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Antidepressant-like activity of 2-pyrazoline derivatives

Year 2013, Volume: 3 Issue: 3, 154 - 158, 30.01.2014

Abstract

Objective: Depression is a common chronic recurrent psychiatric disorder, characterised by clusters of symptoms affecting many different systems. Due to complexity of the pathogenesis and differences in response to treatment, current therapies are incapable of providing an exact recovery, leading to attempts to investigate new treatment options. In many studies, it is shown that pyrazoline derivatives have the therapeutic potential as antidepressant agents. In this study, we aimed to investigate the antidepressant-like profile of a series of new 2-pyrazoline derivatives.

Methods: Antidepressant-like activity was evaluated by using tail suspension test, which was followed by forced swim test for those compounds found effective in tail suspension test in Balb/c mice.The behavioural parameter observed in both tests was immobility period, which is an indicative of antidepressant-like effect.

Results: Test compounds 3d and 3e were effective and a significant reduction in immobility time was observed when compared to results of imipramin, as the reference drug. Additionally, these two compounds did not alter the locomotor activity in mice.

Conclusion: Our results indicate that two 2-pyrazoline derivatives, 3d and 3e, are potential compounds for use in designing of new candidates for the treatment of depression.


Key words: Antidepressant-like activity, 2-pyrazoline derivatives, forced swim test, tail suspension test

References

  • Mental health and development: Targeting people with mental health conditions as a vulnerable group. World Health Organisation, Geneva, 2010.
  • Schechter LE, Ring RH, Beyer CE, Hughes ZA, Khawaja X, Malberg JE, Rosenzweig-Lipson S. Innovative approaches for the development of antidepressant drugs: Current and future strategies. NeuroTherapeutics 2005; 2:590-611.
  • Reynolds EH. Brain and mind: a challenge for WHO. Lancet 2003; 361: 1924‐1925.
  • Vinayak M, Ruckmani A, Chandrashekar K, VenuGopal R.K, Madhavi E, Swati B, Madhusudhan N, Antidepressant activity of ethanolic extract Piper betle leaves in mice. Curr Res Neurosci. 2012; 2 (1): 11-16.
  • Petit-Demouliere B, Chenu F, Bourin M. Forced swimming test in mice: a review of antidepressant activity. Psychopharmacology 2005; 177: 245-255.
  • Santosh P, Venugopl R, Nılakash A S, Kunjbıharı S, Dr. Mangala L. Antidepressant activity of methanolic extract of passiflora foetida leaves in mice. Int J of Pharm Pharmaceut Sci. 2011; 3: 112-115.
  • Rodrigues ALS, Rosa JM, Gadotti VM, Goulart EC, Stos MM, Silva AV, Sehnem B, Rosa LS , Goncalves RM, Correa R, Santos AR. Anti-depressant-like and antinociceptive-like actions of 4-(4’-chlorophenyl)-6-(4’’-methylphenyl)-2-hydrazinepyrimidine Mannich base in mice. Pharmaco Biochem Behav. 2005; 82: 156-162.
  • Özdemir A, Turan-Zitouni G, Kaplancıklı ZA, Revial G, Güven K. Synthesis and antimicrobial activity of 1-(4-aryl-2-thiazolyl)-3-(2thienyl)-5-aryl-2-pyrazoline derivatives. Eur J Med Chem. 2007; 42(3): 403-40
  • Shoman ME, Abdel-Aziz M, Aly OM, Farag HH, Morsy MA. Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives. Eur J Med Chem. 2009; 44(7): 3068-3076.
  • Özdemir Z, Kandilci HB, Gümüşel B, Çalış Ü, Bilgin AA. Synthesis and studies on antidepressant and anticonvulsant activities of some 3-(2-furyl)-pyrazoline derivatives. Eur J Med Chem. 2007; 42(3):3733
  • Satyanarayana M, Tiwari P, Tripathi BK, Srivastava AK, Pratap R. Synthesis and antihyperglycemic activity of chalcone based aryloxypropanolamines. Bioorg Med Chem. 2004; 12(5):883-889.
  • Prasad YR. Kumar PR, Ramesh B. Synthesis and antidepressant activity of some 3-(2’’-hydroxy naphtalen-1’’-yl)-5-phenyl-2-isoxazolines. Int J Chem Sci. 2007; 5(2): 542-548.
  • Soni N, Pande K, Kalsi R, Gupta TK, Parmar SS, Barthwal JP. Inhibition of rat brain monoamine oxidase and succinic dehydrogenase by anticonvulsant pyrazolines. Res Commun Chem Pathol Pharm. 1987; 56: 129-132.
  • Bilgin AA, Palaska E, Sunal R. Studies on the synthesis and antidepressant activity of some 1-thiocarbamoyl-3,5-diphenyl-2pyrazolines, Arzneim Forsch. (Drug Res) 1993; 43: 1041-1042.
  • Bilgin AA, Palaska E, Sunal R, Gumusel B. 1,3,5-Triphenyl-2-pyrazolines with antidepressant activities. Pharmazie 1994; 49: 67-69.
  • Kaplancıklı ZA, Özdemir A, Turan-Zitouni G, Altıntop MD, Can OD. New pyrazoline derivatives and their antidepressant activity. Eur J Med Chem. 2010; 45(9): 4383-4387.
  • Gökhan-Kelekçi N, Yabanoğlu S, Küpeli E, Salgın U, Özgen Ö, Uçar G, Yeşilada E, Kendi E, Yeşilada A, Bilgin AA. A new therapeutic approach in Alzheimer disease: Some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. Bioorg Med Chem. 2007; 15:5775-5786.
  • Beyhan N, Koçyigit-Kaymakçıoglu B, Gümrü S, Arıcıoğlu F. Synthesis and anticonvulsant activity of some 2-pyrazolines derived from chalcones. J Arabjc. 2013 (in press).
  • Cryan JF, Mombereau C, Vassout A. The tail suspension test as a model for assessing antidepressant activity: review of pharmacological and genetic studies in mice. Neurosci Biobehav Rev. 2005; 29(4-5): 5716
  • Porsolt RD, Le Pichon M, Jalfre M. Depression: a new animal model sensitive to antidepressant treatments. Nature 1977; 266(5604): 7307
  • Prasad YR, Rao LA, Prasoona L, Murali K, Kumar RP. Synthesis and antidepressant activity of some 1,3,5-triphenyl-2-pyrazolines and 3-(2''-hydroxy naphthalen-1''-yl)-1,5-diphenyl-2-pyrazolines. Bioorg Med Chem Lett. 2005;15(22): 5030-5034.
  • Cryan JF, Mombereau C, Vassout A. The tail suspension test as a model for assessing antidepressant activity: review of pharmacological and genetic studies in mice. Neurosci Biobehav Rev. 2005; 29(4-5):5716
  • Chatteriee M, Jaiswal M, Palit G. Comparative evaluation of forced swim test and tail suspension test as models of negative symptom of schizophrenia in rodents. ISRN Psychiatry. 2012; 59514, doi: 5402/2012/595141.

Antidepresan benzeri etkili 2-pirazolin türevleri

Year 2013, Volume: 3 Issue: 3, 154 - 158, 30.01.2014

Abstract

Amaç: Yaygın, kronik ve tekrarlama riski olan psikiyatrik bir hastalık olarak depresyon, farklı sistemleri etkileyebilen semptomlar bütünüyle karakterize edilir. Patogenezinde rol oynayan çok farklı sistemlerin olması ve tedaviye verilen yanıtta görülen farklar, ilaç tedavisiyle tam bir iyileşme sağlanmasını engelleyerek yeni tedavi seçeneklerinin keşfedilmesi için yapılan çalışmaları hızlandırmaktadır. Daha önce birçok araştırmada pirazolin türevlerinin antidepresan ajan olarak tedavi potansiyeline sahip oldukları gösterilmiştir. Bu çalışmada ise bir seri yeni 2-pirazolin türevlerinin antidepresan benzeri etki profillerinin aydınlatılması amaçlanmıştır.

Yöntem: Antidepresan benzeri aktivite Balb/C farelerde kuyruktan asma testi ve bu testte etkili olduğu tespit edilen maddeler için zorunlu yüzme testi kullanılarak değerlendirilmiştir. Her iki testte de antidepresan benzeri etkinin göstergesi, her bir hayvan için toplam hareketsiz kalma süresi olarak kabul edilmiştir.

Bulgular: 3d ve 3e kodlu test bileşiklerinin antidepresan benzeri etkili olduğu belirlenmiş ve uygulanan her iki testte de referans ilaç imipramin grubunda gözlendiği gibi hareketsiz kalma sürelerinde kısalma gözlenmiştir. Ayrıca bileşikler farelerde lokomotor aktiviteyi etkilememiştir. 

Sonuç: Sonuçlarımız, 2-pirazolin türevi olan 3d ve 3e’nin depresyon tedavisinde yeni aday bileşiklerin tasarımı için potansiyel test maddeleri olduğunu göstermektedir.


Anahtar Kelimeler : Antidepresan benzeri aktivite, 2-pirazolin türevleri, zorunlu yüzme testi, kuyruktan asma testi

References

  • Mental health and development: Targeting people with mental health conditions as a vulnerable group. World Health Organisation, Geneva, 2010.
  • Schechter LE, Ring RH, Beyer CE, Hughes ZA, Khawaja X, Malberg JE, Rosenzweig-Lipson S. Innovative approaches for the development of antidepressant drugs: Current and future strategies. NeuroTherapeutics 2005; 2:590-611.
  • Reynolds EH. Brain and mind: a challenge for WHO. Lancet 2003; 361: 1924‐1925.
  • Vinayak M, Ruckmani A, Chandrashekar K, VenuGopal R.K, Madhavi E, Swati B, Madhusudhan N, Antidepressant activity of ethanolic extract Piper betle leaves in mice. Curr Res Neurosci. 2012; 2 (1): 11-16.
  • Petit-Demouliere B, Chenu F, Bourin M. Forced swimming test in mice: a review of antidepressant activity. Psychopharmacology 2005; 177: 245-255.
  • Santosh P, Venugopl R, Nılakash A S, Kunjbıharı S, Dr. Mangala L. Antidepressant activity of methanolic extract of passiflora foetida leaves in mice. Int J of Pharm Pharmaceut Sci. 2011; 3: 112-115.
  • Rodrigues ALS, Rosa JM, Gadotti VM, Goulart EC, Stos MM, Silva AV, Sehnem B, Rosa LS , Goncalves RM, Correa R, Santos AR. Anti-depressant-like and antinociceptive-like actions of 4-(4’-chlorophenyl)-6-(4’’-methylphenyl)-2-hydrazinepyrimidine Mannich base in mice. Pharmaco Biochem Behav. 2005; 82: 156-162.
  • Özdemir A, Turan-Zitouni G, Kaplancıklı ZA, Revial G, Güven K. Synthesis and antimicrobial activity of 1-(4-aryl-2-thiazolyl)-3-(2thienyl)-5-aryl-2-pyrazoline derivatives. Eur J Med Chem. 2007; 42(3): 403-40
  • Shoman ME, Abdel-Aziz M, Aly OM, Farag HH, Morsy MA. Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives. Eur J Med Chem. 2009; 44(7): 3068-3076.
  • Özdemir Z, Kandilci HB, Gümüşel B, Çalış Ü, Bilgin AA. Synthesis and studies on antidepressant and anticonvulsant activities of some 3-(2-furyl)-pyrazoline derivatives. Eur J Med Chem. 2007; 42(3):3733
  • Satyanarayana M, Tiwari P, Tripathi BK, Srivastava AK, Pratap R. Synthesis and antihyperglycemic activity of chalcone based aryloxypropanolamines. Bioorg Med Chem. 2004; 12(5):883-889.
  • Prasad YR. Kumar PR, Ramesh B. Synthesis and antidepressant activity of some 3-(2’’-hydroxy naphtalen-1’’-yl)-5-phenyl-2-isoxazolines. Int J Chem Sci. 2007; 5(2): 542-548.
  • Soni N, Pande K, Kalsi R, Gupta TK, Parmar SS, Barthwal JP. Inhibition of rat brain monoamine oxidase and succinic dehydrogenase by anticonvulsant pyrazolines. Res Commun Chem Pathol Pharm. 1987; 56: 129-132.
  • Bilgin AA, Palaska E, Sunal R. Studies on the synthesis and antidepressant activity of some 1-thiocarbamoyl-3,5-diphenyl-2pyrazolines, Arzneim Forsch. (Drug Res) 1993; 43: 1041-1042.
  • Bilgin AA, Palaska E, Sunal R, Gumusel B. 1,3,5-Triphenyl-2-pyrazolines with antidepressant activities. Pharmazie 1994; 49: 67-69.
  • Kaplancıklı ZA, Özdemir A, Turan-Zitouni G, Altıntop MD, Can OD. New pyrazoline derivatives and their antidepressant activity. Eur J Med Chem. 2010; 45(9): 4383-4387.
  • Gökhan-Kelekçi N, Yabanoğlu S, Küpeli E, Salgın U, Özgen Ö, Uçar G, Yeşilada E, Kendi E, Yeşilada A, Bilgin AA. A new therapeutic approach in Alzheimer disease: Some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics. Bioorg Med Chem. 2007; 15:5775-5786.
  • Beyhan N, Koçyigit-Kaymakçıoglu B, Gümrü S, Arıcıoğlu F. Synthesis and anticonvulsant activity of some 2-pyrazolines derived from chalcones. J Arabjc. 2013 (in press).
  • Cryan JF, Mombereau C, Vassout A. The tail suspension test as a model for assessing antidepressant activity: review of pharmacological and genetic studies in mice. Neurosci Biobehav Rev. 2005; 29(4-5): 5716
  • Porsolt RD, Le Pichon M, Jalfre M. Depression: a new animal model sensitive to antidepressant treatments. Nature 1977; 266(5604): 7307
  • Prasad YR, Rao LA, Prasoona L, Murali K, Kumar RP. Synthesis and antidepressant activity of some 1,3,5-triphenyl-2-pyrazolines and 3-(2''-hydroxy naphthalen-1''-yl)-1,5-diphenyl-2-pyrazolines. Bioorg Med Chem Lett. 2005;15(22): 5030-5034.
  • Cryan JF, Mombereau C, Vassout A. The tail suspension test as a model for assessing antidepressant activity: review of pharmacological and genetic studies in mice. Neurosci Biobehav Rev. 2005; 29(4-5):5716
  • Chatteriee M, Jaiswal M, Palit G. Comparative evaluation of forced swim test and tail suspension test as models of negative symptom of schizophrenia in rodents. ISRN Psychiatry. 2012; 59514, doi: 5402/2012/595141.
There are 23 citations in total.

Details

Primary Language Turkish
Journal Section Articles
Authors

Bedia Koçyiğit Kaymakçıoğlu

Salih Gümrü This is me

Nagihan Beyhan This is me

Feyza Aricioglu This is me

Publication Date January 30, 2014
Submission Date January 30, 2014
Published in Issue Year 2013 Volume: 3 Issue: 3

Cite

APA Koçyiğit Kaymakçıoğlu, B., Gümrü, S., Beyhan, N., Aricioglu, F. (2014). Antidepresan benzeri etkili 2-pirazolin türevleri. Clinical and Experimental Health Sciences, 3(3), 154-158. https://doi.org/10.5455/musbed.20130916091055
AMA Koçyiğit Kaymakçıoğlu B, Gümrü S, Beyhan N, Aricioglu F. Antidepresan benzeri etkili 2-pirazolin türevleri. Clinical and Experimental Health Sciences. February 2014;3(3):154-158. doi:10.5455/musbed.20130916091055
Chicago Koçyiğit Kaymakçıoğlu, Bedia, Salih Gümrü, Nagihan Beyhan, and Feyza Aricioglu. “Antidepresan Benzeri Etkili 2-Pirazolin türevleri”. Clinical and Experimental Health Sciences 3, no. 3 (February 2014): 154-58. https://doi.org/10.5455/musbed.20130916091055.
EndNote Koçyiğit Kaymakçıoğlu B, Gümrü S, Beyhan N, Aricioglu F (February 1, 2014) Antidepresan benzeri etkili 2-pirazolin türevleri. Clinical and Experimental Health Sciences 3 3 154–158.
IEEE B. Koçyiğit Kaymakçıoğlu, S. Gümrü, N. Beyhan, and F. Aricioglu, “Antidepresan benzeri etkili 2-pirazolin türevleri”, Clinical and Experimental Health Sciences, vol. 3, no. 3, pp. 154–158, 2014, doi: 10.5455/musbed.20130916091055.
ISNAD Koçyiğit Kaymakçıoğlu, Bedia et al. “Antidepresan Benzeri Etkili 2-Pirazolin türevleri”. Clinical and Experimental Health Sciences 3/3 (February 2014), 154-158. https://doi.org/10.5455/musbed.20130916091055.
JAMA Koçyiğit Kaymakçıoğlu B, Gümrü S, Beyhan N, Aricioglu F. Antidepresan benzeri etkili 2-pirazolin türevleri. Clinical and Experimental Health Sciences. 2014;3:154–158.
MLA Koçyiğit Kaymakçıoğlu, Bedia et al. “Antidepresan Benzeri Etkili 2-Pirazolin türevleri”. Clinical and Experimental Health Sciences, vol. 3, no. 3, 2014, pp. 154-8, doi:10.5455/musbed.20130916091055.
Vancouver Koçyiğit Kaymakçıoğlu B, Gümrü S, Beyhan N, Aricioglu F. Antidepresan benzeri etkili 2-pirazolin türevleri. Clinical and Experimental Health Sciences. 2014;3(3):154-8.

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