期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 20, 页码 5432-5435出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.07.051
关键词
cannabinoid; cannabimimetic pyrroles; CB1 receptor; CB2 receptor
资金
- NIDA NIH HHS [DA15340, DA15579, DA03672, DA03590] Funding Source: Medline
Two series of 1-alkyl-2-aryl-4-(1-naphthoyl)pyrroles were synthesized and their affinities for the cannabinoid CB, and CB2 receptors were determined. In the 2-phenyl series (5) the N-alkyl group was varied from n-propyl to n-heptyl. A second series of 23 1-pentyl-2-aryl-4-(1-naphthoyl)-pyrroles (6) was also prepared. Several compounds in both series have CB, receptor affinities in the 6-30 nM range. The high affinities of these pyrrole derivatives relative to JWH-030 (1,R = C5H11) support the hypothesis that these pyrroles interact with the CB, receptor primarily by aromatic stacking. (c) 2006 Elsevier Ltd. All rights reserved.
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