournals.org)
- The comparison of the structures between MAOA and MAOB clearly explains the specificity of clorgyline for MAOA inhibition. (rcsb.org)
- The effect of cocaine on the overflow of noradrenaline was potentiated by prior inhibition of MAO with clorgyline. (springer.com)
Inhibitors6
- Inactivation of cytochrome P4502B1 by the monoamine oxidase inhibitors R-(-)-deprenyl and clorgyline. (aspetjournals.org)
- The monoamine oxidase inhibitors R-(-)-deprenyl (deprenyl) and clorgyline inactivated the 7-ethoxy-4-trifluoromethylcoumarin O-deethylase activity of purified cytochrome P4502B1 (P4502B1) in a reconstituted system containing P4502B1, NADPH-cytochrome P450 oxidoreductase, and L-alpha-phosphatidylcholine dilauroyl as the lipid. (aspetjournals.org)
- Sivam, SP 1993, ' Influence of monoamine oxidase inhibitors on striatonigral dynorphin system: a study with deprenyl and clorgyline ', Neuropeptides , vol. 25, no. 1, pp. 35-45. (elsevier.com)
- Now that we know clorgyline works, we can focus future drug testing on newer, safer MAO-A inhibitors, such as moclobemide, whose chemical bindings are reversible, unlike those of clorgyline," says Paolocci. (hopkinsmedicine.org)
- Hippocampal 5HT reuptake was slightly inhibited by clorgyline (IC50 205.0 mumol/l), while the other MAO-inhibitors were devoid of potency. (nih.gov)
- Monoamine oxidase inhibitors l-deprenyl and clorgyline protect nonmalignant human cells from ionising radiation and chemotherapy toxicity. (lenus.ie)
Deprenyl and clorgyline3
- The partition ratio for deprenyl and clorgyline was between 2 and 3. (aspetjournals.org)
- Co-administration of low doses (2.5 mg/kg/day, s.c. for 4 d) of deprenyl and clorgyline, that would selectively inhibit MAO-B and MAO-A respectively, produced a marked increase in DA and 5-HT, a decrease in DOPAC and 5-HIAA, an increase in DYN levels in the striatum and substantia nigra and an increase in PD-mRNA levels in the striatum. (elsevier.com)
- Since the Bcl-2 has been shown to be an inhibitor of apoptosis or programmed cell death, this would imply that the protective effects of l-deprenyl and clorgyline involve activation of antiapoptotic pathways within the normal cell. (lenus.ie)
Moclobemide2
- He says newer drugs in the same class, such as moclobemide (sold as Aurorix or Manerix, and already approved by the U.S. Food and Drug Administration), will have to be tested first, citing numerous and potentially lethal drug effects with clorgyline that prevent it from being prescribed. (hopkinsmedicine.org)
- R at i o n a l e s atypical antipsychotics inhibit dopamine metabolismmaois metoclopramide clorgyline phenytoin isocarboxazid linezolid dopamine antagonism moclobemide block dopamine receptors dopamine receptors. (childbirthsolutions.com)
Irreversible1
- Patients who have taken clorgyline, whose chemical binding to MAO-A is irreversible, had to carefully avoid such tyramine-rich foods as red wine, chocolate, certain beans, meat and especially aged cheeses. (hopkinsmedicine.org)
MAOA1
- Brain MAOA activity was measured with PET using clorgyline labeled with carbon 11. (mssm.edu)
Selegiline1
- Clorgyline Rasagiline Selegiline Fisar Z, Hroudová J, Raboch J (2010). (wikipedia.org)
Preferentially inhibited1
- Because of these observations, Johnston proposed that there are two forms of MAO: type A and type B. Type A, found mainly in the gut and other organs outside the brain, is preferentially inhibited by clorgyline. (mindandmuscle.net)
Inhibits1
- Clorgyline differed from deprenyl in two respects: 1) clorgyline selectively inhibits the deanimation of serotonin as opposed to phenylethylamine and 2) clorgyline potentiated tyramine induced hypertension (9). (mindandmuscle.net)
Inactivation3
- Deprenyl exhibited a KI (concentration of inactivator required for half-maximal inactivation) of 1.05 microM, and clorgyline had a KI of 1.5 microM. (aspetjournals.org)
- The maximum rate of inactivation of the enzyme at saturating levels of inactivator (kinactivation) was 0.23 min-1 for deprenyl and 0.28 min-1 for clorgyline. (aspetjournals.org)
- The inactivation of clorgyline was characterized by KI value of 2.5 ± 0.3 and k(inact) value of 0.045 ± 0.001 min(-1). (sigmaaldrich.com)
Enzyme1
- In a report to be published in the Jan. 8 edition of the journal Circulation Research, the international team of U.S. and Italian heart experts describes in a dozen key laboratory experiments in rodents how the antidepressant clorgyline, which is no longer in use in humans, blocks the action of enzyme monoamine oxidase-A (MAO-A) and stops its breakdown of a key neurohormone. (hopkinsmedicine.org)
Chronic1
- In contrast, chronic treatment with clorgyline and electroconvulsive shock treatment induced a slight but significant reduction of 5-HT's ability to inhibit hippocampal adenylyl cyclase. (aspetjournals.org)
Significantly increased2
- The expression of 156 genes was significantly increased by clorgyline at all time points over the time course of 6 - 96 hr identified by Significance Analysis of Microarrays (SAM). (biomedcentral.com)
- Treatment of cultures of nontumorigenic cells with l-deprenyl or clorgyline significantly increased the levels of the protein Bcl-2 following irradiation, but there was no such effect on the already-elevated levels of this protein in the tumour samples. (lenus.ie)
Ineffective1
- Clorgyline was ineffective as a protective agent. (cdc.gov)
Amines1
- For example if taking an MAO inhibitor (e.g., clorgyline) then the ingestion of sympathomimetic amines (e.g. amphetamine or even tyramine from cheese) will increase their [amines] apparent absorption as there is no longer functional MAO in the gut epithelium to degrade it. (protocol-online.org)
Mice2
- Among the study's first findings was that after six weeks, mice with failing hearts responded to concurrent low-dose clorgyline treatment, with restoration of normal heart function and only half the harmful changes seen in untreated mice over the same time period. (hopkinsmedicine.org)
- Heart muscle cell death rates were normal in clorgyline-treated mice, but three and a half times higher in untreated mice. (hopkinsmedicine.org)
Secretory2
- Clorgyline, an MAO-A inhibitor, induces secretory differentiation of normal prostate cells. (biomedcentral.com)
- Another striking effect of clorgyline was the induction of androgen receptor (AR) and classic AR target genes such as prostate-specific antigen together with other secretory epithelial cell-specific genes, suggesting that clorgyline promotes differentiation of cancer cells. (biomedcentral.com)
Drugs1
- Our study helps describe heart failure as a vicious chemical circle of stimulant norepinephrine overload and breakdown, and it offers a disease blueprint with monoamine oxidase-A as the target for drugs similar to clorgyline to rein in the disease," says senior study investigator and cardiologist Nazareno Paolocci, M.D. (hopkinsmedicine.org)
Rats1
- Another group of rats was pretreated with clorgyline (10 mg/kg i.v.). Monkeys were injected with [ 11 C]befloxatone (222-370 MBq), and the chest was imaged with PET for 2 h. (aspetjournals.org)
Vivo1
- The distribution of functionally active monoamine oxidase type A (MAO-A) was investigated by in vivo quantitative autoradiography using [ 14 C]clorgyline in normal, conscious rat brain. (springer.com)
Concentration1
- In addition, we found that co-treatment of M. oryzae with 'repurposed' clorgyline and radio-labeled fluconazole prevented energy-dependent efflux of fluconazole, resulting in an increased intracellular concentration of fluconazole in the fungal cell. (frontiersin.org)
Specific1
- The interaction between clorgyline and the Type-A monoamine oxidase (MAO-A) in homogenates and mitochondrial fractions of the rat heart appears to take place almost entirely at specific binding sites. (aspetjournals.org)
Protein1
- Notable side effects from clorgyline, Paolocci says, include insomnia and agitation, or high blood pressure after ingestion of foods containing the amino acid tyramine, a protein building block that stimulates a surge of stored stimulatory hormones, specifically, norepinephrine. (hopkinsmedicine.org)
Effects1
- We examined the effects of clorgyline on the transcriptional program of epithelial cells cultured from high grade PCa (E-CA). (biomedcentral.com)
Dose2
- Deprenyl, a MAO-B selective inhibitor (0.25, 0.5, 5, 10 or 20 mg/kg/day, subcutaneously (s.c.) for 4 d) and clorgyline, a MAO-A inhibitor (0.5, 5, 10 or 20 mg/kg/day, s.c. for 4 d) produced a dose-related increase in DA and 5-HT and a decrease in their metabolites in the striatum. (elsevier.com)
- In rodents, cardiac uptake was high (3.39 ± 0.5% injected dose/g tissue) and strongly inhibited (80%) by clorgyline. (aspetjournals.org)
Administration2
- Sixty minutes after [ 14 C]clorgyline administration (1.58 MBq/animal i.v.), the brains were removed and prepared for autoradiography by washing the brain sections with 5% trichloroacetic acid solution to remove the nonbinding free tracer. (springer.com)
- Autonomic and Behavioral Thermoregulation in the Golden Hamster during Subchronic Administration of Clorgyline. (epa.gov)
Studies1
- Paolocci cautions that their studies with clorgyline are initial proof of an important principle, but far from any current use of the drug to treat heart disease in humans. (hopkinsmedicine.org)
Effect2
- In addition, genes downregulated ≥ 2-fold by clorgyline were significantly enriched with those upregulated by key oncogenes including beta-catenin and ERBB2, indicating an anti-oncogenic effect of clorgyline. (biomedcentral.com)
- Indeed, many genes in the PcG repression signature that predicts PCa outcome were upregulated by clorgyline, suggesting that the differentiation-promoting effect of clorgyline may be mediated by its downregulation of EZH2. (biomedcentral.com)
Cells1
- We systematically assessed gene expression changes induced by clorgyline in E-CA cells using high-density oligonucleotide microarrays. (biomedcentral.com)
Group2
- Moreover, clorgyline downregulated EZH2, a critical component of the Polycomb Group (PcG) complex that represses the expression of differentiation-related genes. (biomedcentral.com)
- Heart muscle chamber expansion also slowed in the clorgyline-treated group, returning to an average chamber dimension of 1.2 millimeters, when the heart was contracting. (hopkinsmedicine.org)
Significant1
- PET images showed clear accumulation of C-11-hydroxytryptophan in the pancreas in both animal groups, but with a significant 3-fold higher retention of the radiopharmaceutical in clorgyline-treated animals. (ugent.be)
Topic1
- This graph shows the total number of publications written about "Clorgyline" by people in this website by year, and whether "Clorgyline" was a major or minor topic of these publications. (umassmed.edu)
Publications1
- Below are the most recent publications written about "Clorgyline" by people in Profiles. (umassmed.edu)