Tokumoto H, Watanabe Y, Yamashita A, Arai Y, Hayaishi O
Brain Res. 1986 Jan 1;362(1):114-21. doi: 10.1016/0006-8993(86)91404-6.
The structural requirement of the prostaglandin D2 molecule for binding to the synaptic membrane fraction of rat brain was extensively studied by using various prostaglandin D derivatives. Most strict specificity was found in the structures of the cyclo-pentane ring and the double bond in 13,14-position. The addition and deprivation of the double bond in alpha- and omega-chain, except on 13,14-position, moderately affected the binding. The modification in the carboxyl terminus and omega-chain terminus did not seriously influence the binding. BW 245C and 9-beta-prostaglandin D2, potent agonists for the prostaglandin D2 receptor in the platelet membrane, were almost ineffective. [3H]prostaglandin D2 binding was not affected by the addition of various neuroactive substances to the binding assay mixture. Further, prostaglandin D2 did not affect the known neurotransmitter receptor bindings in the rat brain.
通过使用各种前列腺素D衍生物,对前列腺素D2分子与大鼠脑突触膜部分结合的结构要求进行了广泛研究。发现环戊烷环和13,14位双键的结构具有最严格的特异性。除13,14位外,α链和ω链双键的添加和去除对结合有中度影响。羧基末端和ω链末端的修饰对结合没有严重影响。BW 245C和9-β-前列腺素D2是血小板膜中前列腺素D2受体的有效激动剂,但几乎无效。在结合测定混合物中添加各种神经活性物质不会影响[3H]前列腺素D2的结合。此外,前列腺素D2不影响大鼠脑中已知的神经递质受体结合。