Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues
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- 作者：Chhuttan L. Meenaa ; Avinash Thakurb ; Prajwal P. Nandekarc ; Shyam S. Sharmab ; Abhay T. Sangamwarc ; Rahul Jaina ; rahuljain@niper.ac.in" class="auth_mail" title="E-mail the corresponding author
- 关键词：TRH ; TRH analogues ; Synthesis ; TRH receptors ; TSH ; TRH-DE ; Molecular modeling
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：23 March 2016
- 年：2016
- 卷：111
- 期：Complete
- 页码：72-83
- 全文大小：1405 K
文摘
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A new series of TRH analogues was synthesized.
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Peptide 7k showed 925-fold selectivity towards mTRH-R2 receptor in the IP-1 assay.
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Peptide 7k showed 272-fold selectivity towards mTRH-R2 receptor in the FLIPR assay.
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Peptide 7k decreased the sleeping time by >76% in a PB-induced assay.