Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting
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- 作者：Lei Zhoua ; b ; Edward L. Stahla ; b ; Kimberly M. Lovella ; b ; Kevin J. Frankowskic ; Thomas E. Prisinzanoc ; Jeffrey Aubé ; c ; Laura M. Bohna ; b ; lbohn@scripps.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：Dynorphin ; Kappa opioid receptor ; [35S]GTPγS binding ; Mouse striatum ; Selectivity ; Drug discovery ; KOR antagonist
- 刊名：Neuropharmacology
- 出版年：2015
- 出版时间：December 2015
- 年：2015
- 卷：99
- 期：Complete
- 页码：131-141
- 全文大小：1310 K
文摘
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Dynorphin peptides stimulate [35S]GTPγS binding in KOR- and MOR-KO mouse striata.
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NorBNI and 5′GNTI block dynorphin-induced G protein coupling in KOR-KO striata.
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A novel sulfonamide KOR antagonist is more selective than NorBNI in mouse striatum.