Synthesis, structure-activity relationship of nociceptin and its fragments

Dong Shouliang; Wang Tao; Chen Qiang

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Synthesis, structure-activity relationship of nociceptin and its fragments

机译：伤害感受肽及其片段的合成，构效关系

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Nociceptin(NC)and its 4 fragments have been synthesized by solid phase peptide synthesis. Their hypotensive activity and mechanism, MVD assay and structure-activity rela- tionship have been investigated. Results show that NC(1-13)NH_2 is smallest fragment that shares the same activity with NC. The truncation of C_terminal not only leads the decrease of receptor affinity but also the changes of receptor selectivity. The entire sequence may not be required for the full activity since NC(1-13)NH_2 is as active as NC.

机译：Nociceptin（NC）及其4个片段已通过固相肽合成法合成。已经研究了它们的降压活性和机理，MVD分析和结构活性关系。结果表明，NC（1-13）NH_2是与NC具有相同活性的最小片段。 C_末端的截短不仅导致受体亲和力的降低，而且导致受体选择性的改变。由于NC（1-13）NH_2与NC一样活跃，因此完整活动可能不需要整个序列。

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《Chinese science bulletin》 |1999年第18期|p.1655-1659|共5页
作者
Dong Shouliang; Wang Tao; Chen Qiang;
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正文语种 eng
中图分类自然科学现状及发展;
关键词
nociceptin; solid phase peptide synthesis; hypotensive activity;

机译：伤害感受素固相肽合成;降压活动;

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1. Synthesis and Structure-Activity Relationships of Triazaspirodecanone Derivatives as Nociceptin/Orphanin FQ Receptor Ligands [J] . Corrado Sandra, Battisti Umberto M., Sorbi Claudia, Chemical biology and drug design . 2015,第4期

机译：Triazaspirodecanone衍生物Nociceptin / Orphanin FQ受体配体的合成与构效关系
2. Discovery of {1-(4-(2-{hexahydropyrrolo(3,4-c)pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin- 1-yl)cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relationships. [J] . Hayashi S, Nakata E, Morita A, Bioorganic and medicinal chemistry . 2010,第21期

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3. Discovery of {1-(4-(2-{hexahydropyrrolo(3,4-c)pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin- 1-yl)cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relationships. [J] . Hayashi S, Nakata E, Morita A, Bioorganic and medicinal chemistry . 2010,第21期

机译：发现{{（4-（2- {6- {hexahydropyrrolo（3,4-c）pyrrol-2（1H）-yl} -1H-benzimidazol-1-yl）piperidin-1--1-yl）cyclooctyl}甲醇的系统性强Nociceptin / orphanin FQ受体作为镇痛药的新型非肽激动剂，用于神经性疼痛的治疗：设计，合成和构效关系。
4. Structure-activity relationships of linear and cyclic nociceptin analogs and conformational analysis by CD and NMR spectroscopy [C] . Ralf Schmidt, Ibtihal Fadhil, Katharine Carpenter, the International Peptide Symposium . 2001

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5. Synthesis of new glutamate receptor probes: I. Total synthesis of dysiherbaine, a potent glutamate receptor excitotoxin; II. Design and synthesis of dysiherbaine analogues; III. Synthesis and structure-activity relationships of substituted benzothiadiazides and their role as AMPA receptor modulators. [D] . Phillips, Dean Paul. 2001

机译：新型谷氨酸受体探针的合成：I. dysiherbaine的全合成，一种有效的谷氨酸受体兴奋性毒素；二。 dysiherbaine类似物的设计和合成；三，取代的苯并噻二叠氮化物的合成及其构效关系及其作为AMPA受体调节剂的作用。
6. Probing ligand recognition of the opioid pan antagonist AT-076 at nociceptin kappa mu and delta opioid receptors through structure-activity relationships [O] . V. Blair Journigan, Willma E. Polgar, Edward W. Tuan, -1

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7. Comparison of the structure-activity relationships of nociceptin and dynorphin A using chimeric peptides [O] . Lapalu Sophie, Moisand Christiane, Mazarguil Honoré, 1997

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8. Quantitative Structure-Activity Relationships of Beta-Adrenergic Agents. Application of the Computer Automated Structure Evaluation (CASE) Technique of Molecular Fragment Recognition [R] . Klopman, G., Kalos, A. N. 1986

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Synthesis, structure-activity relationship of nociceptin and its fragments

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