Neil T. Burford,Ying Han,Martyn N. Banks,Litao Zhang,Samuel Gerritz,Andrew Alt
申请号:
US15535652
公开号:
US20170370929A1
申请日:
2015.12.17
申请国别(地区):
US
年份:
2017
代理人:
摘要:
Described are the discovery, synthesis and pharmacological characterization of δ-opioid receptor-selective positive allosteric modulators (δ PAMs). These δ PAMs may increase the affinity and/or efficacy of the orthosteric agonists leu-enkephalin and SNC80, as measured by β-arrestin recruitment and adenylyl cyclase inhibition. The compounds may be useful pharmacological tools to probe the molecular pharmacology of the δ receptor and to explore the therapeutic potential of δ PAMs in diseases such as chronic pain and depression.