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New tetrazole-based selective anandamide uptake inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 May 01; Vol. 18 (9), pp. 2820-4. Date of Electronic Publication: 2008 Apr 04. - Publication Year :
- 2008
-
Abstract
- A new series of 1,5- and 2,5-disubstituted tetrazoles have been synthesized and evaluated as inhibitors of anandamide cellular uptake. Some of them inhibit the uptake process with a relatively high potency (IC(50)=2.3-5.1microM) and selectively over other proteins involved in endocannabinoid action and metabolism.
- Subjects :
- Alkylation
Animals
Arachidonic Acids metabolism
Biological Transport drug effects
COS Cells drug effects
Cell Line, Tumor drug effects
Chlorocebus aethiops
Endocannabinoids
Humans
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Models, Chemical
Polyunsaturated Alkamides metabolism
Structure-Activity Relationship
Tetrazoles chemical synthesis
Arachidonic Acids antagonists & inhibitors
Polyunsaturated Alkamides antagonists & inhibitors
Tetrazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18424134
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.04.003