Stenton G R, Chow S M, Lau H Y
Department of Pharmacology, Basic Medical Sciences Building, Chinese University of Hong Kong, Shatin, New Territories.
Life Sci. 1998;62(3):PL49-54. doi: 10.1016/s0024-3205(97)01107-7.
Among the loop diuretics, frusemide possesses unique airway protective activities which may be due to the inhibition of airway inflammatory cells such as the mast cell. We previously reported that frusemide and disodium cromoglycate (DSCG) demonstrated a similar profile of inhibitory activities against histamine release from rat peritoneal mast cells activated by various stimuli which increased intracellular calcium via different routes. Furthermore, the inhibitory activities of both compounds demonstrated marked tachyphylaxis and we hence postulated that frusemide and DSCG might share the same mechanism of action which involves the prevention of extracellular calcium influx into the mast cell cytoplasm. The present study confirmed the postulation by (a) demonstrating that cross-tachyphylaxis exists between the two compounds and (b) extending the observations on histamine release to the influx of extracellular calcium (45Ca) into rat peritoneal mast cells.
在袢利尿剂中,速尿具有独特的气道保护活性,这可能归因于对气道炎症细胞(如肥大细胞)的抑制作用。我们之前报道过速尿和色甘酸钠(DSCG)对通过不同途径增加细胞内钙的各种刺激所激活的大鼠腹膜肥大细胞释放组胺具有相似的抑制活性。此外,两种化合物的抑制活性均表现出明显的快速耐受性,因此我们推测速尿和DSCG可能具有相同的作用机制,即防止细胞外钙流入肥大细胞胞质。本研究通过以下方式证实了这一推测:(a)证明两种化合物之间存在交叉快速耐受性;(b)将对组胺释放的观察扩展到细胞外钙(45Ca)流入大鼠腹膜肥大细胞的情况。