Exploration of the molecular architecture of the orthosteric binding site in the 伪4尾2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane
详细信息 查看全文
- 作者：Tinna B. Bacha ; Anders A. Jensena ; Jette G. Petersena ; Troels E. Sø ; rensena ; b ; Serena Della Volpea ; Jun Liub ; Antoni R. Blaazerc ; Jacqueline E. van Muijlwijk-Koezenc ; Thomas Balleb ; thomas.balle@sydney.edu.au" class="auth_mail" title="E-mail the corresponding author ; Bente Frø ; lunda ; bfr@sund.ku.dk" class="auth_mail" title="E-mail the corresponding author
- 关键词：nACh receptor agonists ; Structure&ndash ; activity studies ; Ls-AChBP ; Ac-AChBP ; Lobeline ; DMABC analogs
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2015
- 出版时间：18 September 2015
- 年：2015
- 卷：102
- 期：Complete
- 页码：425-444
- 全文大小：2552 K
文摘
- •
Elongated 伪4尾2 nAChR ligands have retained partial agonist profile.
- •
SAR indicate classical binding mode for the core agonist part of the molecule.
- •
Substituents bind along the subunit interface.
- •
Ligands showing preference for Ls-AChBP over Ac-AChBP.