GABAA receptor targeting peptide DZ2 with analgesic activity as well as synthesis method and application of GABAA receptor targeting peptide DZ2

The invention belongs to the technical field of biological medicines, and discloses a GABAA receptor-targeted cyclopeptide analgesic drug DZ2, the amino acid sequence of the GABAA receptor-targeted cyclopeptide analgesic drug DZ2 is Cys-Asn-Thr-Glu-Arg-Pro-Gly-Met-Leu-Asp-Phe-Lys-Gly-Lys-Ala-Lys-Trp...

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Bibliographische Detailangaben
Hauptverfasser: LU YANG, DONG LILONG, YU XIALIN, DU XIAONA, HAO HAN, ZHAO WEIXIN, CHEN MENGYU, WANG MIAOMIAO
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the technical field of biological medicines, and discloses a GABAA receptor-targeted cyclopeptide analgesic drug DZ2, the amino acid sequence of the GABAA receptor-targeted cyclopeptide analgesic drug DZ2 is Cys-Asn-Thr-Glu-Arg-Pro-Gly-Met-Leu-Asp-Phe-Lys-Gly-Lys-Ala-Lys-Trp-Asp-Ala-Trp-Cys, the N-terminal Cys and the C-terminal Cys form a ring through a disulfide bond, and the molecular weight is 2454.81 g/mol. The cyclic peptide can be obtained through classical Fmoc-solid phase synthesis, and plays an important role in drug development taking a GABAA receptor as a target spot. The compound provided by the invention can activate a GABAA receptor to generate a GABA-similar inward current. In addition, the DZ2 shows a good analgesic effect in a mouse pain model, and a new thought and theoretical basis are provided for development of analgesic drugs based on GABAA receptors. 本发明属于生物医药技术领域,公开了一种靶向GABAA受体的环肽类镇痛药物DZ2,其氨基酸序列为:Cys-Asn-Thr-Glu-Arg-Pro-Gly-Met-Leu-Asp-Phe-Lys-Gly-Lys-Ala-Lys-