Voigt K H, Kiehling C, Frösch D, Schiebe M, Martin R
Neurosci Lett. 1981 Nov 18;27(1):25-30. doi: 10.1016/0304-3940(81)90200-7.
Immunocytochemical evidence for the occurrence of "vertebrate" peptides in the neuropil of the vena cava [12, 13] and the structural similarity between enkephalin precursor peptides and the molluscan cardioexcitatory peptide [16], lead us to study the action of enkephalin-related peptides on the octopus heart. Systemic hearts of Octopus vulgaris were perfused with sea wate and test substances and a crude extract of vena cave were added for 1 min; frequency and pressure were monitored continuously. The heptapeptide Leu5-enkephalin-Arg6-Phe7 and the Met5-analogue, both in the amidized form, displayed dose-response relationship with a sensitivity of about 10 nmol. The C-terminal tetrapeptide amides, Phe-Leu/Met-Arg-Phe-NH2, were active at the same doses. Opiate receptors do not seem to be involved in this action on the octopus heart, as naloxone treatment had no effect. Whereas the N-terminal portion of the heptapeptide is known to be crucial for activity as an opioid, the C-terminal NH2 group is essential for cardioexcitatory activity.
腔静脉神经纤维中存在“脊椎动物”肽的免疫细胞化学证据[12, 13]以及脑啡肽前体肽与软体动物心脏兴奋肽之间的结构相似性[16],促使我们研究脑啡肽相关肽对章鱼心脏的作用。用海水和测试物质灌注普通章鱼的体心脏,并添加腔静脉粗提物1分钟;持续监测频率和压力。七肽亮氨酸5 - 脑啡肽 - 精氨酸6 - 苯丙氨酸7及其甲硫氨酸5类似物,均为酰胺化形式,显示出剂量 - 反应关系,灵敏度约为10 nmol。C末端四肽酰胺,苯丙氨酸 - 亮氨酸/甲硫氨酸 - 精氨酸 - 苯丙氨酸 - NH2,在相同剂量下具有活性。纳洛酮处理无效,表明阿片受体似乎不参与对章鱼心脏的这种作用。虽然已知七肽的N末端部分作为阿片类物质对于活性至关重要,但C末端NH2基团对于心脏兴奋活性必不可少。