Bleehen Tirza, Keele C A
Department of Pharmacology and Therapeutics, The Middlesex Hospital Medical School, London W1P 7PN, Great Britain.
Pain. 1977 Aug;3(4):367-377. doi: 10.1016/0304-3959(77)90066-5.
The action of the adenyl compounds adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP) and adenosine was studied on the human blister base preparation. All 4 adenyl compounds produced pain which was slow in onset and not maintained. The threshold concentration for pain was of the order of 1-3 micron. The slopes of log concentration:pain intensity plots were relatively shallow and for moderate to severe pain a 100-fold increase of the threshold concentration was required. The adenyl compounds resembled 5-hydroxytryptamine and bradykinin with respect to onset and duration of action but were less potent. On the other hand, for threshold effects they were more potent than acetylcholine or potassium. Evidence was found for an interaction of adenyl compounds with 5-hydroxytryptamine but not with potassium, acetylcholine or bradykinin. Cyclic adenosine 3',5'-monophosphate or the chelation of extracellular calcium or magnesium were shown not to be involved in the algogenic action of adenyl compounds and the action of adenyl compounds on the rabbit isolated jejunum too was found to be unrelated to their algogenic action on the human blister base preparation.
研究了腺苷化合物三磷酸腺苷(ATP)、二磷酸腺苷(ADP)、一磷酸腺苷(AMP)和腺苷对人体水疱基底制剂的作用。所有这4种腺苷化合物均产生疼痛,起效缓慢且不能持续。疼痛的阈浓度约为1 - 3微米。对数浓度:疼痛强度图的斜率相对较浅,对于中度至重度疼痛,阈浓度需要增加100倍。腺苷化合物在作用起效和持续时间方面类似于5 - 羟色胺和缓激肽,但效力较低。另一方面,对于阈效应,它们比乙酰胆碱或钾更有效。发现有证据表明腺苷化合物与5 - 羟色胺相互作用,但与钾、乙酰胆碱或缓激肽无相互作用。结果表明,环磷酸腺苷3',5'-单磷酸或细胞外钙或镁的螯合不参与腺苷化合物的致痛作用,并且还发现腺苷化合物对兔离体空肠的作用与其对人体水疱基底制剂的致痛作用无关。