Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta

Criddle, David N.; Moura, Roberto Soares de

doi:10.1590/s0100-879x2000000800013

Cited by 3 publications

(3 citation statements)

References 11 publications

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“…Each of the three substances used in the present study represents one prototype of a different subclass of ATP-sensitive PCOs; cromakalim belongs to the benzopyran series, pinacidil is a cyanoguanidine derivative. The atypical PCO minoxidil is clinically known to treat high blood pressure [8] and topically used as a hair-growth stimulant, and is a pyrimidine derivative.…”

Section: Introductionmentioning

confidence: 99%

Inhibitory effects of the ATP-sensitive potassium channel openers cromakalim, pinacidil and minoxidil on the carbachol–response curve in porcine detrusor muscle

Badawi

Kirschner‐Hermanns

Ding

2012

Arab Journal of Urology

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AimsATP-sensitive potassium channels represent promising drug targets for treating specific bladder diseases. The inhibitory effects of ATP-selective potassium channel openers (PCOs) on the carbachol–response curve in porcine detrusor muscle were examined.Materials and methodsEach of the three substances used in the study represent one prototype of a different class of PCO: cromakalim belongs to the benzopyran series, pinacidil is a cyanoguanidine derivative, and minoxidil represents a pyrimidine derivative. The porcine detrusor muscle represents one of the best models for human detrusor. Experiments were conducted on muscle strips of porcine detrusor muscle suspended in a tissue bath. Concentration–response curves of carbachol were constructed after pretreatment with cromakalim at 10−7, 10−6 and 10−5 M, and with pinacidil and minoxidil at 10−6, 10−5.5 and 10−5 M, respectively. Each muscle strip was only used to examine one concentration of one substance.ResultsCromakalim had the greatest inhibitory effect, significantly suppressing the carbachol–response curve at 10−6 and 10−5 M. Pinacidil showed a significant inhibitory effect at 10−5.5 and 10−5 M, which was smaller than that of cromakalim. Minoxidil did not significantly inhibit the contractions at all examined concentrations.ConclusionsThe examined ATP-sensitive PCOs belonging to the benzopyrans and cyanoguanidines significantly suppressed detrusor contractions. The development of derivatives of these prototypes could open new possibilities for the pharmacological treatment of selected bladder diseases.

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Section: Introductionmentioning

confidence: 99%

Inhibitory effects of the ATP-sensitive potassium channel openers cromakalim, pinacidil and minoxidil on the carbachol–response curve in porcine detrusor muscle

Badawi

Kirschner‐Hermanns

Ding

2012

Arab Journal of Urology

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“…It also reduces the opening probability of ion channels which are necessary for membrane depolarization [14]. Additionally, the concentration-relaxation curves of the atypical PCO minoxidil clinically used as antihypertensive medication [16] was determined in both species. Among the different classes of potassium channels ATP-sensitive channels are interesting with regard to their use as targets for the treatment of detrusor overactivity.…”

Section: Introductionmentioning

confidence: 99%

“…In the present study the concentration-relaxation curves of the two first-generation PCOs, cromakalim and pinacidil, in porcine and human detrusor muscle were determined. Additionally, the concentration-relaxation curves of the atypical PCO minoxidil clinically used as antihypertensive medication [16] was determined in both species.…”

Section: Introductionmentioning

confidence: 99%

Inhibitory effects of different ATP‐sensitive potassium channel openers on electrically generated and carbachol‐induced contractions of porcine and human detrusor muscle

Badawi

Ding

Bross

2008

Fundamemntal Clinical Pharma

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The inhibitory effects of different potassium channel openers (PCOs) on electrically generated and carbachol-induced contractions of porcine and human detrusor muscle were examined. PCOs could be an interesting substance class for treatment of detrusor overactivity. Experiments were performed on muscle strips suspended in a tissue bath. Human tissue originated from patients who underwent total cystectomy. The concentration-relaxation curves of the first-generation PCOs cromakalim and pinacidil and the untypical PCO minoxidil were performed using carbachol-precontracted detrusor muscle strips of pigs and humans. Additionally, the inhibitory effects of cromakalim, pinacidil and minoxidil on electrically generated contractions of porcine detrusor muscle were examined. Furthermore, the inhibitory effect of the second-generation, bladder-selective PCO ZM 226600 on electrically generated contractions of the human detrusor muscle was determined. Frequency-response curves were performed before and after incubation with one PCO used in two different concentrations. In humans, cromakalim and pinacidil led to a maximum decrease of 73.5 and 68.4% and showed mean pD2 values of 6.65 and 5.5, respectively. In pigs, cromakalim and pinacidil led to a maximum decrease of 90.6 and 93.6% and showed mean pD2 values of 6.39 and 5.01, respectively. Minoxidil did not significantly decrease the precontraction at the highest used concentration in both species. Cromakalim exhibited the biggest inhibitory effect being significant at 10(-5) and 10(-6) M. Pinacidil showed only a significant inhibitory effect at 10(-5) M which was smaller than that of cromakalim. At 3 x 10(-6) M only a very small effect occurred at 1 Hz. Minoxidil did not inhibit the contractions at both examined concentrations except for a very small effect at 1 Hz. In humans, ZM 226600 exhibited at 10(-6) and 10(-5) M a significant inhibitory effect. At 10(-7) M it was only significant at one frequency.

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The vascular effect of glibenclamide: A systematic review

Al‐Karagholi

Sode

Gozalov

et al. 2019

Cephalalgia Reports

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Objective: To systematically review the vascular effects of glibenclamide. Background: Infusion of adenosine triphosphate (ATP)-sensitive potassium (KATP) channel opener (KCO) levcromakalim dilates cranial arteries and induces headache and migraine attacks. Recent data show that levcromakalim-induced vasodilation is associated with headache. Glibenclamide is a KATP channel blocker that may alter the vascular tone and thus has an impact on headache or migraine prevention. Methods: A search through PubMed was undertaken for studies investigating the vascular effects of glibenclamide in vitro as well as in vivo published until July 2019. Results: We identified 58 articles; 31 in vitro studies, 24 in vivo studies and 3 studies with both. The main findings were that glibenclamide inhibited levcromakalim-induced and other KCOs-induced vasodilation, while the basal vascular tone remained unchanged. Conclusion: Glibenclamide could inhibit vasodilation by KCOs, and further studies are needed to clarify the vascular effect of glibenclamide on human cranial arteries.

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Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta

Cited by 3 publications

References 11 publications

Inhibitory effects of the ATP-sensitive potassium channel openers cromakalim, pinacidil and minoxidil on the carbachol–response curve in porcine detrusor muscle

Inhibitory effects of the ATP-sensitive potassium channel openers cromakalim, pinacidil and minoxidil on the carbachol–response curve in porcine detrusor muscle

Inhibitory effects of different ATP‐sensitive potassium channel openers on electrically generated and carbachol‐induced contractions of porcine and human detrusor muscle

The vascular effect of glibenclamide: A systematic review

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