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学科主题: 公共卫生
题名:
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
作者: 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
发表日期: 2007-04-01
DOI: 10.1016/j.peptides.2007.01.002
卷: 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
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/123342
Appears in Collections:北京大学医药卫生分析中心_期刊论文

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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

Recommended Citation:
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.
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