Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity.
Published
Journal Article
Exploration of the central CB1 cannabinoid receptors using positron emission tomography (PET) will allow for an understanding of the pharmacological and physiological role played by these receptors in the CNS. Current tracers are highly lipophilic compounds that exhibit very high nonspecific to specific binding ratios and as a result are inapt for use in humans. We have synthesized a series of less lipophilic analogues of SR141716 to serve as potential radioligands. Binding affinities of the series and a functional electrophysiological assay of three of our compounds have been presented.
Full Text
Duke Authors
Cited Authors
- Katoch-Rouse, R; Pavlova, OA; Caulder, T; Hoffman, AF; Mukhin, AG; Horti, AG
Published Date
- February 13, 2003
Published In
Volume / Issue
- 46 / 4
Start / End Page
- 642 - 645
PubMed ID
- 12570386
Pubmed Central ID
- 12570386
International Standard Serial Number (ISSN)
- 0022-2623
Digital Object Identifier (DOI)
- 10.1021/jm020157x
Language
- eng
Conference Location
- United States