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1.
Summary— To investigate if the functional alterations observed in resistance arteries of spontaneously hypertensive rats (SHRs) were also present at the coronary level, in vitro experiments were performed in mesenteric resistance arteries (MRA) and in right (RIC) and left interventricular coronary (LIC) arteries taken from 15–25-week-old SHR and age-matched Wistar Kyoto rats WKYs. Using a passive extension protocol, internal diameters corresponding to 100 mmHg intraluminal pressure (D100) were determined and vessels were set up to a normalized internal diameter (0.9 D100). SHR mesenteric resistance arteries had a significantly smaller diameter compared to WKY arteries, whereas both types of SHR coronary arteries had a greater diameter compared to those of WKY rats. In arteries in the absence of contracting agonist, nitro-L-arginine (NOLA, 100 μM) induced a progressive rise in basal tone, which could be reversed by subsequent addition of L-arginine (100 μM) but not D-arginine (100 μM). When expressed as percent of maximal contractions induced by agonists (noradrenaline, NA [10 μM] in MRA; serotonin, 5-HT [10 μM], in RIC and LIC), these contractions were significantly stronger in WKY compared to SHR coronary and mesenteric resistance arteries. In NA-precontracted MRA and 5HT-precontracted coronary arteries in the presence of indomethacin (10 μM), the magnitude of acetylcholine-induced maximal relaxations (expressed as percent of maximal contractions induced by agonists) was greater in WKY compared to SHR arteries. After a 30-min incubation period, NOLA (100 μM) completely inhibited relaxations induced by acetylcholine (0.01–10 μM) in all types of precontracted arteries. Subsequent additions of sodium nitroprusside, (SNP, 10 μM) induced complete relaxations in all preparations. These results show that a basal release of NO or NO-like compound by endothelial cells is present in isolated mesenteric resistance and coronary arteries of WKY rats and SHRs. The contribution of endothelium-derived relaxing factor-nitric oxide (EDRF-NO) to arterial tone was lower in MRA compared to coronary arteries in both strains and in SHR compared to WKY arteries. In the SHR preparations, the impaired relaxation induced by acetylcholine appeared to be due to a functional alteration of the endothelium in the presence of normal reactivity of the smooth muscle cells. 相似文献
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表小檗碱对α受体的作用 总被引:2,自引:0,他引:2
表小檗碱(epiberberine,EB)是从湖北产黄连(Coptis chinensis Franch)中提取的一种生物碱,属苯喹嗪类原小檗碱,对其药理作用的研究资料甚少,未见其对α肾上腺素体作用的报道。资料表明,许多原小檗碱类化合物有α受体阻滞作用,为从该类化合物中选择 相似文献
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Zusammenfassung Obwohl Arbeitsunf?higkeit (AU) eine direkte Folge der durch die Erkrankung reduzierten Arbeitskraft ist, wurde sie im Frühstadium
der chronischen Polyarthritis (cP) kaum untersucht. Deshalb wurden die H?ufigkeit und die Dauer der AU in einer multizentrischen
Querschnittsstudie von Patienten im Frühstadium der cP (≤12 Monate Krankheitsdauer) im Vergleich zu Pflichtmitgliedern der
gesetzlichen Krankenversicherung ermittelt. 134 ambulante erwerbst?tige Patienten erfüllten die Kriterien des American College
of Rheumatology für die cP von 1987: 85 Frauen (63% von 134 Patienten), Alter im Median 50 Jahre. AU wurde entsprechend den
Patientenangaben zur „Krankschreibung“ dokumentiert. Bei der im Median 7 Monate bestehenden Erkrankung trat bisher wenigstens
einmal AU wegen cP bei 102 Patienten (76%) auf. Sie bestand bei den M?nnern für ca. 11 Tage pro Monat, d.h. ca. ein Drittel
der Krankheitszeit, und bei den Frauen für 8 Tage pro Monat entsprechend ca. einem Viertel der seit Beginn der cP vergangenen
Zeit. AU wegen cP dauerte fast fünfmal l?nger als aufgrund der Referenzdaten zu erwarten war. über die „Krankschreibung“ wegen
cP hinaus waren diese Patienten wegen anderer Erkrankungen etwa im gleichen Ausma? wie in die Referenzpopulation arbeitsunf?hig.
Der gro?e Anteil der von Arbeitsunf?higkeit wegen cP betroffenen Patienten und die Dauer der AU verdeutlichen das Ausma? gravierender
Beeintr?chtigungen der Erwerbst?tigkeit bereits im ersten Jahr der cP.
Eingegangen: 21. M?rz 1996 Akzeptiert: 11. November 1996 相似文献
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Quinoids undergo metabolism by a number of flavoenzymes. Reactive species formed during the metabolism of some quinoids might be anticipated to inhibit flavoenzyme activity. Several quinoids have been tested for their ability to inhibit rat liver thioredoxin reductase (TR). The antitumor quinones diaziquone and doxorubicin, and the quinoneimine 2,6-dichloroindophenol, were found to be inhibitors of the reduction of 5,5'-dithiobis-2-nitrobenzoic acid (DTNB) by TR. The inhibition was most marked after incubation of the quinoid with NADPH and the enzyme for 60 min before adding DTNB, with Ki values of 0.5 microM for diaziquone, 0.5 microM for doxorubicin, and 0.07 microM for 2,6-dichloroindophenol. The three quinoids all produced a time-dependent and first order loss of TR activity. There was formation of electron spin resonance-detectable semiquinoid free radicals upon incubation of diaziquone, doxorubicin and 2,6-dichloroindophenol with TR and NADPH under anaerobic conditions. Oxygen radicals formed by redox cycling of the quinoids did not make a major contribution to the inhibition of TR by the quinoids, as shown by the absence of significant reversal of the inhibition by anaerobic incubation conditions and the lack of effect of the oxygen radical scavengers dimethyl sulfoxide, superoxide dismutase and catalase. It was not possible to demonstrate NADPH-dependent covalent binding of radiolabeled diaziquone or doxorubicin to the TR apoprotein. It is possible that the quinoids bind noncovalently to the enzyme apoprotein, or bind to the FAD prosthetic group. The results of the study suggest that some antitumor quinoids are mechanism-based inhibitors of TR showing metabolism- and time-dependent irreversible inhibition of enzyme activity. 相似文献
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Pernes JM; Vitoux JF; Brenoit P; Raynaud A; Parola JL; Roth JP; Angel CY; Fiessinger JN; Roncato M; Gaux JC 《Radiology》1986,158(2):481-485
Thirty-five patients hospitalized for recent angiographically documented arterial occlusion in the legs (27 femoropopliteal arteries and eight grafts) benefited from local fibrinolytic therapy delivered at the site of the occlusion with a 4- or 5-F catheter. This therapy combined a continuous urokinase (UK) infusion of 1,000 U/kg/hour and a lysyl plasminogen (LYS-PLG) infusion of 15 microkatals every 30 minutes. Angiographically confirmed lysis was obtained in 85% of the cases. Only 3% of the patients had major and 6% had minor groin hematomas. Only two patients had concentrations of fibrinogen as low as 100 mg/dl. Intravascular infusion of UK-LYS-PLG is as effective as streptokinase. Its excellent tolerance makes it a good alternative in the treatment of acute ischemia in the lower limbs. 相似文献