Dowdle E B, Maske R
Br J Pharmacol. 1980;71(1):235-44. doi: 10.1111/j.1476-5381.1980.tb10931.x.
1 The longitudinal muscle-myenteric plexus strip prepared from guinea-pig ileum has been used to study the actions of dipyridamole and its interactions with adenine derivatives. 2 Dipyridamole augmented the inhibitory effects of adenine derivatives on the twitch response induced by 0.1 Hz field stimulation of the preparation. This synergistic effect was apparent with relatively low concentrations of dipyridamole (10 to 100 nM) and after short pretreatment times (1 to 2 min) that did not inhibit the twitch response on their own. Appropriate studies suggested the dipyridamole-adenosine synergism followed a pattern of facilitative agonist competition. 3 Dipyridamole did not inhibit either uptake of [3H]-adenosine by the preparation or adenosine deaminase activity under the same conditions that it exhibited synergism with adenosine. 4 Higher concentrations of dipyridamole inhibited the twitch response, mainly by decreasing acetylcholine release but partly by a direct action on smooth muscle. The direct action of dipyridamole on muscle was not synergistic with adenosine. 5 Fluorescence microscopy showed preferential binding of dipyridamole to the myenteric plexus.
从豚鼠回肠制备的纵行肌 - 肌间神经丛条带已被用于研究双嘧达莫的作用及其与腺嘌呤衍生物的相互作用。
双嘧达莫增强了腺嘌呤衍生物对该制备物0.1Hz场刺激诱导的抽搐反应的抑制作用。这种协同效应在相对低浓度的双嘧达莫(10至100 nM)以及短预处理时间(1至2分钟)后很明显,这些低浓度和短时间预处理本身并不抑制抽搐反应。适当的研究表明双嘧达莫 - 腺苷协同作用遵循促进性激动剂竞争模式。
在与腺苷表现出协同作用的相同条件下,双嘧达莫既不抑制该制备物对[3H] - 腺苷的摄取,也不抑制腺苷脱氨酶活性。
更高浓度的双嘧达莫抑制抽搐反应,主要是通过减少乙酰胆碱释放,但部分是通过对平滑肌的直接作用。双嘧达莫对肌肉的直接作用与腺苷没有协同作用。
荧光显微镜显示双嘧达莫优先与肌间神经丛结合。