Literature DB >> 8298791

Cardiovascular effects of SCA40, a novel potassium channel opener, in rats.

A Michel1, F Laurent, J Bompart, K Hadj-Kaddour, J P Chapat, M Boucard, P A Bonnet.   

Abstract

1. Experiments have been performed to investigate the cardiovascular actions in the rat of SCA40, a novel potassium channel opener which is a potent relaxant of guinea-pig airway smooth muscle in vivo and in vitro. 2. SCA40 (0.01-30 microM) caused a complete and concentration-dependent relaxation of rat isolated thoracic aorta contracted with 20 mM KCl but failed to inhibit completely the spasmogenic effects of 80 mM KCl. 3. The ATP-sensitive K(+)-channel blocker, glibenclamide (3 microM), failed to antagonize the relaxant action of SCA40 on 20 mM KCl-contracted rat isolated thoracic aorta. 4. SCA40 (0.001-100 microM) had dual effects on rat isolated atria. At low concentrations, SCA40 produced a concentration-dependent decrease in the rate and force of contractions. At higher concentrations (greater than 1 microM) SCA40 induced concentration-dependent increases of atrial rate and force. 5. In vivo, in normotensive Wistar rats, SCA40 elicited a dose-dependent (1-100 micrograms kg-1) decrease in mean arterial pressure which was accompanied by a moderate dose-dependent increase in heart rate. SCA40 (100 micrograms kg-1) had a slightly greater hypotensive effect than cromakalim (100 micrograms kg-1) but the duration of the hypotension was longer with cromakalim than with SCA40. 6. The hypotensive effect of SCA40 was not reduced by propranolol, atropine, NG-nitro-L-arginine methyl ester (L-NAME) or glibenclamide. 7. It is concluded that the mechanism by with SCA40 relaxes vascular smooth muscle in vitro and in vivo involves activation of K(+)-channels distinct from glibenclamide-sensitive ATP-sensitive K(+)-channels.

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Year:  1993        PMID: 8298791      PMCID: PMC2175828          DOI: 10.1111/j.1476-5381.1993.tb13917.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  21 in total

1.  Calcium-activated potassium channels in single smooth muscle cells of rabbit jejunum and guinea-pig mesenteric artery.

Authors:  C D Benham; T B Bolton; R J Lang; T Takewaki
Journal:  J Physiol       Date:  1986-02       Impact factor: 5.182

2.  Evaluation of the relaxant effects of SCA40, a novel charybdotoxin-sensitive potassium channel opener, in guinea-pig isolated trachealis.

Authors:  F Laurent; A Michel; P A Bonnet; J P Chapat; M Boucard
Journal:  Br J Pharmacol       Date:  1993-03       Impact factor: 8.739

3.  Cardiovascular effects of apamin and BRL 34915 in rats and rabbits.

Authors:  N S Cook; R P Hof
Journal:  Br J Pharmacol       Date:  1988-01       Impact factor: 8.739

Review 4.  Toxins in the characterization of potassium channels.

Authors:  N A Castle; D G Haylett; D H Jenkinson
Journal:  Trends Neurosci       Date:  1989-02       Impact factor: 13.837

Review 5.  Moving together: K+ channel openers and ATP-sensitive K+ channels.

Authors:  U Quast; N S Cook
Journal:  Trends Pharmacol Sci       Date:  1989-11       Impact factor: 14.819

6.  The negative inotropic effect of nicorandil is independent of cyclic GMP changes: a comparison with pinacidil and cromakalim in canine atrial muscle.

Authors:  T Yanagisawa; H Hashimoto; N Taira
Journal:  Br J Pharmacol       Date:  1988-10       Impact factor: 8.739

7.  Comparison of the effects of BRL 34915 and verapamil on electrical and mechanical activity in rat portal vein.

Authors:  T C Hamilton; S W Weir; A H Weston
Journal:  Br J Pharmacol       Date:  1986-05       Impact factor: 8.739

8.  Charybdotoxin-sensitive K+ channels regulate the myogenic tone in the resting state of arteries from spontaneously hypertensive rats.

Authors:  M Asano; K Masuzawa-Ito; T Matsuda
Journal:  Br J Pharmacol       Date:  1993-01       Impact factor: 8.739

9.  Interaction of potassium channel openers and blockers in canine atrial muscle.

Authors:  T Yanagisawa; H Hashimoto; N Taira
Journal:  Br J Pharmacol       Date:  1989-07       Impact factor: 8.739

10.  Characterization of high affinity binding sites for charybdotoxin in sarcolemmal membranes from bovine aortic smooth muscle. Evidence for a direct association with the high conductance calcium-activated potassium channel.

Authors:  J Vázquez; P Feigenbaum; G Katz; V F King; J P Reuben; L Roy-Contancin; R S Slaughter; G J Kaczorowski; M L Garcia
Journal:  J Biol Chem       Date:  1989-12-15       Impact factor: 5.157

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  2 in total

1.  Effects of SCA40 on human isolated bronchus and human polymorphonuclear leukocytes: comparison with rolipram, SKF94120 and levcromakalim.

Authors:  J Cortijo; V Villagrasa; C Navarrete; C Sanz; L Berto; A Michel; P A Bonnet; E J Morcillo
Journal:  Br J Pharmacol       Date:  1996-09       Impact factor: 8.739

2.  Further analysis of the mechanisms underlying the tracheal relaxant action of SCA40.

Authors:  S J Cook; K Archer; A Martin; K H Buchheit; J R Fozard; T Müller; A J Miller; K R Elliott; R W Foster; R C Small
Journal:  Br J Pharmacol       Date:  1995-01       Impact factor: 8.739

  2 in total

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