Tümmler B, Maass G, Müller W, Lamprecht W
Biochim Biophys Acta. 1978 Mar 21;508(1):122-9. doi: 10.1016/0005-2736(78)90193-1.
Frog motor nerves and isolated heart cells from neonatal rats were incubated with solutions of open chain crown-type polyether or pyridinophane cryptand. The following alterations in membrane excitability and energy consumption were found: 1. The non-cyclic ligand stabilizes the resting potential of the frog nerve and reduces the pulsation rate of heart muscle cells. It is reversibly bound at the cell surface and does not affect the energy metabolism of the heart cells. (formula: see text) 2. The cryptand 1,12-dioxo-2,11-diaza-5,8,21,24-tetraoxa[12-8(2,11)] (2,6)-pyridinophane) ([2.2.1py]-diamide) is irreversibly bound by the tissues. It facilitates the depolarization of the nerve and shows a positively chronotropic effect upon the heart muscle cells. Single treatment of the cell cultures with 10 microgram [2.2.1py]-diamide per ml medium increased the activities of lactate dehydrogenase and of creatine kinase. When the cell cultures were treated three times at 24 h intervals with 10 microgram complexone/ml, the creatine kinase activity of the heart muscle cells decreased by about 40%. The physiological properties of the ligands are correlated with the stability of their alkali metal ion complexes and with the rate constants of complex formation. It is concluded that [2.2.1py]-diamide can act as a passive carrier for Na+ K+.
将青蛙运动神经和新生大鼠的离体心脏细胞与开链冠型聚醚或吡啶并环番穴醚溶液一起孵育。发现膜兴奋性和能量消耗有以下变化：1. 非环状配体可稳定青蛙神经的静息电位并降低心肌细胞的搏动率。它在细胞表面可逆结合，且不影响心脏细胞的能量代谢。（化学式：见正文）2. 穴醚1,12 - 二氧代 - 2,11 - 二氮杂 - 5,8,21,24 - 四氧杂[12 - 8(2,11)] (2,6) - 吡啶并环番（[2.2.1py] - 二酰胺）被组织不可逆结合。它促进神经去极化，并对心肌细胞显示正性变时作用。每毫升培养基用10微克[2.2.1py] - 二酰胺单次处理细胞培养物会增加乳酸脱氢酶和肌酸激酶的活性。当细胞培养物每隔24小时用10微克络合剂/毫升处理三次时，心肌细胞的肌酸激酶活性降低约40%。配体的生理特性与其碱金属离子络合物的稳定性以及络合物形成的速率常数相关。得出结论，[2.2.1py] - 二酰胺可作为Na + K +的被动载体。
