Potent Biphalin Analogs with μ/δ Mixed Opioid Activity: In Vivo and In Vitro Biological Evaluation

被引：10
作者：
Costante, Roberto [1 ]
Pinnen, Francesco [1 ]
Stefanucci, Azzurra [2 ]
Mollica, Adriano [1 ]
机构：
[1] Univ Chieti Pescara G dAnnunzio, Dipartimento Farm, I-66100 Chieti, Italy
[2] Univ Roma La Sapienza, Dipartimento Chim, I-00185 Rome, Italy
来源：
ARCHIV DER PHARMAZIE | 2014年 / 347卷 / 05期
关键词：
Analgesic; Antinociception; Biphalin; Intrathecal administration; Opioids; ANTINOCICEPTIVE PROFILE; HYDRAZINE TOXICITY; ENKEPHALIN ANALOG; DEPENDENCE LIABILITY; PEPTIDE BIPHALIN; SPINAL-CORD; PROTEINS; MORPHINE; RAT; BINDING;
D O I：
10.1002/ardp.201300380
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Biphalin [(Tyr-D-Ala-Gly-Phe-NH-)(2)] is an octapeptide with mixed / opioid activity. Its structure is based on two identical enkephalin-like portions linked tail-to-tail by a hydrazine bridge. This study presents the synthesis and in vitro and in vivo bioassays of two biphalin analogs that do not present the toxicity connected with the presence of the hydrazine moiety and are able to elicit a higher antinociceptive effect than biphalin.
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页码：305 / 312
页数：8
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