Pharmacological characterization of metamizol-induced relaxation in phenylephrine-precontracted rabbit thoracic aorta smooth muscle

Ergün, Hakan; Ayhan, I.H.; Tulunay, F. Cankat

doi:10.1016/s0306-3623(99)00013-0

Cited by 23 publications

(20 citation statements)

References 2 publications

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“…Ergün et al [25] observed that dipyrone concentration dependently inhibited Phe-induced contractions on rabbit thoracic aorta. This result is in agreement with the results of our study.…”

Section: Discussionmentioning

confidence: 98%

The Role of Cyclooxygenase Enzymes in the Effects of Losartan and Lisinopril on the Contractions of Rat Thoracic Aorta

Özatik¹,

Kaygisiz²,

Erol³

2017

Eurasian J Med

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Objective: It was suggested that prostaglandins which are synthesized by cyclooxygenase (COX) enzymes contribute to the actions of angiotensin-converting enzyme (ACE) inhibition and angiotensin AT1 receptor antagonism and there is an interaction between ACE signaling pathway and COX enzymes. We aim to investigate the role of COX enzymes in the effects of losartan, an angiotensin II (Ang II) receptor antagonist or lisinopril, an ACE inhibitor, on the contractions of rat thoracic aorta in isolated tissue bath. , 2 × 10 -3 M, respectively) augmented the relaxant effects of losartan or lisinopril. Also, dipyrone potentiated the effect of lisinopril on KCl-induced contractions. Conclusion:We suggest that dipyrone increases the smooth-muscle relaxing effects of losartan or lisinopril and that COX enzyme inhibition may have a role in the enhancement of this relaxation.Keywords: Cyclooxygenase, dipyrone, lisinopril, losartan, thoracic aorta ÖZ Amaç: Siklooksijenaz (COX) enzimleri tarafından sentezlenen prostaglandinlerin anjiotensin dönüştürücü enzim (ADE) inhibisyonu ve anjiotensin AT1 reseptör antagonizmasının etkilerine katkıda bulunduğu ve ADE sinyal yolakları ile COX enzimleri arasında etkileşme olduğu ileri sürülmüştür. Bu çalışmada anjiotensin II (Ang II) reseptör antagonisti bir ilaç olan losartan veya ADE inhibitörü bir ilaç olan lizinoprilin izole organ banyosunda sıçan torasik aorta kasılmaları üzerindeki etkilerinde COX enzimlerinin rolünün araştırılmasını amaçladık. Sonuç: Dipironun losartan veya lizinoprilin düz kas gevşetici etkilerini artırdığını ve COX enzim inhibisyonunun bu gevşemede rolü olabileceğini ileri sürüyoruz.

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“…Ergün et al [25] observed that dipyrone concentration dependently inhibited Phe-induced contractions on rabbit thoracic aorta. This result is in agreement with the results of our study.…”

Section: Discussionmentioning

confidence: 98%

The Role of Cyclooxygenase Enzymes in the Effects of Losartan and Lisinopril on the Contractions of Rat Thoracic Aorta

Özatik¹,

Kaygisiz²,

Erol³

2017

Eurasian J Med

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“…Therefore, COX inhibition might not be an explanation for spasmolytic effect of dipyrone. The probable mechanism of spasmolytic effect was recently investigated in detail, but in the vascular system [16,21] . Ergun et al [16] reported that dipyrone produces a time-and dose-dependent relaxation in rabbit thoracic aorta smooth muscle.…”

Section: Discussionmentioning

confidence: 99%

“…Following the equilibration period, the rings were contracted by using 100 mmol/l potassium chloride (KCl), which were then quickly washed with Krebs solution 3 times and then allowed to equilibrate for another hour under the conditions mentioned above. As it is previously reported that under physiological conditions dipyrone hydrolyses to active metabolites, it was separately pre-incubated for 2 h in Krebs-Henseleit solution under the organ bath conditions before evaluating dipyrone's effect in experiments [16][17][18] . Tracheal rings were then contracted either with histamine or adenosine triphosphate (ATP) at previously determined submaximal contracting concentrations.…”

Section: Tracheal Relaxation Experimentsmentioning

confidence: 99%

“…There is only one study in which 4-MAA and 4-AA were found to be responsible for the analgesic effect; having a correlation between human saliva 4-MAA and 4-AA concentrations and the analgesic effect [15] . Previous studies indicate that the active metabolites of dipyrone, not itself, probably mediate the smooth muscle relaxation response of dipyrone [16][17][18] .…”

Section: Introductionmentioning

confidence: 97%

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Airway Smooth Muscle Relaxations Induced by Dipyrone

Gülmez

Gürdal

Tulunay³

2006

Pharmacology

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Background: Dipyrone differs from other nonsteroidal anti-inflammatory drugs with a distinctive spasmolytic effect; however, the mechanism of action is not clear yet. The possible mechanism behind this effect was investigated on airway smooth muscle tone in vitro. Method:The effect of dipyrone on inositol phosphate (IP) accumulation was evaluated on guinea pig trachea smooth muscle. Changes in intracellular free calcium levels and IP accumulation were evaluated in LTK8 cells.Results: Dipyrone (0.01, 0.1, 1 mmol/l) had a relaxing effect on histamine (0.02 mmol/l)- and adenosine triphosphate- (ATP) (0.01 mol/l)-induced contractions, but not potassium chloride (KCl)-stimulated contractions. This relaxing effect was not observed with in- domethacin. Indomethacin did not inhibit the relaxation response of dipyrone. In isolated tracheal smooth muscle, histamine- (0.02 mmol/l) and ATP (0.01 mmol/l)-induced IP accumulation was significantly inhibited by dipyrone (1 mmol/l). ATP (0.01 mmol/l)-induced IP accumulation was also significantly inhibited by dipyrone (0.01 mmol/l) in LTK8 cells. Dipyrone inhibited ATP-induced (0.01 and 0.1 mmol/l) intracellular calcium increase in LTK8 cells.Conclusion: Inhibition of the release of intracellular Ca²⁺ may play a role in the smooth muscle relaxing effect of dipyrone. The inhibitor effect of dipyrone on IP accumulation may be due to direct inhibition of phospholipase C (PLC) or impairment of the activation of PLC by G protein-coupled receptor (GPCR).

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“…Dipyron, kendisi veya metaboliti aracılığı ile düz kaslarda gevşeme yapar (1). Dipyron oddi sfinkterindeki tonusu azaltarak safra yollarındaki basıncı düşürür (2,3). Arter peristaltizminin arttığı durumlarda ise kasılma frekansını yavaşlatır (4) …”

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Spinal Kord Travmalarinda Topi̇kal Di̇pyron'un Etki̇nli̇ği̇

Celal;KARATAŞ¹

2000

Ankara Üniversitesi Tıp Fakültesi Mecmuası

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Pharmacological characterization of metamizol-induced relaxation in phenylephrine-precontracted rabbit thoracic aorta smooth muscle

Cited by 23 publications

References 2 publications

The Role of Cyclooxygenase Enzymes in the Effects of Losartan and Lisinopril on the Contractions of Rat Thoracic Aorta

The Role of Cyclooxygenase Enzymes in the Effects of Losartan and Lisinopril on the Contractions of Rat Thoracic Aorta

Airway Smooth Muscle Relaxations Induced by Dipyrone

Spinal Kord Travmalarinda Topi̇kal Di̇pyron'un Etki̇nli̇ği̇

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