Estrogen and selective estrogen receptor modulator LY117018 enhance release of nitric oxide in rat aorta.
Estrogen and selective estrogen receptor modulator LY117018 enhance release of nitric oxide in rat aorta.
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雌激素和选择性雌激素受体调节剂 LY117018 增强大鼠主动脉中一氧化氮的释放。
DOI：
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发表时间：
1997
影响因子：
3.5
通讯作者：
C. Breemen
中科院分区：
文献类型：
--
作者：
R. Rahimian;Ismail Laher;Gregory Dube;C. Breemen
我们报道了慢性皮下或口服雌激素和选择性雌激素受体调节剂LY117018在等长条件下对大鼠主动脉环一氧化氮释放的调节作用。在苯肾上腺素（PE； 2微米）收缩的主动脉中获得乙酰胆碱（ACh; 10[8] ~ 10[-5] M）的扩张剂反应，并在一氧化氮合酶抑制剂N - omega-硝基- l -精氨酸甲酯（L-NAME； 200微米）预处理前后生成收缩剂对乙酰胆碱（10[-8]~ 10[-5]M）的剂量反应曲线。从五组大鼠中获得组织片段，植入皮下微丸输送系统21天：(1)雄性大鼠，(2)假手术安慰剂治疗的雌性大鼠，(3)去卵巢安慰剂治疗的大鼠，(4)去卵巢17 -雌二醇（0.5 mg/粒）治疗的大鼠，(5)去卵巢17 -雌二醇（15 mg/粒）和17 -雌二醇（0.5 mg/粒）治疗的大鼠。假手术大鼠和去卵巢大鼠经雌激素处理后的主动脉环对乙酰胆碱的松弛程度（10[-6]~ 10[-5]M）高于去卵巢大鼠、孕酮加雌激素处理大鼠和雄性大鼠（P < 0.05）。与雄性大鼠、黄体酮加雌激素治疗大鼠和去卵巢大鼠相比，L-NAME治疗后PE反应更强（P < 0.05），对PE的敏感性相似。此外，口服LY117018大鼠主动脉环中乙酰胆碱诱导的松弛和l - name诱导的PE收缩增强与口服雌激素大鼠主动脉环的反应相似。结果表明，长期给予雌激素和LY117018可促进大鼠主动脉环内皮细胞一氧化氮的释放。
We report on the modulatory effects of chronic subcutaneous or oral estrogen and LY117018, a selective estrogen receptor modulator, on the release of nitric oxide in rings of rat aorta studied under isometric conditions. Dilator responses to acetylcholine (ACh; 10[8] to 10[-5] M) were obtained in phenylephrine (PE; 2 microM)-contracted aorta, and constrictor dose-response curves to PE (10[-8] to 10[-5] M) were generated before and after pretreatment with N omega-nitro-L-arginine methyl ester (L-NAME; 200 microM), an inhibitor of nitric oxide synthase. Tissue segments were obtained from five groups of rats implanted with a subcutaneous pellet delivery system for 21 days: (1) male, (2) sham-operated placebo-treated female, (3) ovariectomized placebo-treated, (4) ovariectomized, 17beta-estradiol treated (0.5 mg/pellet) and (5) ovariectomized, progesterone (15 mg/pellet) and 17beta-estradiol (0.5 mg/pellet)-treated. Aortic rings from sham rats and ovariectomized rats receiving estrogen relaxed more to ACh (10[-6] to 10[-5] M) than did the rings from ovariectomized, progesterone plus estrogen-treated and male rats (P < .05). They were also characterized by a greater potentiation of the PE responses after L-NAME compared with male, progesterone plus estrogen-treated and ovariectomized rats (P < .05) and a similar sensitivity to PE. In addition, ACh-induced relaxation and L-NAME-induced potentiation of PE contractions in aortic rings from rats dosed orally with LY117018 were similar to responses of aortic rings from rats dosed orally with estrogen. These results demonstrate that chronically administered estrogen and LY117018 enhance the release of nitric oxide from endothelium in rat aortic rings.
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DOI：
10.1152/ajpregu.1991.261.4.r1022
发表时间：
1991
期刊：
The American journal of physiology
影响因子：
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作者：
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DOI：
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发表时间：
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影响因子：
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作者：
Cheng,DY;Feng,CJ;Kadowitz,PJ;Gruetter,CA
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