Serotonergic-like profile of 4-propyl-2H-benzo[h]-chromen-2-one (FCS-304) in mice and rats

Laura M. MORENO; Luis Enrique CUCA; Mario F. GUERRERO

doi:10.17533/udea.vitae.v26n1a03

Serotonergic-like profile of 4-propyl-2H-benzo[h]-chromen-2-one (FCS-304) in mice and rats

Revista Vitae ◽

10.17533/udea.vitae.v26n1a03 ◽

2019 ◽

Vol 26 (1) ◽

pp. 17-22

Author(s):

Laura M. MORENO ◽

Luis Enrique CUCA ◽

Mario F. GUERRERO

Keyword(s):

Mao A

ANTECEDENTES: 4-propil-2H-benzo [h] -cromen-2-ona (FCS-304) es una cumarina semisintética con actividad inhibidora de MAO-A y resultados positivos en natación forzada y prueba de suspensión de cola en ratones, pero hasta ahora, no se ha estudiado en otros modelos de antidepresivos de detección en ratones y ratas.OBJETIVOS: El objetivo de este trabajo fue evaluar el efecto similar a la serotonina de FCS-304 en la prueba de 5-hidroxitriptófano (5-HTP) en ratones, en la prueba de desesperación del comportamiento en ratas y en la prueba de reserpina en ratas.MÉTODOS: Se evaluó la potenciación de 5-HTP (100 mg / kg, ip), sacudidas de cabeza inducidas en ratones, previamente tratados con FCS-304 (50-75-150 mg / Kg, po). La prueba de desesperación del comportamiento se realizó en ratas tratadas con FCS-304, registrando el tiempo de inmovilidad alcanzado por los animales sometidos a natación forzada. Se examinó el antagonismo de la ptosis inducida por reserpina en ratas, evaluando el nivel de cierre palpebral. La imipramina (30 mg / kg, po) y el vehículo (aceite de canola) sirvieron como controles positivos y negativos, respectivamente.RESULTADOS: FCS-304 potenció significativamente las contracciones en la cabeza inducidas por 5-HTP en ratones, de una manera dependiente de la dosis. En ratas, FCS-304 redujo significativamente el tiempo de inmovilidad en la prueba de desesperación conductual y antagonizó la ptosis inducida por reserpina.CONCLUSIÓN: Estos resultados agregan apoyo para proponer que el FCS-304 podría provocar efectos antidepresivos relacionados con la actividad inhibidora de MAO-A.

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Estrogen Drop + MAO-A Enzyme Rise = The Biology of Postpartum Blues Uncovered

PsycEXTRA Dataset ◽

10.1037/e546422011-002 ◽

2010 ◽

Keyword(s):

Postpartum Blues ◽

Mao A

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Seaweeds: new source of MAO-A inhibiting compounds

Planta Medica ◽

10.1055/s-0031-1282827 ◽

2011 ◽

Vol 77 (12) ◽

Cited By ~ 2

Author(s):

C Grosso ◽

PB Andrade ◽

P Valentão ◽

T Mouga ◽

AK Jäger

Keyword(s):

Mao A

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Vers une « nouvelle histoire » du communisme chinois

Annales Histoire Sciences Sociales ◽

10.3406/ahess.1985.283209 ◽

1985 ◽

Vol 40 (4) ◽

pp. 931-943

Author(s):

Yves Chevrier

Keyword(s):

Mao Zedong ◽

Mise En Œuvre ◽

Mao A

Dans une étude classique sans cesse rééditée depuis trente ans (Chinese Communism and the Rise of Mao, Harvard Univ. Press, 1951), Benjamin Schwartz attribuait la victoire du parti communiste dans la révolution chinoise et l'ascension de Mao Zedong au sein de ce Parti à la mise au point — par Mao — d'une « formule » révolutionnaire originale reposant sur la paysannerie et sur l'armée. Avec le tournant des soviets du Jiangxi (1928-1934), Mao s'était fait l'homme de la militarisation et de la ruralisation d'une stratégie jusqu'alors calquée sur le modèle urbain des révolutions européennes, modèle que l'Internationale communiste avait relayé et appliqué sans succès en Chine dans les années 1920. La mise en oeuvre de la guérilla rurale avait opposé Mao à Moscou et plus encore aux hommes de Moscou, maîtres du Comité central demeuré clandestinement à Shanghai après le désastre de 1927 : Li Lisan tout d'abord (1929-1930) puis, derrière Wang Ming et Bo Gu, les « Vingt-huit bolcheviks ». En 1933, l'installation du Comité central à Ruijin (capitale des soviets du Jiangxi) avait consacré, selon Schwartz, la victoire d'une légitimité des faits (Mao) sur la légalité (les hommes de Shanghai et de Moscou).

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Inhibition of Butyrylcholinesterase and Human Monoamine Oxidase-B by the Coumarin Glycyrol and Liquiritigenin Isolated from Glycyrrhiza uralensis

Molecules ◽

10.3390/molecules25173896 ◽

2020 ◽

Vol 25 (17) ◽

pp. 3896

Author(s):

Geum Seok Jeong ◽

Myung-Gyun Kang ◽

Joon Yeop Lee ◽

Sang Ryong Lee ◽

Daeui Park ◽

...

Keyword(s):

Monoamine Oxidase ◽

Binding Affinity ◽

Competitive Inhibitor ◽

Glycyrrhiza Uralensis ◽

Form Hydrogen Bond ◽

Docking Simulations ◽

Mao B ◽

Mao A ◽

Ic50 Values ◽

Noncompetitive Inhibitor

Eight compounds were isolated from the roots of Glycyrrhiza uralensis and tested for cholinesterase (ChE) and monoamine oxidase (MAO) inhibitory activities. The coumarin glycyrol (GC) effectively inhibited butyrylcholinesterase (BChE) and acetylcholinesterase (AChE) with IC50 values of 7.22 and 14.77 µM, respectively, and also moderately inhibited MAO-B (29.48 µM). Six of the other seven compounds only weakly inhibited AChE and BChE, whereas liquiritin apioside moderately inhibited AChE (IC50 = 36.68 µM). Liquiritigenin (LG) potently inhibited MAO-B (IC50 = 0.098 µM) and MAO-A (IC50 = 0.27 µM), and liquiritin, a glycoside of LG, weakly inhibited MAO-B (>40 µM). GC was a reversible, noncompetitive inhibitor of BChE with a Ki value of 4.47 µM, and LG was a reversible competitive inhibitor of MAO-B with a Ki value of 0.024 µM. Docking simulations showed that the binding affinity of GC for BChE (−7.8 kcal/mol) was greater than its affinity for AChE (−7.1 kcal/mol), and suggested that GC interacted with BChE at Thr284 and Val288 by hydrogen bonds (distances: 2.42 and 1.92 Å, respectively) beyond the ligand binding site of BChE, but that GC did not form hydrogen bond with AChE. The binding affinity of LG for MAO-B (−8.8 kcal/mol) was greater than its affinity for MAO-A (−7.9 kcal/mol). These findings suggest GC and LG should be considered promising compounds for the treatment of Alzheimer’s disease with multi-targeting activities.

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Development of Monoamine Oxidase and Aldehyde Dehydrogenase in Reaggregating Cultures of Fetal Rat Brain Cells

Alternatives to Laboratory Animals ◽

10.1177/026119298901600313 ◽

1989 ◽

Vol 16 (3) ◽

pp. 281-286

Author(s):

Olof Tottmar ◽

Maria Söderbäck ◽

Anders Aspberg

Keyword(s):

Monoamine Oxidase ◽

Rat Brain ◽

Aldehyde Dehydrogenase ◽

Brain Cells ◽

Mao B ◽

Adult Rat ◽

Fetal Rat ◽

Adult Rat Brain ◽

Mao A ◽

Fetal Rat Brain

The development of monoamine oxidase (MAO) and aldehyde dehydrogenase (ALDH) in reaggregation cultures of fetal rat brain cells was compared with that of enzymatic markers for glial and neuronal cells. Only MAO-A was detected in the cultures during the first week, but, during the following three weeks, the activity of MAO-B increased more rapidly than that of MAO-A. The ratio MAO-A/MAO-B in four-week aggregates was close to that found in the adult rat brain. The activity of ALDH started to increase rapidly after 15 days, and the developmental pattern was intermediate to those of the glial and neuronal markers. The activity after four weeks was close to that found in the adult rat brain. Epidermal growth factor (EGF) caused a slight decrease in the activities of the low-Km ALDH (after four weeks) and the neuronal marker, choline acetyltransferase (after two weeks), whereas the other markers were not affected. By contrast, the activities of MAO-A and MAO-B were greatly increased during almost the entire culture period. It is suggested that this effect of EGF was the result of increased mitotic activity and/or biochemical differentiation of other cell types present in the cell aggregates, e.g. capillary endothelial cells.

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Strategy to develop a MAO-A-resistant 5-hydroxy-l-[β-11C]tryptophan isotopologue based on deuterium kinetic isotope effects

EJNMMI Research ◽

10.1186/s13550-014-0062-2 ◽

2014 ◽

Vol 4 (1) ◽

Cited By ~ 1

Author(s):

Jonas Eriksson ◽

Ola Åberg ◽

Ram Kumar Selvaraju ◽

Gunnar Antoni ◽

Lars Johansson ◽

...

Keyword(s):

Isotope Effects ◽

Kinetic Isotope Effects ◽

Kinetic Isotope ◽

Mao A

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In Vitro,In Vivo, and Clinical Studies of Tedizolid To Assess the Potential for Peripheral or Central Monoamine Oxidase Interactions

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00431-13 ◽

2013 ◽

Vol 57 (7) ◽

pp. 3060-3066 ◽

Cited By ~ 61

Author(s):

S. Flanagan ◽

K. Bartizal ◽

S. L. Minassian ◽

E. Fang ◽

P. Prokocimer

Keyword(s):

Blood Pressure ◽

Monoamine Oxidase ◽

Clinical Research ◽

Systolic Blood Pressure ◽

Clinical Studies ◽

Geometric Mean ◽

Interaction Study ◽

Mao B ◽

Mao A

ABSTRACTTedizolid phosphate is a novel oxazolidinone prodrug whose active moiety, tedizolid, has improved potency against Gram-positive pathogens and pharmacokinetics, allowing once-daily administration. Given linezolid warnings for drug-drug and drug-food interactions mediated by monoamine oxidase (MAO) inhibition, including sporadic serotonergic toxicity, these studies evaluated tedizolid for potential MAO interactions.In vitro, tedizolid and linezolid were reversible inhibitors of human MAO-A and MAO-B; the 50% inhibitory concentration (IC50) for tedizolid was 8.7 μM for MAO-A and 5.7 μM for MAO-B and 46.0 and 2.1 μM, respectively, with linezolid. Tedizolid phosphate was negative in the mouse head twitch model of serotonergic activity. Two randomized placebo-controlled crossover clinical studies assessed the potential of 200 mg/day tedizolid phosphate (at steady state) to enhance pressor responses to coadministered oral tyramine or pseudoephedrine. Sensitivity to tyramine was determined by comparing the concentration of tyramine required to elicit a ≥30-mmHg increase in systolic blood pressure (TYR30) when administered with placebo versus tedizolid phosphate. The geometric mean tyramine sensitivity ratio (placebo TYR30/tedizolid phosphate TYR30) was 1.33; a ratio of ≥2 is considered clinically relevant. In the pseudoephedrine study, mean maximum systolic blood pressure was not significantly different when pseudoephedrine was coadministered with tedizolid phosphate versus placebo. In summary, tedizolid is a weak, reversible inhibitor of MAO-A and MAO-Bin vitro. Provocative testing in humans and animal models failed to uncover significant signals that would suggest potential for hypertensive or serotonergic adverse consequences at the therapeutic dose of tedizolid phosphate. Clinical studies are registered atwww.clinicaltrials.govas NCT01539473 (tyramine interaction study conducted at Covance Clinical Research Center, Evansville, IN) and NCT01577459 (pseudoephedrine interaction study conducted at Vince and Associates Clinical Research, Overland Park, KS).

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