Abstract
Objectives: The present study was designed to investigate the anti-depressant activity of 5 – aminoindazole and the possible mechanism involved.
Methods: Anti-depressant activity was evaluated in mice by employing forced swim test. The involvement of opioidergic system was investigated by using naloxone.
Results: 5 - aminoindazole exhibited a significant and dose dependent reduction in period of immobility in the forced swim test. Pretreatment with naloxone attenuated the reduction in immobility period produced by 5 - aminoindazole.
Conclusion: The investigated 5 - aminoindazole exhibited promising anti-depressant activity in animal models of depression. The participation of opioidergic mechanism in the antidepressant activity of 5 - aminoindazole was elucidated from the results.
References
Andrew JS, Ju G, Michael B, Eugene B, Dariusz W, Anil V, Andrew SJ, Mathew M, Sevan B, Brian D, Robin S, Lisa EH, Kennan CM, Hing LS, Christine AC and Philip RK. Discovery and Characterization of Aminopiperidinecoumarin Melanin Concentrating Hormone Receptor 1 Antagonists. Journal of medicinal chemistry 2005; 48 (5): 1318 – 1321.
Aran VJ, Ochoa C, Boiani L, Buccino P, Cerecetto H, Gerpe A, Gonzalez M, Montero D, Nogal JJ, Gomez-Barrio A, Azqueta A, Lopez de Cerain A, Piro OE and Castellano EE. Synthesis and biological properties of new 5-nitroindazole derivatives. Bioorg Med Chem 2005; 13(9): 3197 – 207.
Bodkin JA, Zorenberg GL, Lukas SE and Cole JO. Buprenorphine treatment of refractory depression. J Clin Psychopharmacology. 15: 49 – 57; 1995.
Djurovic D, Milic-Askrabic J and Majikic-Singh N. Serum beta endorphin level in patients with depression on fluvoxamine. Farmaco. 54: 130 – 133; 1999.
Fichna J, Janecka A, Costentin J, and Jean - Claude Do Rego. The Endomorphin System and Its Evolving Neurophysiological. Pharmacol Rev. 59: 88 – 123; 2007.
Jesse AM, Anura PD, Paul WZ, Marsha AM and Najam AS. Oral Cholesteryl Ester Transfer Protein (CETP) Inhibitors:? A Potential New Approach for Treating Coronary Artery Disease. Journal of medicinal chemistry 2006; 49(1): 318 – 328.
Jian XD, Xiaohong C, Fanying M, Leslie L, Charles H and Mark M. Potent Antitubulin Tumor Cell Cytotoxins Based on 3-Aroyl Indazoles. J. Med. Chem 2007; 50 (5): 1001 - 1006.
Jin CL, Fang YL, Li JH, Shiow LP, Jih HG and Che MT. 1-Benzyl – 3 - (5’-hydroxymethyl – 2’ -furyl) indazole (YC-1) Derivatives as Novel Inhibitors Against Sodium Nitroprusside - Induced Apoptosis. Journal of Medicinal Chemistry 2002; 45(23): 4947– 4949.
Kessler RC, Berglund P, Demler O, Jin R, Merikangas KR, Walters EE. Lifetime prevalence and age-of-onset distributions of DSM-IV disorders in the National Co morbidity Survey Replication. Arch Gen Psych 2005; 62(6): 593–602
O’Donnell JM, Shelton RC. Drug Therapy of Depression and Anxiety Disorders. In: Brunton L, Chabner B, Knollman B, editors. Goodman and Gilman's the Pharmacological Basis of Therapeutics. 12th ed. New York: McGraw Hill. pp. 397–415; 2011.
Porsolt RD, Bertin A and Jalfre M. Behavioural despair in rats and mice: Strain differences and the effects of imipramine. Eur. J. Pharmacol. 51(3): 291 – 294; 1978.
Robert JS, Edward M, Mark AA, William JM, William RS, Eugene TCC. Chadwick SC, Thomas K, Amy E, Lisa BM, James CK, Zhang Xu, Lydia M and Douglas CH. Synthesis and Activity of Substituted 4-(Indazol-3-yl)phenols as Pathway – Selective Estrogen Receptor Ligands Useful in the Treatment of Rheumatoid Arthritis. Journal of medicinal chemistry 2004; 47 (26): 6435 – 6438.
Rush AJ, Trivedi MH, Wisniewski SR, Nierenberg AA, Stewart JW, Warden D, Niederehe G, Thase ME, Lavori PW, Lebowitz BD, McGrath PJ, Rosenbaum JF, Sackeim HA, Kupfer DJ, Luther J, Fava M. Acute and longer-term outcomes in depressed outpatients requiring one or several treatment steps: a STARD report. Am J Psychiatry. 163: 1905 – 1917; 2006.
Thomas JS, Leroy JH, Charles SD and Guy SL. Synthesis and hypotensive activity of a series of 2-substituted 5,6-dimethoxyindazoles. Journal of Pharmaceutical Sciences 2003; 67 (7): 1022 – 1024.
Vasiliki G, Ioannis KK, Nicole P, Panagiotis M, Olga Ch, Kousidou GN. Tzanakakis and Nikos KK, Design. Synthesis and Evaluation of the Antiproliferative Activity of a Series of Novel Fused Xanthenone Aminoderivatives in Human Breast Cancer Cells. Journal of medicinal Chemistry 2007; 50(7): 1716 – 1719.
Wyrick SD, Voorstad PJ, Cocolas G and Hall IH. Hypolipidemic activity of phthalimide derivatives. 7. Structure-activity studies of indazolone analogues. J Med Chem 1984; 27(6): 768 -72.
This work is licensed under a Creative Commons Attribution-NoDerivatives 4.0 International License.
Copyright (c) 2020 Array