Zamfirova R, Todorov S, Klusha V, Svirskis S, Muceniece R
Institute of Physiology, Bulgarian Academy of Sciences, Sofia.
Methods Find Exp Clin Pharmacol. 1988 Oct;10(10):609-12.
The effects of the C-terminal tripeptide fragment of substance P(SP-C-TP) and its interactions with substance P(SP) were studied on isolated smooth-muscle preparations (rat musculus anococcygeus and vas deferens and rabbit ear central artery). Like SP, SP-C-TP (1 x 10(-8) M-1 x 10(-4)M) potentiated contractions of vas deferens and musculus anococcygeus elicited by low frequency electrical stimulation (LFES), the effect of the fragment being much weaker than that of the neuropeptide. The potentiating effect of SP was strongly reduced by SP-C-TP. The fragment slightly decreased the noradrenaline (NA)-induced contractions of vas deferens only. When the pharmacological agents were applied extralumenally only high SP concentrations (1 x 10(-7)M and 1 x 10(-6)M) significantly potentiated the LFES-evoked smooth-muscle contractions. SP-induced potentiation was abolished by SP-C-TP. Intralumenal administration of the neuropeptide and its fragment always led to a marked inhibition of the LFES contractile effects. The observed effects suggest that SP-C-TP acts as a competitive dualist of SP. The data is interpreted in terms of the hypothesis that the neuropeptide fragments might perform as a natural antagonist of the peptides and may control their effects.
研究了P物质C末端三肽片段(SP-C-TP)的作用及其与P物质(SP)的相互作用,实验对象为离体平滑肌制剂(大鼠尾骨肌、输精管和兔耳中央动脉)。与SP一样,SP-C-TP(1×10⁻⁸M - 1×10⁻⁴M)增强了低频电刺激(LFES)引起的输精管和尾骨肌收缩,该片段的作用比神经肽弱得多。SP-C-TP强烈降低了SP的增强作用。该片段仅轻微降低了去甲肾上腺素(NA)诱导的输精管收缩。当仅在管腔外应用药物时,只有高浓度的SP(1×10⁻⁷M和1×10⁻⁶M)能显著增强LFES诱发的平滑肌收缩。SP-C-TP消除了SP诱导的增强作用。神经肽及其片段的管腔内给药总是导致LFES收缩效应的显著抑制。观察到的效应表明,SP-C-TP作为SP的竞争性拮抗剂发挥作用。这些数据根据以下假设进行解释:神经肽片段可能作为肽的天然拮抗剂发挥作用,并可能控制其效应。