Kappa receptor bivalent ligands.
Kappa receptor bivalent ligands.
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DOI：
10.2174/156802607779941251
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发表时间：
2007-01
影响因子：
3.4
通讯作者：
Xuemei Peng;J. Neumeyer
中科院分区：
文献类型：
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作者：
Xuemei Peng;J. Neumeyer
κ阿片激动剂和拮抗剂的二价配体，如norBNI和BNI，被用作阐明κ受体特征的工具。二价配体也可能是有效的镇痛剂，尽管迄今为止还没有一种用于临床。构效关系（SAR）和分子建模导致开发了一种更有效和选择性的κ拮抗剂（5 '-胍基纳曲吲哚，GNTI）。具有高的混合kappa/micro或混合kappa/delta亲和力和有趣的药理学性质的新型均二价和杂二价配体可能最终导致具有较少不良副作用的有用的镇痛剂。二价配体也被开发，可以作为探针的受体寡聚化和组织现象。结构独特的κ拮抗剂（JDTic）提供了表征κ阿片受体的额外工具。
Bivalent ligands of kappa opioid agonists and antagonists, such as norBNI and BNI, are used as tools to elucidate the kappa receptor characteristics. Bivalent ligands may also be effective analgesics although none have this far been used clinically. Structure-activity relationships (SAR) and molecular modeling led to the development of a more potent and selective kappa antagonist (5'-guanidinylnaltrindole, GNTI). Novel homo and hetero bivalent ligands with high mixed kappa/micro or mixed kappa/delta affinity and intriguing pharmacological properties may eventually lead to useful analgesics with fewer adverse side effects. Bivalent ligands were also developed that could act as probes of the receptor-oligomerzation and organization phenomena. A structurally unique kappa antagonist (JDTic) provides an additional tool to characterize kappa opioid receptor.