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R. Lemmens-Gruber H. Marei P. Heistracher 《Naunyn-Schmiedeberg's archives of pharmacology》1997,355(2):230-238
GE 68 ((Rac.)-1-[3-(Phenylethyl)-2-benzofuryl]-2-(propylamino)-ethanol hydrochloride) is structurally related to propafenone,
and exerts negative inotropic and negative chronotropic effects similar to the parent drug, but lacks any β-adrenoceptor blocking
activity contrary to propafenone. Thus, the electrophysiological effects of GE 68 were studied in papillary muscles, left
atria, Purkinje fibres, sinoatrial nodes and ventricular myocytes of the guinea-pig heart with the intracellular microelectrode
technique and the patch-clamp technique in the cell-attached mode.
The decrease of the maximum upstroke velocity (V˙max) by GE 68 (1 to 10 μM) was use- and frequency-dependent. V˙max recovered from the use-dependent block with a time constant of 4.1 ± 0.6 s. In papillary muscles and Purkinje fibres action
potential duration was shortened, while it was prolonged in left atria and sinoatrial nodes. Half-maximal steady-state inactivation
of the sodium channels was shifted to more negative membrane potentials (control: –91.5 ± 0.8 mV, 10 μM GE 68: –97.9 ± 2.5 mV).
The peak of the current-voltage relationship and the reversal potential were not changed by GE 68. The amplitude of the unitary
current remained unaltered, while open state probability was decreased. The most striking effect of GE 68 was an increase
of the number of sweeps without single channel openings (1 μM: 2 fold, 10 μM: 6 fold). GE 68 also caused a decrease of the
mean open times, and an increase of the mean closed times in unmodified and pronase-modified sodium channels.
Besides the lack of β-adrenoceptor blocking activity, data present a faster recovery from the use-dependent block by GE 68
and a lower affinity to inactivated sodium channels compared to the reference drug propafenone, as well as differences in
the effect on single channel kinetics.
Received: 25 July 1996 / Accepted: 14 October 1996 相似文献
3.
目的探讨过氧化物酶体增殖物激活受体δ(PPARδ)基因第四外显子的单核苷酸多态(C294T)是否与有氧运动能力及训练敏感性相关联。方法对102名中国北方地区汉族男性青年进行为期18周的耐力训练(每次5000米、每周3次)。强度以个体通气无氧阈(VT)对应的心率(HRVT)为标准,前10周采用95%通气无氧阈对应的心率(HRVT±3),后8周采用105%通气无氧阈对应的心率(HRVT±3)。递增负荷运动实验测定受试者训练前后VO2max及相关指标和跑节省化时的心率(HR)、通气量(VE)和摄氧量(VO2)。采用限制性片断长度多态(PCR-RFLP)法测定PPARδ基因C294T位点。结果三种基因型的分布频率分别为CC基因型9人(0.09)、CT基因型37人(0.36)和TT基因型56人(0.55),符合Hardy-Weinberg平衡。按基因型分组后,CC基因型训练前的VO2max相对值显著性高于CT基因型和TT基因型(P<0.05);携带不同基因型群体的VO2max、跑节省化测试中的各项指标的变化率无显著性差异(P>0.05)。结论PPARδ基因第四外显子的单核苷酸C294T多态与VO2max相对值的初始值相关联,但与有氧耐力训练效果不关联。 相似文献
4.
The purpose of this study was to evaluate the specificity of maximal oxygen uptake (Vo2max) and the dynamic response of oxygen uptake (Vo2) to sinusoidal work load in distance runners and in American-football players. Sinusoidal work load during ergometer cycling was carried from 30 W to 60% to Vo2max(60% Vo2max) for a 2 min period. Vo2 was measured by the breath-by-breath method. The subjects were 10 distance runners (DRs), 10 American-football players (AFPs), and 11 untrained men (UTM). Mean Vo2max was 64.4 mL kg-1 min-1 in the DRs, 53.1 mL kg-1 min-1 in the AFPs and 47.3 mL kg-1 min-1 in the UTM. The fundamental amplitudes ofthe Vo2 response, nomalized by dividing by steady state Vo2 at 60% Vo2max were similar in the AFPs (20.3%) and the UTM (19.5%), and both were significantly less than in the DRs (25.5%). Phase shift to work load expressed in degrees was similar in the AFPs (87.7d?) and UTM (88.0d?), but significantly greater than in the DRs (80.4d?). HR dynamics in all three groups were similar to a dynamic Vo2 response. These findings suggest that development of the dynamic Vo2 response and higher Vo2max in the AFPs there is no improvement in the dynamic Vo2 response. The results of the present study demonstrate that athletes participating in different sports have characteristic dynamic Vo2 responses during cycling exercise. 相似文献
5.
M. Boulangé J. C. Cnockaert G. Lensel E. Pertuzon B. Vigreux 《European journal of applied physiology》1979,41(1):17-25
Summary The effects of long-term fatigue upon maximal force and peak rate of tension development (PRTD) (dF/dt max) are studied in man (elbow flexors), in the rat (pseudo-isolated gastrocnemius muscle) and in the frog (isolated sartorius muscle). The muscles are fatigued by voluntary anisometric anisotonic contractions against an elastic resistance in man, and by maximal tetanic contractions in the frog and the rat. In man, the excitation level of the muscle is controlled by the integrated surface EMG of the biceps brachii. In the animals, the muscles are stimulated by a neurostimulator. The PRTD and the maximal isometric force are measured during fatigue tests.In man, frog and rat, the maximal voluntary isometric torque or the maximal force and the PRTD decrease initially more or less rapidly according to the power developed during the fatigue process, and then less rapidly. The relationship between PRTD and maximal force is linear in the animals and curvilinear in man.The variations of maximal force and PRTD are discussed in relation to the level of excitation of the muscles and of the composition in different motor units types and their spatio-temporal recruitment. From a biomechanical point of view, it seems necessary to study the behavior of the series elastic component during the evolution of long term fatigue. 相似文献
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7.
William Dunlop Lachlan Hegarty Margaret Staples Michele Levinson Michael Ben‐Meir Katherine Walker 《Emergency medicine Australasia : EMA》2018,30(1):61-66
Objective
We aimed to evaluate patient perceptions of medical scribes in the ED and to test for scribe impacts on ED Net Promoter Scores, Press Ganey Surveys and other patient‐centred topics.Methods
Exploratory semi‐structured interviews were conducted in the ED during wait times after scribed consultations. Interview results were used to derive topics relating to scribes. Items addressing these topics from validated surveys were combined with items from widely used patient satisfaction questionnaires. Questionnaires were administered in the ED by face‐to‐face approach while patients were waiting for admission/discharge or test results. Patients and doctors were blinded to the purpose of the questionnaire. The survey evaluated for non‐inferiority of scribed consultations, using Net Promoter Scores, Press Ganey questions and questions specific to the presence of the scribe.Results
Patient interviews did not identify any negative views regarding the presence of scribes during consultations. Thematic saturation was achieved after seven interviews. Two hundred and fifty‐eight patients were approached to complete the questionnaire, and 215 participated (83%); 95 and 118 participants in the scribed and non‐scribed groups, respectively. There was no difference between scribed and non‐scribed consultations on the following measures of satisfaction: the Net Promoter Score, Press Ganey questions, quality of information received from doctors, communication, privacy concerns or inhibition about revealing private information and room crowding.Conclusion
We found no evidence that scribes reduce patient satisfaction during emergency consultations, nor prompt discomfort that might cause a patient to withhold information. 相似文献8.
采用活动平板和心肺运动试验的方法,评定VVI起搏患者无氧阈和最大氧耗量。受试者40例,分为2组。病窦(SSS)组24人,年龄52.3±10.1岁。三度房室传导阻滞(Ⅲ°A-VB)组16人,年龄53.7±10.7岁。试验仪器包括Case-15活动平板心电图和CPX/MAX心肺运动试验系统。SSS组有8人运动未达到无氧阈,Ⅲ°A-VB组有9人运动未达到无氧阈。SSS组无氧阈的做功53.7±16.3W/min,氧耗量18.25±3.66ml/kg/min;Ⅲ°A-VB组无氧阈时的做功21.7±14.4W/min,氧耗量6.58±1.71ml/kg/min。极量运动时,SSS组的最大氧耗量26.20±8.33ml/kg/min,最大做功110±20W/min。Ⅲ°A-VB组最大氧耗量17.38±4.48ml/kg/min,最大做功886±16W/min。SSS组能够承受7METS的最大运动负荷。Ⅲ°A-VB组的最大运动负荷5METS。在进行康复训练时,SSS患者开始康复训练的运动强度5METS。Ⅲ°A-VB阻滞病人的康复训练应从2METS开始。 相似文献
9.