Effects of relaxants on electrical and mechanical activities in the guinea-pig tracheal muscle.

In isolated tracheal muscles of the guinea-pig, effects of several relaxants were studied by simultaneously recording the membrane potential and mechanical response. Intracellular recordings showed regular slow waves in most preparations. There was a close correlation between membrane potential and slow wave amplitude. The linear regression line of the slow wave amplitude (Y mV) on the membrane potential (X mV) could be expressed by Y = -0.35X-5.9. The mean values of resting potential and slow wave amplitude were -50.6 +/- 0.6 mV and 11.9 +/- 0.5 mV, respectively. Relaxant drugs used (isoprenaline, terbutaline, adrenaline, noradrenaline, theophylline, forskolin and dibutyryl cyclic AMP) all produced hyperpolarization of the membrane and abolished the slow wave. The degree of relaxation was closely related to these electrical responses, although the recovery of electrical responses was faster than the mechanical response. It was concluded that the relaxation caused by the agents, which are known to increase the intracellular cyclic AMP level, was accompanied by a clear hyperpolarization and suppression of slow waves.     

Effects of palytoxin on mechanical and electrical activities of guinea pig papillary muscle.

Effects of palytoxin (PTX) on isolated papillary muscles of guinea pigs were studied in an attempt to elucidate the mechanical and electrical activities. Inotropic effects of PTX above 3 x 10(-9) g/ml; an early positive inotropic effect, slowly developing contracture accompanied by decline in phasic tension, appearance of aftercontractions and arrhythmias at high doses. The positive inotropic effect of PTX was enhanced in high Ca2+ medium but was not modified by propranolol. PTX induced a sustained depolarization and decrease in the amplitude, upstroke velocity and duration of action potential. During development of depolarization, arrhythmias occurred, which lasted for 5--10 min and reappeared 30--60 min after. Oscillatory afterpotential often appeared. Neither reserpine nor practolol prevented the PTX-induced arrhythmia while propranolol prevented it. Tetrodotoxin slowed the development of depolarization due to PTX and inhibited PTX-arrhythmias. In low Na+ medium, PTX exerted fewer effects on resting and action potentials and produced no arrhythmia. The results suggest that PTX-induced depolarization is responsible for the generation of contracture and arrhythmia and that the depolarization is due to the change in membrane Na permeability.     

Effects of pethidine and nalorphine on the mechanical and electrical activities of mammalian isolated ventricular muscle

1. The strength of the isometric mechanical contraction of electricallydriven ventricular muscle has been recorded simultaneously with the resting and action potentials; the effects of pethidine and of nalorphine on these parameters have been studied.2. When lower concentrations of pethidine (0.22-6.5 mug/ml) were perfused, isometric peak tension was decreased in parallel with the maximum upstroke velocity of the action potential; these actions are considered to result from membrane stabilization. At higher concentrations (11.8-109 mug/ml) pethidine usually produced, in addition, a progressive decrease in the resting and action potentials associated with marked irregularities in, or even abolition of, the mechanical response. It is suggested that these effects of the higher doses might be due to a depression of ATPase activity in the myocardial membrane.3. Compared with pethidine, nalorphine had similar, but weaker, actions.     

Effects of suramin on electrical and mechanical activities in antrum smooth muscle of the guinea-pig stomach

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The effects of lanthanum on electrical and mechanical events in mammalian cardiac muscle

1. The effects of various concentrations of lanthanum (La3+) on the force of contraction and on action potentials was investigated in isolated papillary muscles of the guinea-pig. 2. The force of contraction was initially reduced by La3+. During long exposure to high concentrations (i.e. 50, 100 and 500 muM) the contraction amplitude was increased again and a rise in resting tension was observed. These late changes in force of contraction also occurred after short exposure to 500 muM La3+ (2 min) when La3+ had been removed from the medium. 3. The action potentials were shortened at 20% of repolarization (plateau level) during La3+ exposure, whereas at 90% of repolarization a transient prolongation was observed. The resting potentials were reduced only at high concentrations and long duration of exposure. 4. 500 muM La3+ reduced the force of contraction to the control value obtained before addition of ouabain (5x10(-7)M). The ouabain-induced shortening in action potential duration at the plateau level was not reversed by the same concentration of La3+. 5. It is concluded that the action of La3+ on cardiac muscle cannot be explained by a simple displacement of superficially bound calcium. The characteristic effects observed at high concentrations reduce the value of La3+ as a pharmacological tool used in the study of calcium turnover.     

Effects of trapidil on electrical activities of canine ventricular muscle

The effects of N,N-diethyl-5-methyl[1,2,4]triazolo[1,5-alpha]pyrimidine-7-amine (trapidil) on the electrical activities of canine right ventricular muscle were studied using standard microelectrode techniques. Trapidil (10(-4) and 10(-3) mol/l) increased the plateau amplitude and shortened the duration of the action potential without changing the resting membrane potential and the maximum rate of rise of the action potential. Trapidil (10(-3) mol/l) restored regenerative action potentials (the slow response) in the ventricular muscle depolarized by elevation of extracellular K+ concentrations to 30 mmol/l. The slow response induced by trapidil was not affected by pindolol (10(-7) mol/l) which abolished that elicited by isoprenaline (10(-6) mol/l). These results indicate that the action of trapidil on the cardiac cell membrane is to increase the slow inward current during the action potential independently of stimulation of beta-adrenoceptors. Taken together with the results obtained by previous investigations the present results suggest that the increase in slow inward current during the action potential would be responsible for the positive inotropic effect of trapidil and would probably be related to its inhibitory action on cyclic AMP phosphodiesterase.     

Effects of phalloidin on electrical and mechanical activity of frog muscle fibres

The effects of phalloidin (10(-15) to 10(-5) M) on isolated muscle fibres of the frog were investigated under current or voltage clamp conditions in a double mannitol gap device coupled to a mechanoelectric transducer which allowed the estimation of isometric tension. The toxin significantly increased the action potential duration and the amplitude of the associated contraction. Under voltage-clamp conditions, for a concentration range of 10(-14) to 10(-8) M, phalloidin reversibly decreased (up to 42.7% +/- 3.1) the fast outward potassium current responsible for the delayed rectification. For concentrations from 10(-8) to 10(-5) M, the toxin irreversibly reduced (up to 43.3% +/- 2.9) the amplitude of the contractile response. It is concluded that, in skeletal muscle fibre of frog, phalloidin acts at two different levels, one which may be located at the outer face of the surface membrane while the other may be located deeper within the cell.     

Effects of trimebutine maleate on electrical activities of isolated mammalian cardiac preparations

The effects of trimebutine maleate on electrical activity in guinea-pig isolated papillary muscles and rabbit sino-atrial nodes have been studied by means of a standard microelectrode method. In papillary muscles, trimebutine (above 10 microM) decreased the maximum rate of rise (Vmax) and the action potential duration at 90% repolarization (APD90), whereas the resting potential was not significantly altered. As to a decrease in Vmax, trimebutine produced a negative shift of the curve relating Vmax to the resting potential along the voltage axis. Trimebutine also depressed the slow action potentials of papillary muscles produced by 27 mM K and 0.2 mM Ba. In spontaneously beating sino-atrial node preparations, trimebutine (above 10 microM) decreased the heart rate, Vmax and the rate of diastolic depolarization. These results indicate that trimebutine maleate possesses a depressant action on the electrical activities of the fast- and slow-response fibres of the heart mainly due to inhibitions of both fast Na+ and slow Ca2+ channels.     

Effects of aluminium on electrical and mechanical properties of frog atrial muscle.

1. The effects of aluminium on membrane ionic currents were studied in single cardiac myocytes. Most of the work was done on frog atrial cells, but some experiments were also carried out on single cells isolated from rabbit ventricles and atria. 2. The effects of aluminium on the force of contraction of frog atrial trabeculae were also investigated. 3. Aluminium was prepared from AlCl3 as a stock 0.5 M solution which has a pH of 3.5. Before each experiment, this solution was added to the control solution, to give a final concentration of 20-100 micrograms ml-1 aluminium (0.75-3.75 mM AlCl3). The solutions were brought to a pH of 7.4 or 7.6. at which they consist of a mixture of amorphous aluminium hydroxides and a very small amount of soluble ionic aluminium complexes: free aluminium cations (less than 10 pM), aluminohydroxide anions (less than 8 microM). The addition of this suspension reduced the peak inward calcium currents in single rabbit atrial and ventricular cells and in frog atrial cells. In the latter, the peak current was reduced (at + 10 mV) to 45% of control (mean of 9 cells). This effect was reversible upon washout, and was obtained at all membrane potentials, with no shift of the calcium current voltage relationship along the voltage axis. 4. Aluminium also reduced the time-dependent potassium current IK. This reduction was observed at all membrane potentials. For example, at + 10 mV, the mean reduction of IK (n = 9) was to 69% of the control amplitude. This effect, which was very difficult to reverse, was not due to IK rundown.(ABSTRACT TRUNCATED AT 250 WORDS)     

氯化汞对豚鼠心室肌电机械活动的影响

目的：观察氯化汞（ＨｇＣｌ２）对离体豚鼠乳头状肌的电生理作用。方法：采用心肌细胞内固定微电极技术。结果：ＨｇＣｌ２１～５０μｍｏｌ·Ｌ－１对豚鼠乳头状肌动作电位和收缩力的影响，具有剂量依赖性。ＨｇＣｌ２５μｍｏｌ·Ｌ－１使ＡＰＡ和Ｖｍａｘ降低，动作电位时程及ＥＲＰ缩短，心肌收缩力加强。用药物阻滞钙通道，ＨｇＣｌ２改变动作电位的ＡＰＡ，Ｖｍａｘ，ＡＰＤ。ＨｇＣｌ２１０～２０μｍｏｌ·Ｌ－１增加哇巴因诱发的震荡后电位，使触发电活动增强。结论：ＨｇＣｌ２对心脏的毒性，可能通过其使心肌细胞内钙超负荷。     

Further studies of the action of cyclic AMP on the electrical and mechanical activities of intestinal smooth muscle.

Effects of externally applied cyclic AMP and other adrenergic stimulants on the electrical and mechanical activities of the cat small intestine were observed by using pressure electrodes. The electrical and mechanical activities were suppressed by cyclic AMP and beta-stimulants. Those inhibitory actions of cyclic AMP and beta-stimulants were potentiated under the treatment with caffeine, theophylline and papaverine which inhibits the phosphodiesterase activity. On the other hand, the inhibitory action of cyclic AMP and beta-stimulants was decreased in imidazole, an agent that increases phosphodiesterase activity. Exogenous applied concanavalin A, an agent that inhibits the adenyl cyclase activity, showed no observable changes in both activities but the effects of beta-stimulants were decreased after treatment with concanavalin A. No obvious changes on both activities were obtained in cyclic GMP and dibutyryl cyclic GMP. These findings tentatively support the hypothesis that cyclic AMP is a second messenger in the inhibitory responses to beta-stimulants on the intestinal smooth muscle. However, it is also concluded that the inhibition of mechanical activity caused by cyclic AMP is partially due to suppression of the membrane activity.     

Effects of 3,4-diaminopyridine on mechanical and electrical responses of frog single muscle fibres

The effects of 3,4-diaminopyridine (3,4-DAP) were studied on isolated muscle fibres of the frog in concentrations ranging between 0.025 and 5.0 mM. Isometric twitch and tetanus responses were recorded at temperatures between 2.5 and 3.9 degrees. 3,4-DAP caused a concentration-dependent increase in twitch amplitude, maximum effects being obtained at a concentration of 3 mM with a mean increase in tension of 70 +/- 12% of control (n = 7). 3,4-DAP in 3 mM concentration had only a slight increase in initial rate of rise of twitch tension (mean increase 8 +/- 4%) but increased the time to half peak tension by 59 +/- 9% and the time from peak tension to half relaxation by 78 +/- 10%. No significant effect of 3,4-DAP was observed on the initial rate of rise and total amplitude of the isometric tetanus. The twitch potentiating effect of 3,4-DAP developed gradually with the number of times the fibre was stimulated and reached a maximum level after 40-50 stimulations. A gradual increase in the duration of the action potential was also observed. It is suggested that 3,4-DAP, like 4-aminopyridine, potentiates the twitch by means of prolonging the duration of the action potential.     

Effects of Bay K 8644 on the spontaneous electrical and mechanical activities of the rat portal vein

Summary Effects of Bay K 8644 on the spontaneous electrical and mechanical activities of the rat portal vein were studied. Bay K 8644 enhanced contractions in amplitude and duration. Bay K 8644 prolonged the duration of the spontaneous spike potential bursts and increased the number of spike potentials in a burst. These results indicate that the increase in the amplitude and duration of spontaneous contractions of the rat portal vein induced by Bay K 8644 are mediated mainly by the facilitation of the membrane electrical activity.Send offprint requests to: K. Shimamura at the above address     

Effect of diltiazem on electrical and mechanical activity of isolated cardiac ventricular muscle of guinea pig.

Diltiazem, a new 1,5-benzothiazepine derivative, antagonized calcium ion and thus caused a reduction in the contractile force of isolated papillary muscle. The antagonistic ratio of diltiazem to calcium ion was estimated to be approx. 1: 100. A lower concentration of diltiazem (2.2 x 10(-6) M) decreased the contractile force without affecting significantly the intracellularly recorded resting and action potentials. When the concentration of the compound was increased to 2.2 x 10(-5) M, only the maximum rate of rise of the action potential was reduced, while the other parameters of the action potential were also affected at 1.1 x 10(-4) M diltiazem. There was no significant change in the resting potential. Under conditions where the contractile force almost disappeared (1.1 x 10(-4) M), the membrane excitability was retained. It is concluded that diltiazem is an excitation-contraction uncoupler in the cardiac muscle cell and that the compound may exhibit its negative inotropic action by reducing in some way the intracellular concentration of free calcium ion available for the contractile mechanism.     

Comparison of pinaverium bromide, manganese chloride and D600 effects on electrical and mechanical activities in rat uterine smooth muscle

The effects of pinaverium bromide, were compared with those of D600 and manganese chloride (Mn), on membrane potentials, ionic currents and isometric contractions in uterine smooth muscle strips from pregnant rats. Pinaverium bromide (10(-7) - 10(-6) M) depressed twitch contractions and K-contractures within 15-20 min while D600 (2 X 10(-6) M) and Mn (10(-3) M) abolished both contractions. D600 and pinaverium bromide were more potent inhibitors in K-depolarized preparations than in polarized tissues. At a supramaximal dose (10(-5) M), pinaverium bromide decreased the rate of rise, amplitude, and rate of repolarization of the action potential, and prolonged the potential duration. The inward Ca current was depressed and the reduction in Cai was responsible for the decrease in K current. Pinaverium bromide (10(-5) M) depressed the myometrial contractions induced in Ca-free solution by acetylcholine (10(-4) M) and by prolonged membrane depolarizations. Mn (2.5 X 10(-3) M) only reduced the Ach-induced contraction and D600 (10(-5) M) had no effect on intracellular Ca stores. The results indicate that pinaverium bromide has Ca channel blocking properties similar to those of currently used Ca antagonists; it may also exert an effect to depress contractions supported by intracellular Ca release.     

戊巴比妥钠对豚鼠乳头状肌电活动和机械收缩的影响

戊巴比妥钠对豚鼠乳头状肌电活动和机械收缩的影响张翼，谷双振，郝永昌，宋立林，郭书梅，卢慎圭（河北医科大学生理教研室，石家庄０５００１７，中国）关键词戊巴比妥；电生理学；动作电位；乳头状肌；钾通道目的：研究戊巴比妥钠（ＳＰ）对豚鼠心室乳头状肌动作电位（...