Tatham P E, Cusack N J, Gomperts B D
Department of Experimental Pathology, University College London, U.K.
Eur J Pharmacol. 1988 Feb 16;147(1):13-21. doi: 10.1016/0014-2999(88)90628-0.
ATP (as the tetrabasic acid, ATP4-) applied externally to rat mast cells causes the formation of lesions which permit influx and efflux of low molecular weight, normally impermeant aqueous solutes. To monitor membrane permeabilisation we have used two fluorescent dyes, ethidium which stains the nucleus, and TMA-DPH which stains the cytosolic surfaces of intracellular membranes following entry into the cells Permeabilisation by ATP is not affected by the metabolic status of the cells, and is maintained at temperatures as low as 8 degrees C. We have tested the ability of 30 structural analogues of ATP to effect mast cell permeabilisation. The analogues include those having substituents in the 2- and 8-positions of the purine ring, structural and optical isomers of the ribose sugar, and variations in the triphosphate chain. The pattern of selectivity displayed by the rat mast cell ATP4- receptor is distinct from those characteristic of the P1 purinoceptor for adenosine and the P2X and P2Y purinoceptors for adenine nucleotides.
向大鼠肥大细胞外部施加ATP（作为四元酸，ATP4-）会导致形成损伤，使低分子量、通常不可渗透的水性溶质能够流入和流出。为了监测膜通透性，我们使用了两种荧光染料，一种是能对细胞核进行染色的溴化乙锭，另一种是进入细胞后能对细胞内膜的胞质表面进行染色的TMA-DPH。ATP引起的通透性不受细胞代谢状态的影响，并且在低至8摄氏度的温度下仍能维持。我们测试了30种ATP结构类似物影响肥大细胞膜通透性的能力。这些类似物包括在嘌呤环的2位和8位有取代基的化合物、核糖的结构和旋光异构体，以及三磷酸链的变化。大鼠肥大细胞ATP4-受体表现出的选择性模式不同于腺苷的P1嘌呤受体以及腺嘌呤核苷酸的P2X和P2Y嘌呤受体的特征模式。
