Nyborg N C, Byg-Hansen J, Mulvany M J
J Cardiovasc Pharmacol. 1985;7 Suppl 6:S43-6. doi: 10.1097/00005344-198500076-00008.
We have investigated the effect of felodipine [4-(2,3,-dichlorophenyl)-1,4-dihydro-2, 6-dimethyl-3-ethoxycarbonyl-5-ethoxycarbonylpyridine] on the calcium concentration response relations of noradrenaline-activated mesenteric resistance vessels from 3-mo-old spontaneously hypertensive (SHR) and age-matched Wistar-Kyoto (WKY) rats. SHR vessels were more sensitive to calcium (ED50 approximately equal to 5.49 X 10(-5) M) than WKY vessels (ED50 approximately equal to 1.01 X 10(-4) M) in control condition. Also, maximal active tension development in SHR vessels was greater (3.14 N/m) than in WKY vessels (2.22 N/m). Felodipine (10(-12) M) decreased calcium sensitivity in vessels from both strains and also decreased maximal active tension development of SHR vessels. In a higher concentration (5 X 10(-10) M), the calcium sensitivity of both SHR and WKY vessels became similar. The active tension development was equally reduced in both rat strains. The results indicate that at least part of the antihypertensive effect of felodipine is due to a direct vasodilation, and also that vessels from SHRs may be more sensitive to felodipine than those from WKY rats.
我们研究了非洛地平[4-(2,3-二氯苯基)-1,4-二氢-2,6-二甲基-3-乙氧羰基-5-乙氧羰基吡啶]对3月龄自发性高血压大鼠(SHR)和年龄匹配的Wistar-Kyoto(WKY)大鼠去甲肾上腺素激活的肠系膜阻力血管钙浓度反应关系的影响。在对照条件下,SHR血管比WKY血管对钙更敏感(SHR的半数有效浓度[ED50]约为5.49×10⁻⁵M,WKY的ED50约为1.01×10⁻⁴M)。此外,SHR血管的最大主动张力发展(3.14N/m)大于WKY血管(2.22N/m)。非洛地平(10⁻¹²M)降低了两种品系血管的钙敏感性,也降低了SHR血管的最大主动张力发展。在较高浓度(5×10⁻¹⁰M)时,SHR和WKY血管的钙敏感性变得相似。两种大鼠品系的主动张力发展均同等降低。结果表明,非洛地平的降压作用至少部分归因于直接血管舒张,并且SHR的血管可能比WKY大鼠的血管对非洛地平更敏感。