Vasoactive intestinal peptide binding to specific receptors on rat parotid acinar cells induces amylase secretion accompanied by intracellular accumulation of cyclic adenosine 3'-5'-monophosphate.
Vasoactive intestinal peptide binding to specific receptors on rat parotid acinar cells induces amylase secretion accompanied by intracellular accumulation of cyclic adenosine 3'-5'-monophosphate.
复制标题
血管活性肠肽与大鼠腮腺腺泡细胞上的特定受体结合，诱导淀粉酶分泌，并伴随细胞内环腺苷 3-5-单磷酸的积累。
DOI：
10.1210/endo-116-2-686
复制
发表时间：
1985
期刊：
影响因子：
4.8
通讯作者：
T. Kanno
中科院分区：
文献类型：
--
作者：
Y. Inoue;K. Kaku;T. Kaneko;N. Yanaihara;T. Kanno
对分散的大鼠腮腺腺泡内血管活性肠肽(VIP)的特异性结合部位进行了研究。[125I]VIP的结合是快速的、可饱和的、可逆的和温度依赖的。Scatchard分析表明有两类功能独立的受体位点：每个细胞41,000个高亲和力-低容量位点，解离常数(Kd)为6.4 nM；每个细胞420,000个低亲和力-高容量位点，Kd值为150 nM。与VIP结构相关的N-末端组氨酸、C-末端异亮氨酸和分泌素对示踪剂结合的抑制作用分别比VIP弱30倍和200倍。肾上腺素和卡巴胆碱不能抑制[125I]VIP与腮腺腺泡细胞的结合。VIP以剂量依赖的方式刺激腮腺小叶cAMP积聚，并诱导淀粉酶分泌。在cAMP积聚(分别为VIP的1/12和1/80)和淀粉酶分泌(分别为VIP的1/40和1/500)方面，含有N-末端组氨酸和C-末端异亮氨酸和分泌素的多肽的效力低于VIP。P物质对cAMP无刺激作用，但对淀粉酶分泌的刺激作用强于VIP。这些观察结果清楚地表明，大鼠腮腺存在与腺苷环化酶系统偶联的VIP受体，该受体在调节淀粉酶的分泌中起着重要作用。VIP对腮腺功能的调节不依赖于肾上腺素或M胆碱能调节系统，也不受P物质的影响。
Specific binding sites for vasoactive intestinal polypeptide (VIP) were characterized in dispersed rat parotid acini. The binding of [125I]VIP was rapid, saturable, reversible, and temperature dependent. Scatchard analysis indicated two functionally independent classes of receptor sites: 41,000 high affinity-low capacity sites per cell with a dissociation constant (Kd) of 6.4 nM and 420,000 low affinity-high capacity sites per cell with a Kd of 150 nM. A peptide with N-terminal histidine and C-terminal isoleucine and secretin, which are structurally related to VIP, inhibited the tracer binding 30 and 200 times less strongly, respectively, than VIP. Epinephrine and carbachol did not inhibit [125I]VIP binding to parotid acinar cells. VIP stimulated cAMP accumulation in parotid lobules and induced amylase secretion in a dose-dependent manner. A peptide with N-terminal histidine and C-terminal isoleucine and secretin were less potent than VIP regarding cAMP accumulation (1/12 and 1/80 of VIP, respectively) and amylase secretion (1/40 and 1/500 of VIP, respectively). Substance P did not stimulate cAMP accumulation but stimulated amylase secretion more strongly than VIP. These observations clearly demonstrated the presence of VIP receptors coupled to adenylate cyclase system in the rat parotid gland, which plays an important role in the regulation of the amylase secretion. The regulation of parotid function by VIP was independent of the adrenergic or muscarinic regulatory system and of the influence of substance P.