A comparison of the relaxant effects of pinacidil in rabbit renal and mesenteric artery

Gojkovic, L; Kazić, T

doi:10.1016/0306-3623(94)90376-x

Cited by 8 publications

(4 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Glibenclamide is known to be one of the most selective blockers of K ATP channels [14]. In the present study, glibenclamide reversed the inhibition induced by pinacidil on spontaneous rhythmic contractions and elicited contractions, in a concentration‐dependent manner with potency comparable to those described in a various smooth muscles [10,11,15], including animal [12,13] and human uterus [1,5,6]. The obtained pA 2 value of 5.59 is consistent to those reported for K ATP channels on the human internal mammary artery (5.46) [16].…”

Section: Discussionsupporting

confidence: 90%

“…Our data agree with the observations of Morrison et al [5] and Khan et al [6] that revealed a competitive antagonism on the oxytocin-stimulated contractions in the human uterus. The pA 2 value for glibenclamide was similar to those found for K ATP channels in the smooth muscle of human and rat uterus [5,12], and comparable to those obtained in other smooth muscle experimental models [4,10,11].…”

Section: Myometrial Contractionssupporting

confidence: 87%

“…The pharmacology of pinacidil has been studied on a wide variety of smooth muscle preparations, including cardiac vascular, tracheal, bladder and neuronal preparations [4,9–11]. However, only few studies have shown that pinacidil induces relaxation of rat [12], goat [13] and human uterus [1,5,6].…”

Section: Discussionmentioning

confidence: 99%

See 2 more Smart Citations

The Effect of Potassium Channel Opener Pinacidil on the Non‐Pregnant Rat Uterus

Novaković

Milovanović²,

Protić

et al. 2007

Basic Clin Pharma Tox

View full text Add to dashboard Cite

The effects of the K + channel opener, pinacidil on the spontaneous rhythmic contractions and contractions provoked by electrical field stimulation (50 Hz) or by oxytocin were investigated in the isolated uterus of the non-pregnant rat in oestrus. Pinacidil produced more potent inhibition of oxytocin-elicited contractions than of spontaneous rhythmic contractions or electrical field stimulation-induced contractions. Glibenclamide, a selective blocker of adenosine triphosphate (ATP)-sensitive K + (K ATP ) channels, antagonized the pinacidil-induced inhibition of contractions elicited by oxytocin in a competitive manner. However, the pinacidil-induced inhibition of electrical field stimulation-elicited contractions and spontaneous rhythmic contractions was antagonized non-competitively by glibenclamide. In the uterine strips precontracted with 80 mM K + , the pinacidil-induced maximal relaxation was not affected. The present data show that pinacidil exhibits potent relaxant properties in the rat non-pregnant uterus in oestrus and therefore should be taken into account as a possible agent for treatment of dysmenorrhoea. Based on glibenclamide affinity, it appears that the inhibitory response to pinacidil involves K ATP channels. We need further investigations to explain why the interaction between glibenclamide and pinacidil in this experimental model depends on the nature of contractions. The ability of pinacidil to completely relax the rat non-pregnant uterus pre-contracted with K + -rich solution suggests that K + channel-independent mechanism(s) also play a part in its relaxant effect.

show abstract

Section: Discussionsupporting

confidence: 90%

Section: Myometrial Contractionssupporting

confidence: 87%

See 1 more Smart Citation

The Effect of Potassium Channel Opener Pinacidil on the Non‐Pregnant Rat Uterus

Novaković

Milovanović²,

Protić

et al. 2007

Basic Clin Pharma Tox

View full text Add to dashboard Cite

show abstract

“…There are very few reports showing that pinacidil induces vasorelaxation by opening vascular smooth muscle big calcium-sensitive K + (BK Ca ) channels, including the study performed on the human coronary arteries and rabbit renal artery (17,18). However, in the present study, we did not confirm this result.…”

Section: Discussioncontrasting

confidence: 94%

Potassium Channel Opener Pinacidil Induces Relaxation of the Isolated Human Radial Artery

Stojnic¹,

Gojkovic-Bukarica²,

Perić³

et al. 2007

J Pharmacol Sci

View full text Add to dashboard Cite

Abstract. Taking into consideration that the search for drugs capable of modifying blood flow through human radial artery (RA) is warranted, the present study was designed to examine the vasodilatatory effects of the potassium channel opener, pinacidil on the RA and to define the contribution of different K + -channel subtypes in the endothelium-independent pinacidil action on this blood vessel. Pinacidil relaxed the RA rings with endothelium and without endothelium with comparable potency. N-nitro-L-arginine methyl ester (L-NAME) and methylene blue did not affect the pinacidil-induced vasorelaxation in rings with endothelium. In the rings without endothelium, the K + -channel blockers glibenclamide and tetraethylammonium (TEA) moderately antagonized the pinacidil-induced relaxation, while charybdotoxin and 4-aminopiridine did not. In endothelium-denuded rings, precontracted with 100 mM K + , the relaxant responses to pinacidil were highly significantly shifted to the right compared to those obtained in RA precontracted with phenylephrine, but pinacidil-induced maximal relaxation was not affected. Addition of nifedipine did not but addition of nifedipine and nickel (Na + -Ca 2+ exchanger inhibitor) did cause a statistically significant rightward shift of the pinacidil concentration-relaxation curve, although the effect 0.1 mM pinacidil was preserved. Thus, pinacidil induces relaxation of the human RA in endothelium-independent manner, and glibenclamide-and TEA-sensitive vascular smooth muscle K + channels are probably involved. Its ability to completely relax the RA precontracted with K + -rich solution suggests that pinacidil has additional K + channel-independent mechanism(s) of action. It seems that stimulation of the forward mode of the Na + -Ca 2+ exchanger plays a part in this K + channel-independent effect of pinacidil.

show abstract

Potassium Channels in the Renal Circulation

Stockand

Sansom

2001

Potassium Channels in Cardiovascular Biology

View full text Add to dashboard Cite

A comparison of the relaxant effects of pinacidil in rabbit renal and mesenteric artery

Cited by 8 publications

References 33 publications

The Effect of Potassium Channel Opener Pinacidil on the Non‐Pregnant Rat Uterus

The Effect of Potassium Channel Opener Pinacidil on the Non‐Pregnant Rat Uterus

Potassium Channel Opener Pinacidil Induces Relaxation of the Isolated Human Radial Artery

Potassium Channels in the Renal Circulation

Contact Info

Product

Resources

About