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Efficacy in CB 1 receptor‐mediated signal transduction
Author(s) -
Howlett Allyn C
Publication year - 2004
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0705881
Subject(s) - receptor , signal transduction , colocalization , agonist , g protein , microbiology and biotechnology , g protein coupled receptor , effector , transduction (biophysics) , functional selectivity , biology , chemistry , pharmacology , biochemistry
CB 1 receptor cellular signal transduction is dependent on the expression of G proteins to which the receptor couples, the potential for precoupling of particular G proteins to the receptors either by scaffolding mechanisms or colocalization in lipid raft domains, and the effector mechanisms that these transducer molecules regulate. This discourse will evaluate studies of efficacy for CB 1 receptor‐Gi/o activation at the molecular level. Evidence for brain regional differences in CB 1 receptor signal transduction efficacy and agonist selectivity for G proteins will be summarized. The possibility that CB 1 receptors interact with Gs or Gq will be evaluated, and questions with regard to the constitutive activity and G protein sequestration will be posed. British Journal of Pharmacology (2004) 142 , 1209–1218. doi: 10.1038/sj.bjp.0705881