Bilezikjian L M, Vale W W
Endocrinology. 1983 Nov;113(5):1726-31. doi: 10.1210/endo-113-5-1726.
The stimulation of GH secretion from the anterior pituitary by synthetic GRF (hpGRF) is associated with a rapid increase in cAMP production. Within 5 min of the addition of 1 nM hpGRF to cultured rat anterior pituitary cells, intracellular cAMP levels are elevated 6-fold, with a maximal response being observed at 30 min. cAMP accumulation in the extracellular medium is also enhanced by this peptide. Comparison of the two cellular responses (GH secretion and cAMP formation) at various concentrations of hpGRF indicates that 10 times more hpGRF is required to obtain half-maximal stimulation of cAMP production than for GH secretion. Somatostatin totally blocks hpGRF-stimulated GH release, but only partially attenuates cAMP production in the presence or absence of a phosphodiesterase inhibitor. Verapamil also inhibits GH release in response to hpGRF, but, unlike somatostatin, this effect is not associated with an attenuation of cAMP production. In fact, intracellular cAMP levels are slightly augmented in the presence of verapamil, indicating that Ca2+ is required for hormone release but not for the activation of adenylate cyclase. Consistent with this is the observation that the release of GH due to 8-bromo-cAMP is also blocked by verapamil. A requirement for Ca2+ is further indicated by the inhibitory effects of CoCl2 and CdCl2 on both basal and hpGRF-stimulated GH release. These results suggest that cAMP may play a role as an intracellular mediator of GRF action in somatotrophs and that Ca2+ is required for the release process. Somatostatin may exert its inhibitory effects on GH secretion either by interfering with cAMP production or by an action on the secretory process subsequent to cAMP production.
合成的生长激素释放因子(hpGRF)对垂体前叶生长激素(GH)分泌的刺激与环磷酸腺苷(cAMP)生成的快速增加有关。在培养的大鼠垂体前叶细胞中加入1 nM hpGRF后5分钟内,细胞内cAMP水平升高6倍,30分钟时观察到最大反应。该肽也增强了细胞外培养基中cAMP的积累。在不同浓度的hpGRF下比较两种细胞反应(GH分泌和cAMP形成)表明,获得cAMP生成的半数最大刺激所需的hpGRF比GH分泌多10倍。生长抑素完全阻断hpGRF刺激的GH释放,但在有或没有磷酸二酯酶抑制剂的情况下,仅部分减弱cAMP生成。维拉帕米也抑制对hpGRF的GH释放,但与生长抑素不同,这种作用与cAMP生成的减弱无关。事实上,在维拉帕米存在的情况下细胞内cAMP水平略有升高,表明Ca2+是激素释放所必需的,但不是腺苷酸环化酶激活所必需的。与此一致的是,观察到8-溴-cAMP引起的GH释放也被维拉帕米阻断。CoCl2和CdCl2对基础和hpGRF刺激的GH释放的抑制作用进一步表明需要Ca2+。这些结果表明,cAMP可能作为生长激素释放因子在生长激素细胞中作用的细胞内介质发挥作用,并且Ca2+是释放过程所必需的。生长抑素可能通过干扰cAMP生成或通过对cAMP生成后的分泌过程起作用来对GH分泌发挥其抑制作用。