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2
Effect of chronic intra-peritoneally administered chimeric peptide of met-enkephalin and FMRFa-[D-Ala2]YFa-on antinociception and opioid receptor regulation.慢性腹腔内给予[Met]-脑啡肽和 FMRFa-[D-Ala2]YFa 嵌合肽对镇痛和阿片受体调节的影响。
Eur J Pain. 2010 Mar;14(3):295.e1-9. doi: 10.1016/j.ejpain.2009.05.014. Epub 2009 Jun 26.
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Lack of tolerance and morphine-induced cross-tolerance to the analgesia of chimeric peptide of Met-enkephalin and FMRFa.对甲硫氨酸脑啡肽和FMRFa嵌合肽镇痛作用缺乏耐受性及吗啡诱导的交叉耐受性。
Peptides. 2008 Dec;29(12):2266-75. doi: 10.1016/j.peptides.2008.09.013. Epub 2008 Sep 26.
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Kappa opioid antagonists: past successes and future prospects.κ阿片受体拮抗剂：过去的成就与未来的前景
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YFa 及其类似物：平滑肌收缩中阿片受体的研究。

YFa and analogs: investigation of opioid receptors in smooth muscle contraction.

机构信息

Peptide Synthesis Laboratory, Institute of Genomics and Integrative Biology, Delhi 110007, India.

出版信息

World J Gastroenterol. 2011 Oct 28;17(40):4523-31. doi: 10.3748/wjg.v17.i40.4523.

DOI:10.3748/wjg.v17.i40.4523
PMID:22110284
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3218144/
Abstract

AIM

To study the pharmacological profile and inhibition of smooth muscle contraction by YFa and its analogs in conjunction with their receptor selectivity.

METHODS

The effects of YFa and its analogs (D-Ala2) YFa, Y (D-Ala2) GFMKKKFMRF amide and Des-Phe-YGGFMKKKFMR amide in guinea pig ileum (GPI) and mouse vas deferens (MVD) motility were studied using an isolated tissue organ bath system, and morphine and DynA (1-13) served as controls. Acetylcholine was used for muscle stimulation. The observations were validated by specific antagonist pretreatment experiments using naloxonazine, naltrindole and norbinaltorphimine norBNI.

RESULTS

YFa did not demonstrate significant inhibition of GPI muscle contraction as compared with morphine (15% vs 62%, P = 0.0002), but moderate inhibition of MVD muscle contraction, indicating the role of κ opioid receptors in the contraction. A moderate inhibition of GPI muscles by (Des-Phe) YFa revealed the role of anti-opiate receptors in the smooth muscle contraction. (D-Ala-2) YFa showed significant inhibition of smooth muscle contraction, indicating the involvement of mainly δ receptors in MVD contraction. These results were supported by specific antagonist pretreatment assays.

CONCLUSION

YFa revealed its side-effect-free analgesic properties with regard to arrest of gastrointestinal transit. The study provides evidences for the involvement of κ and anti-opioid receptors in smooth muscle contraction.

摘要

目的

研究 YFa 及其类似物对平滑肌收缩的药理学特征和抑制作用，并研究其与受体选择性的关系。

方法

采用离体组织器官浴槽系统，研究 YFa 及其类似物（D-Ala2）YFa、Y（D-Ala2）GFMK-KKFMRF 酰胺和 Des-Phe-YGGFMKKKFMR 酰胺对豚鼠回肠（GPI）和小鼠输精管（MVD）运动的影响，并用吗啡和 DynA（1-13）作为对照。乙酰胆碱用于肌肉刺激。通过使用纳洛酮嗪、纳曲吲哚和 norbinaltorphimine norBNI 进行特异性拮抗剂预处理实验，对观察结果进行了验证。

结果

与吗啡（15%对 62%，P=0.0002）相比，YFa 对 GPI 肌肉收缩没有明显的抑制作用，但对 MVD 肌肉收缩有中度抑制作用，表明 κ 阿片受体在收缩中起作用。（Des-Phe）YFa 对 GPI 肌肉的中度抑制揭示了抗阿片受体在平滑肌收缩中的作用。（D-Ala-2）YFa 对平滑肌收缩有显著抑制作用，表明 δ 受体主要参与 MVD 收缩。这些结果得到了特异性拮抗剂预处理实验的支持。

结论

YFa 显示出其对胃肠道转运的无副作用的镇痛特性。该研究为 κ 和抗阿片受体参与平滑肌收缩提供了证据。