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In vitro and in vivo characterization of opioid activities of endomorphins analogs with novel constrained C-terminus: Evidence for the important role of proper spatial disposition of the third aromatic ring
Yu, Ye; Shao, Xuan; Wang, Chang-Lin; Liu, Hong-Mei; Cui, Yun; Fan, Ying-Zhe; Liu, Jing; Wang, Rui
关键词endomorphins conformationally constrained analogs third aromatic ring spatial orientation opioid activities
刊名PEPTIDES
2007-04-01
DOI10.1016/j.peptides.2007.01.002
28期:4页:859-870
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
关键词[WOS]ACETYLCHOLINE-RELEASE ; ISOLATED BRONCHUS ; GUINEA-PIG ; RECEPTOR ; BINDING ; MOUSE ; RAT ; CONFORMATION ; INHIBITION ; PEPTIDES
英文摘要

In the present study, the C-terminus of endomorphin (Tyr(1)-Pro(2)-Trp/Phe(3)-Phe(4)-NH2, EMs) analogs [Xaa(4)-R]EMs, modified by substitution of a non-aromatic residue for Phe(4) and ending up with -NH-benzyl, were designed to generate an atypical conformation ally constrained peptide set. We investigated the effects of these analogs on the opioid receptors affinity, guinea pig ileum (GPI) and mouse vas deferens (MVD) activity, system arterial pressure (SAP), heart rate (HR), antinociception and colonic motility. Analogs 5 ([D-V-4- Bzl]EM1) and 10 ([D-V-4 -Bzl]EM2), which exhibit appropriate spatial orientations of the third aromatic ring, were about 3-4 times more potent than their parents both in vivo and in vitro. However, a drastic loss of activity was found in analogs 2 ([A(4)-Bzl]EM1) and 7 ([A(4)-Bzl]EM2), which possess improper spatial orientations of the third aromatic ring. Interestingly, analog 7 or 3 ([G(4) -Bzl]EM1), when injected intravenously (i.v.), produced significantly different changes in SAP from their parents. Surprisingly, analog 4 displayed relatively higher vasodepressor activity but significantly less potent colonic contractile activity than analog 5. This may be elicited by the differences in the spatial disposition of the third aromatic ring, which were verified by molecular modeling. Our results indicate that the proper spatial disposition of the third aromatic ring plays an important role in the regulation of pharmacological activities of EMs. (c) 2007 Elsevier Inc. All rights reserved.

语种英语
WOS记录号WOS:000245625900018
引用统计
被引频次:13[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/123342
专题北京大学医药卫生分析中心
作者单位1.Lanzhou Univ, State Key Lab Appl Organ Chem, Inst Biochem & Mol Biol, Lanzhou 730000, Peoples R China
2.Chinese Acad Sci, Lanzhou Inst Chem Phys, State Key Lab Oxo Synth & Select Oxidat, Lanzhou 730000, Gansu, Peoples R China
3.Peking Univ, Med & Hlth Anal Ctr, Beijing 100871, Peoples R China
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GB/T 7714
Yu, Ye,Shao, Xuan,Wang, Chang-Lin,et al. In vitro and in vivo characterization of opioid activities of endomorphins analogs with novel constrained C-terminus: Evidence for the important role of proper spatial disposition of the third aromatic ring[J]. PEPTIDES,2007,28(4):859-870.
APA Yu, Ye.,Shao, Xuan.,Wang, Chang-Lin.,Liu, Hong-Mei.,Cui, Yun.,...&Wang, Rui.(2007).In vitro and in vivo characterization of opioid activities of endomorphins analogs with novel constrained C-terminus: Evidence for the important role of proper spatial disposition of the third aromatic ring.PEPTIDES,28(4),859-870.
MLA Yu, Ye,et al."In vitro and in vivo characterization of opioid activities of endomorphins analogs with novel constrained C-terminus: Evidence for the important role of proper spatial disposition of the third aromatic ring".PEPTIDES 28.4(2007):859-870.
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