Serotonergic-like profile of 4-propyl-2H-benzo[h]-chromen-2-one (FCS-304) in mice and rats
Background: 4-propil-2H-benzo[h]-cromen-2-ona (FCS-304) is a semisynthetic coumarin with MAO-A inhibitory activity and positive results in forced swimming and tail suspension test in mice, but until now, it has not been studied in other screening antidepressant models in mice and rats. Objectives: The aim of this work was to assess the serotonin like effect of FCS-304 in the 5-hydroxytryptophan (5-HTP) test in mice, in the behavioral despair test in rats, and in the reserpine test in rats. Methods: Potentiation of 5-HTP (100 mg/kg, i.p.), induced head twitches were assessed in mice, previously treated with FCS-304 (50-75-150 mg/kg, p.o.). The behavioral despair test was performed in rats treated with FCS-304, recording the immobility time attained by the animals subjected to forced swimming. Antagonism of reserpine-induced ptosis was examined in rats, assessing the level of palpebral closure. Imipramine (30 mg/kg, p.o.) and vehicle (canola oil) served as positive and negative controls, respectively. Results: FCS-304 significantly potentiated 5-HTP induced head twitches in mice, in a dose dependent manner. In rats, FCS-304 significantly decreased the immobility time in the behavioral despair test and antagonized reserpine induced ptosis. Conclusions: These results add support to propose that FCS-304 could elicit antidepressant effects related to MAO-A inhibitory activity.
Kessler RC, Bromet EJ. The epidemiology of depression across cultures. Annu Rev Public Health. 2013;34:119-38.
Chaskel R, Gaviria SL, Espinel Z, Taborda E, Vanegas R, Shultz JM. Mental health in Colombia. BJPsych Int. 2015 Nov 1;12(4):95-97.
Pampallona S, Bollini P, Tibaldi G, Kupelnick B, Munizza C. Combined pharmacotherapy and psychological treatment for depression: a systematic review. Arch Gen Psychiatry. 2004 Jul;61(7):714-9.
Pemberton R, Fuller Tyszkiewicz MD. Factors contributing to depressive mood states in everyday life: A systematic review. J Affect Disord. 2016 Aug;200:103-10.
Cipriani A, Furukawa TA, Salanti G, Chaimani A, Atkinson LZ, Ogawa Y, Leucht S, Ruhe HG, Turner EH, Higgins JPT, Egger M, Takeshima N, Hayasaka Y, Imai H, Shinohara K, Tajika A, Ioannidis JPA, Geddes JR. Comparative efficacy and acceptability of 21 antidepressant drugs for the acute treatment of adults with major depressive disorder: a systematic review and network metaanalysis. Lancet. 2018 Apr 7;391(10128):1357-1366.
Bied AM, Kim J, Schwartz TL. A critical appraisal of the selegiline transdermal system for major depressive disorder. Expert Rev Clin Pharmacol. 2015;8(6):673-81.
Finberg JP, Rabey JM. Inhibitors of MAO-A and MAO-B in Psychiatry and Neurology. Front Pharmacol. 2016 Oct 18;7:340.
Chiuccariello L, Cooke RG, Miler L, Levitan RD, Baker GB, Kish SJ, Kolla NJ, Rusjan PM, Houle S, Wilson AA, Meyer
JH. Monoamine Oxidase-A Occupancy by Moclobemide and Phenelzine: Implications for the Development of Monoamine
Vergel NE, López JL, Orallo F, Viña D, Buitrago DM, del Olmo E, Mico JA, Guerrero MF. Antidepressant-like profile and MAO-A inhibitory activity of 4-propyl-2H-benzo[h]-chromen2-one. Life Sci. 2010 May 22;86(21-22):819-24.
Potdar MK, Mohile SS, Salunkhe MM. Coumarin syntheses via Pechmann condensation in Lewis acidic chloroaluminate ionic liquid. Tetrahedron Letters. 2001;42(52):9285–9287.
Koe BK, Weissman A, Welch WM, Browne RG. Sertraline, 1S,4S-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro1-naphthylamine, a new uptake inhibitor with selectivity for serotonin. J Pharmacol Exp Ther. 1983 Sep;226(3):686-700.
Kato M, Katayama T, Iwata H, Yamamura M, Matsuoka Y, Narita H. In vivo characterization of T-794, a novel reversible inhibitor of monoamine oxidase-A, as an antidepressant with a wide safety margin. J Pharmacol Exp Ther. 1998 Mar;284(3):983-90.
Porsolt RD, Bertin A, Jalfre M. Behavioral despair in mice: a primary screening test for antidepressants. Arch Int Pharmacodyn Ther. 1977 Oct;229(2):327-36.
Lapa AJ, Souccar C, Lima MT, Lima TCM. Métodos farmacológicos para el estudio de actividad sobre el sistema
nervioso central. In: CY TED/CNPq (Ed), Métodos de evaluación de la actividad farmacológica de plantas medicinales. Florianópolis, Santa Catarina, pp 70–90, 2002.
Worms P, Kan JP, Wermuth CG, Roncucci R, Bizière K. SR 95191, a selective inhibitor of type A monoamine oxidase with dopaminergic properties. I. Psychopharmacological profile in rodents. J Pharmacol Exp Ther. 1987 Jan;240(1):241-50.
Nowakowska E1, Chodera A. Inhibitory monoamine oxidases of the new generation. Pol Merkur Lekarski. 1997 Jul;3(13):1-4. 30. Corne SJ, Pickering RW, Warner BT. A method for assessing the effects of drugs on the central actions of 5-hydroxytryptamine. Brit. J. Pharmacol. 1963;20:106 120.
Mahesh R, Jindal A, Gautam B, Bhatt S, Pandey D. Evaluation of anti-depressant-like activity of linezolid, an oxazolidinone class derivative - an investigation using behavioral tests battery of depression. Biochem Biophys Res Commun. 2011 Jun 17;409(4):723-6.
Castagné V, Moser P, Roux S, Porsolt RD. Rodent models of depression: forced swim and tail suspension behavioral despair tests in rats and mice. Curr Protoc Neurosci. 2011 Apr;Chapter 8:Unit 8.10A.
Ozerov AA, Bagmetova VV, Chernysheva YV, Tyurenkov IN. Comparison of the Efficiency of Adeprophen and Antidepressants of Various Groups on the Model of Reserpine-Induced Depression in Rats. Bull Exp Biol Med. 2016 Mar;160(5):649-52.
Naoi M, Maruyama W, Inaba-Hasegawa K. Type A and B monoamine oxidase in age-related neurodegenerative disorders: their distinct roles in neuronal death and survival. Curr Top Med Chem. 2012;12(20):2177-88.
Pathak A, Srivastava AK, Singour PK, Gouda P. Synthetic and Natural Monoamine Oxidase Inhibitors as Potential Lead Compounds for Effective Therapeutics. Cent Nerv Syst Agents Med Chem. 2016;16(2):81-97
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