von Hungen K, Roberts S, Hill D F
Brain Res. 1975 Feb 7;84(2):257-67. doi: 10.1016/0006-8993(75)90980-4.
Cell-free preparations from superior and inferior colliculi of very young rats (1-3 days old) contained adenylate cyclase systems which were highly responsive to serotonin. The response to serotonin declined markedly during early development and was very low at maturity. Adenylate cyclase activity in the 10,000 times g particulate fraction from colliculi of newborn rats was significantly stimulated by 0.05 muM serotonin. Half-maximal activation was produced with less than 1 muM serotonin. Maximal stimulation of collicular adenylate cyclase was about 80% above basal enzyme activity and occurred with approximately 50 muM serotonin. Tryptamine and several derivatives of serotonin produced responses which were comparable to that obtained with serotonin; 5-methoxytryptamine was uniformly the most active compound tested. Norepinephrine or dopamine produced much smaller increases in adenylate cyclase activity. Stimulation of collicular adenylate cyclase by serotonin was significantly but incompletely blocked by serotonin antagonists, including d-lysergic acid diethylamide (d-LSD), 2-bromo-d-lysergic acid diethylamide, methysergide, 1-methyl-8 beta-carbobenzyloxy-aminomethyl-10 alpha-ergoline and cyproheptadine. Chlorpromazine also produced partial blockade. In contrast, l-lysergic acid diethylamide, haloperidol, propranolol, phenoxybenzamine and morphine were ineffective as serotonin blocking agents. Of the compounds which produced a partial blockage of serotonin action, d-LSD, cyproheptadine and chlorpromazine were themselves capable of stimulating adenylate cyclase activity. These results are consisent with the existence of multiple receptors in rat brain which are capable of interacting with indoleamines.
来自新生大鼠(1 - 3日龄)上丘和下丘的无细胞制剂含有对血清素高度敏感的腺苷酸环化酶系统。在早期发育过程中,对血清素的反应显著下降,成熟时则非常低。新生大鼠丘脑中10,000倍重力微粒部分的腺苷酸环化酶活性受到0.05μM血清素的显著刺激。血清素浓度低于1μM时可产生半数最大激活。丘脑中腺苷酸环化酶的最大刺激约比基础酶活性高80%,在血清素浓度约为50μM时出现。色胺和血清素的几种衍生物产生的反应与血清素相当;5 - 甲氧基色胺始终是测试的最具活性的化合物。去甲肾上腺素或多巴胺使腺苷酸环化酶活性的增加要小得多。血清素对丘脑中腺苷酸环化酶的刺激被血清素拮抗剂显著但不完全阻断,这些拮抗剂包括d - 麦角酸二乙酰胺(d - LSD)、2 - 溴 - d - 麦角酸二乙酰胺、美西麦角、1 - 甲基 - 8β - 苄氧羰基 - 氨基甲基 - 10α - 麦角灵和赛庚啶。氯丙嗪也产生部分阻断作用。相比之下,l - 麦角酸二乙酰胺、氟哌啶醇、普萘洛尔、酚苄明和吗啡作为血清素阻断剂无效。在产生血清素作用部分阻断的化合物中,d - LSD、赛庚啶和氯丙嗪本身能够刺激腺苷酸环化酶活性。这些结果与大鼠脑中存在能够与吲哚胺相互作用的多种受体相一致。