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含硫配体的二亚硝基铁配合物的阴茎勃起活性。

Penile erectile activity of dinitrosyl iron complexes with thiol-containing ligands.

机构信息

Faculty of Biology, M.V. Lomonosov Moscow State University, Moscow, Russia.

出版信息

Nitric Oxide. 2011 May 31;24(4):217-23. doi: 10.1016/j.niox.2011.04.008. Epub 2011 Apr 29.

Abstract

It has been established that intracavernous injections of water-soluble dinitrosyl iron complexes (DNIC) with glutathione or cysteine (0.4-6.0μmoles/kg) to male rats induce short-term (2-3 min) penile erection along with a short-term drop of arterial pressure and appearance of protein-bound DNIC in cavernous tissue and circulating blood. The duration of erection and the hypotensive activity of DNIC increase dramatically after simultaneous intracavernous injection of DNIC and the phosphodiesterase-5 inhibitor papaverine. Surgical denervation of cavernous bodies does not influence the erectile activity of DNIC. No penile erection takes place after intravenous (instead of intracavernous) injection of the same dose of DNIC; in this case, protein-bound DNIC are detected only in the blood. These findings suggest that water-soluble DNIC with thiol-containing ligands (cysteine or glutathione) can be used as a basis in the design of a novel class of drugs for treating erectile dysfunctions.

摘要

已经证实,向雄性大鼠的海绵体内注射水溶性二亚硝基铁复合物(DNIC)与谷胱甘肽或半胱氨酸(0.4-6.0μmoles/kg),会引起短暂的(2-3 分钟)阴茎勃起,同时伴有动脉血压短期下降和海绵组织及循环血液中蛋白结合的 DNIC 出现。同时向海绵体内注射 DNIC 和磷酸二酯酶-5 抑制剂罂粟碱后,DNIC 的勃起持续时间和降压活性会显著增加。海绵体的外科去神经支配并不影响 DNIC 的勃起活性。静脉内(而非海绵体内)注射相同剂量的 DNIC 后不会发生阴茎勃起;在这种情况下,仅在血液中检测到蛋白结合的 DNIC。这些发现表明,含巯基配体(半胱氨酸或谷胱甘肽)的水溶性 DNIC 可作为设计治疗勃起功能障碍的新型药物的基础。

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