Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri

Bürge Doğruer Akan; Ümide Demir Özkay

doi:10.17826/cumj.490690

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Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri

Öz

Amaç: Bu çalışmanın amacı, bazı piperazin alkanol türevi bileşiklerin olası antinosiseptif etkinliklerinin bazı nosiseptif testler ile araştırılmasıdır.

Gereç ve Yöntem: Piperazin alkanol türevlerinin (20 mg/kg) mekanik, termal ve kimyasal ağrılı uyarana karşı potansiyel antinosiseptif etkileri kuyruk sıkıştırma, sıcak plaka, asetik asid kıvranma ve formalin testleri ile araştırılmıştır. Test edilen bileşiklerin farelerin motor koordinasyonları üzerine olası etkinliğini değerlendirmek üzere Rota-Rod testi yapılmıştır.

Bulgular: Referans ilaç olarak kullanılan morfin kuyruk sıkıştırma, sıcak plaka, asetik asid kıvranma ve formalin testlerinde beklenen analjezik etkiyi göstermiştir. 2-(4-sübstitüepiperazin-1-il)-1-fenilpropan-1-ol türevlerinden; 2-hidroksietil (C3), fenil (C6), 4-metilfenil (C7), 4-klorofenil (C8), 4-florofenil (C9), 4-nitrofenil (C10) ve benzhidril (C11) sübstitüentlerini taşıyan bileşikler, kuyruk sıkıştırma ve sıcak plaka testlerinde mekanik ve termal ağrılı uyarana karşı farelerin reaksiyon sürelerini artırmıştır. Aynı test bileşikleri asetik asid kıvranma ve formalin testlerinde, kimyasal uyarı aracılıklı nosiseptif cevapları azaltmıştır. C7, C8 ve C11 kodlu test bileşiklerinin antinosiseptif etkileri C3, C6, C9 ve C10 kodlu test bileşiklerinden istatistiksel olarak daha anlamlı bulunmuştur. Non-selektif opioid reseptör antagonisti nalokson (5 mg/kg) tüm nosiseptif testlerde gözlenen antinosiseptif etkiyi tamamen antagonize etmiştir.

Sonuç: Bu bulgular, C3, C6-C11 kodlu test bileşiklerinin antinosiseptif etkilerini ortaya koymuş ve bu etkinin hem santral hem de periferik mekanizmalar ile ilişkili olduğuna işaret etmiştir. Ayrıca, nalokson antagonizması söz konusu aktiviteye opioid mekanizmaların katılımını göstermektedir.

Anahtar Kelimeler

Piperazin alkanol,kuyruk sıkıştırma testi,sıcak plaka testi,asetik asid kıvranma testi,formalin testi,opioid,Rota-Rod testi

The antinociceptive effects of some piperazine alkanol derivatives

Öz

Purpose: The aim of this study was to investigate probable antinociceptive activities of some piperazine alkanol derivatives in some nociceptive tests.

Materials and Methods: Potential antinociceptive activities of the piperazine alkanol derivatives (20 mg/kg) against mechanic, thermal and chemical nociceptive stimuli were evaluated by tail-clip, hot-plate, acetic acid-induced writhing, and formalin tests. Rota-Rod test was performed to evaluate probable effect of the test compounds on motor coordination of mice.

Results: Morphine used as a reference drug exhibited analgesic effect in tail-clip, hot-plate, acetic acid-induced writhing, and formalin tests, as expected. 2-(4-substituted-piperazin-1-yl)-1-phenylpropan-1-ol compounds, which carry 2-hydroxyethyl (C3), phenyl (C6), 4-methylphenyl (C7), 4-chlorophenyl (C8), 4-fluorophenyl (C9), 4-nitrophenyl (C10) and benzhydryl (C11) substituents, increased the reaction time of mice against mechanic and thermal nociceptive stimuli in tail-clip and hot-plate tests, respectively. The same test compounds decreased chemical stimulus-induced nociceptive response in acetic acid-induced writhing and formalin tests. Antinociceptive effects of the compounds C7, C8, and C11 were found to be statistically more significant than the compounds C3, C6, C9, and C10. Naloxone, non-selective opioid receptor antagonist (5 mg/kg), totally antagonized the antinociceptive effect observed in all of the nociceptive tests.

Conclusion: These findings revealed antinociceptive activity of the compounds C3, C6-C11, and pointed out that this effect was associated with both central and peripheral mechanisms. In addition, naloxone antagonism indicated the involvement of opioid mechanisms in the activity.

Anahtar Kelimeler

Piperazine alkanol,tail-clip test,hot-plate test,acetic acid-induced writhing test,formalin test,opioid,Rota-Rod test

Kaynakça

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Ayrıntılar

Birincil Dil

Türkçe

Konular

Sağlık Kurumları Yönetimi

Bölüm

Araştırma Makalesi

Yazarlar

Bürge Doğruer Akan Bu kişi benim
0000-0002-5896-609X
Türkiye

Ümide Demir Özkay ^*
0000-0002-6773-4266
Türkiye

Yayımlanma Tarihi

30 Eylül 2019

Gönderilme Tarihi

30 Kasım 2018

Kabul Tarihi

27 Aralık 2018

Yayımlandığı Sayı

Yıl 2019 Cilt: 44 Sayı: 3

DOI

https://doi.org/10.17826/cumj.490690

IZ

https://izlik.org/JA85GE98AZ

APA

Doğruer Akan, B., & Demir Özkay, Ü. (2019). Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri. Cukurova Medical Journal, 44(3), 729-744. https://doi.org/10.17826/cumj.490690

AMA

1.Doğruer Akan B, Demir Özkay Ü. Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri. Cukurova Med J. 2019;44(3):729-744. doi:10.17826/cumj.490690

Chicago

Doğruer Akan, Bürge, ve Ümide Demir Özkay. 2019. “Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri”. Cukurova Medical Journal 44 (3): 729-44. https://doi.org/10.17826/cumj.490690.

EndNote

Doğruer Akan B, Demir Özkay Ü (01 Eylül 2019) Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri. Cukurova Medical Journal 44 3 729–744.

IEEE

[1]B. Doğruer Akan ve Ü. Demir Özkay, “Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri”, Cukurova Med J, c. 44, sy 3, ss. 729–744, Eyl. 2019, doi: 10.17826/cumj.490690.

ISNAD

Doğruer Akan, Bürge - Demir Özkay, Ümide. “Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri”. Cukurova Medical Journal 44/3 (01 Eylül 2019): 729-744. https://doi.org/10.17826/cumj.490690.

JAMA

1.Doğruer Akan B, Demir Özkay Ü. Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri. Cukurova Med J. 2019;44:729–744.

MLA

Doğruer Akan, Bürge, ve Ümide Demir Özkay. “Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri”. Cukurova Medical Journal, c. 44, sy 3, Eylül 2019, ss. 729-44, doi:10.17826/cumj.490690.

Vancouver

1.Bürge Doğruer Akan, Ümide Demir Özkay. Bazı piperazin alkanol türevlerinin antinosiseptif etkinlikleri. Cukurova Med J. 01 Eylül 2019;44(3):729-44. doi:10.17826/cumj.490690