Design, Synthesis and Bioactivity Evaluation of GnRH Antagonists with Low Histamine-releasing Potency

doi:10.7503/cjcu20130086

Chem. J. Chinese Universities ›› 2013, Vol. 34 ›› Issue (5): 1139.doi: 10.7503/cjcu20130086

• Organic Chemistry • Previous Articles Next Articles

Design, Synthesis and Bioactivity Evaluation of GnRH Antagonists with Low Histamine-releasing Potency

ZHOU Ning, LIN Fan-Cheng, GAO Xing, ZHOU Wen-Xia, CHENG Jun-Ping, LIU Ke-Liang, ZHANG Yong-Xiang

Beijing Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China

Received:2013-01-24 Online:2013-05-10 Published:2013-05-10
Contact: Keliang Liu E-mail:keliangliu55@126.com

Abstract

Abstract:

The histamine-releasing potency of gonadotropin-releasing hormone(GnRH) antagonists induced the serious side effect in clinical application. Because the histamine-releasing peptides usually had one or more basic amino acids. Therefore, the carboxyl groups were introduced to the position 6, 8 or N-terminal of GnRH in order to develop the safe GnRH antagonists, and novel GnRH analogues were synthesized. The experimental results showed that some GnRH analogues with carboxyl group not only have low histamine-releasing potency, but also retained intrinsical testesterone-inhibiting bioactivity. It suggested the method of decreasing the histamine-releasing potency of the peptides by introducing the carboxyl groups was feasible.

Key words: Histamine-releasing potency, Carboxyl group, GnRH

CLC Number:

O629.7

TrendMD:

ZHOU Ning, LIN Fan-Cheng, GAO Xing, ZHOU Wen-Xia, CHENG Jun-Ping, LIU Ke-Liang, ZHANG Yong-Xiang. Design, Synthesis and Bioactivity Evaluation of GnRH Antagonists with Low Histamine-releasing Potency[J]. Chem. J. Chinese Universities, 2013, 34(5): 1139.

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Design, Synthesis and Bioactivity Evaluation of GnRH Antagonists with Low Histamine-releasing Potency

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