Koenig Andreas, Roegler Carolin, Lange Kathrin, Daiber Andreas, Glusa Erika, Lehmann Jochen
Lehrstuhl für Pharmazeutische/Medizinische Chemie, Institut für Pharmazie, Friedrich-Schiller-Universität Jena, Philosophenweg 14, D-07743 Jena, Germany.
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5881-5. doi: 10.1016/j.bmcl.2007.08.046. Epub 2007 Aug 28.
The vasoactive properties of 14 organic mononitrates were investigated in vitro using PGF(2alpha)-precontracted porcine pulmonary arteries. A surprisingly wide range of vasorelaxant potencies was observed (pD(2): 3.36-7.50). Activities showed to be highly sensitive to the molecular structure and the substituents at the molecular carrier of the nitrate group. A correlation between lipophilicity and vasorelaxant potency could not be recognized. 2-Nitrooxyethylammoniumnitrate (1) was found to be slightly superior to the high potency trinitrate GTN.
使用PGF(2α)预收缩的猪肺动脉，在体外研究了14种有机单硝酸酯的血管活性特性。观察到一系列令人惊讶的广泛血管舒张效力（pD(2)：3.36 - 7.50）。活性显示对分子结构以及硝酸酯基团分子载体上的取代基高度敏感。未发现亲脂性与血管舒张效力之间存在相关性。发现2 - 硝基氧乙基硝酸铵（1）略优于高效力的三硝酸酯GTN。
