C3-heteroaroyl cannabinoids as photolabeling ligands for the CB2 cannabinoid receptor.
Bioorg Med Chem Lett
; 22(16): 5322-5, 2012 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-22796181
ABSTRACT
A series of tricyclic cannabinoids incorporating a heteroaroyl group at C3 were prepared as probes to explore the binding site(s) of the CB1 and CB2 receptors. This relatively unexplored structural motif is shown to be CB2 selective with K(i) values at low nanomolar concentrations when the heteroaromatic group is 3-benzothiophenyl (41) or 3-indolyl (50). When photoactivated, the lead compound 41 was shown to successfully label the CB2 receptor through covalent attachment at the active site while 50 failed to label. The benzothiophenone moiety may be a photoactivatable moiety suitable for selective labeling.
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Base de dados:
MEDLINE
Assunto principal:
Tiofenos
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Benzopiranos
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Canabinoides
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Receptor CB2 de Canabinoide
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Ligantes
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article