Drummond G I, Wernham S, Lukowiak K
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1985;80(1):129-33. doi: 10.1016/0742-8413(85)90143-4.
The effects of serotonin (5-HT), dopamine (DA), several peptides including FMRFamide and arginine vasotocin, the diterpene forskolin and Ca2+ were examined on adenylate cyclase in a particulate fraction from hearts of Aplysia californica. Enzyme activity was stimulated 6-7-fold by 5-HT (EC50, 1 microM) in the presence of GTP. Several 5-HT analogs particularly 5-methoxytryptamine and 5-methoxy-N-N-dimethyltryptamine were also active. The stimulatory action of 5-HT was antagonized by the 5-HT receptor blockers methergoline and metitepine and by the DA receptor blocker chlorpromazine. Dopamine had weak stimulatory action (EC50, 10 microM) and an efficacy relative to that of 5-HT of 0.3. The action of DA was antagonized by chloropromazine and metitepine. Several peptides including FMRFamide and arginine vasotocin had no effect on adenylate cyclase when tested over the concentration range 0.1-100 microM. The enzyme was stimulated 6-fold by the diterpene forskolin (EC50, 2 microM). 5-HT-stimulated activity was strongly inhibited by Ca2+. Calmodulin had no action on the enzyme in the presence of Ca2+.
研究了血清素(5-羟色胺,5-HT)、多巴胺(DA)、包括FMRF酰胺和精氨酸血管加压素在内的几种肽、二萜类福斯可林和Ca2+对加州海兔心脏微粒体部分腺苷酸环化酶的影响。在存在鸟苷三磷酸(GTP)的情况下,5-HT(半数有效浓度,EC50为1微摩尔)可使酶活性增强6至7倍。几种5-HT类似物,特别是5-甲氧基色胺和5-甲氧基-N,N-二甲基色胺也具有活性。5-HT的刺激作用可被5-HT受体阻滞剂麦角新碱和米氮平以及DA受体阻滞剂氯丙嗪所拮抗。多巴胺具有较弱的刺激作用(EC50为10微摩尔),相对于5-HT的效能为0.3。DA的作用可被氯丙嗪和米氮平所拮抗。在0.1至100微摩尔的浓度范围内测试时,包括FMRF酰胺和精氨酸血管加压素在内的几种肽对腺苷酸环化酶没有影响。二萜类福斯可林(EC50为2微摩尔)可使该酶活性增强6倍。Ca2+强烈抑制5-HT刺激的活性。在存在Ca2+的情况下,钙调蛋白对该酶没有作用。