在兔尿道海绵体增加环磷酸鸟苷合成和钙进入封锁帐户氧化氮的独立可溶性鸟苷酸环化酶刺激BAY 41-2272的扩张活性

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所属分类:疗效
摘要

为了研究5环丙基-2- [1-(2-氟苄基)-1H-吡唑并[3,4-b]吡啶-3-基]嘧啶-4-基胺的直接松弛活性(BAY 41-2272)在将R …

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在兔尿道海绵体增加环磷酸鸟苷合成和钙进入封锁帐户氧化氮的独立可溶性鸟苷酸环化酶刺激BAY 41-2272的扩张活性

目标

为了研究的直接松弛活性5-环丙基-2- [1-(2-氟苄基)-1H- - 吡唑并[3,4-b]吡啶-3-基]兔阴茎尿道,并调查对一氧化氮(NO)介导的应答的调节作用嘧啶-4-基胺(BAY 41-2272)。

的方法

尿路上皮-完好(U +)和裸露(U-)环被安装在10毫升器官浴为等长力记录。细胞内环磷酸鸟苷(cGMP)的水平与特定的试剂盒进行定量。

结果

BAY 41-2272(0.0001〜10μmol/ L的)去氧肾上腺素收缩尿道环的松弛引起的(10微摩尔/ L),具有较高的效力( P <0.01) in U+ (pEC50 7.77 ± 0.09) compared with U− (pEC50 6.84 ± 0.19) preparations. The NO synthesis inhibitor Nω-nitro-L-arginine methyl ester (100 μmol/L) or the soluble guanylate cyclase inhibitor 1H-[1,2,4] oxadiazolo [4,3,-a]quinoxalin-1-one (ODQ) (10 μmol/L) had no effect on BAY 41-2272 responses in U+ or U− rings. The phosphodiesterase-5 inhibitor 伐地那非 (0.1 μmol/L) potentiated the relaxant effects of BAY 41-2272 in both U+ (10-fold) and U− (sevenfold) tissues. Ca2+-induced contractions in K+ depolarized rings were significantly attenuated by BAY 41-2272 (1 μmol/L) in an ODQ-insensitive manner. BAY 41-2272 (0.03–0.3 μmol/L) increased the amplitude and duration of electrical field stimulation–induced relaxations (1 to 32 Hz), as well as those evoked by the NO donor glyceryl trinitrate (0.0001 to 10 μmol/L). BAY 41-2272 induced ODQ-resistant increases in cGMP levels above baseline (approximately twofold) in both U+ and U− rings.

结论

BAY 41-2272松弛阴茎尿道以协同方式瓦特第i个NO。靶向可溶性鸟苷酸环化酶同BAY 41-2272可表示在排尿相关联的干扰的管理的新治疗受损NO-cGMP信号。

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