3. Umbruch 4.4..2005 - Online Pot

Cannabinoid chemistry: an overview 29
Structure 2
Structure 3
they discovered that these compounds acted not only as cyclooxygenase
inhibitors, but also as cannabinoid agonists [72]. In vitro structure–activity
relationship studies of these compounds led to numerous new compounds with
cannabinoid receptor agonist activity [73, 74]. The best-known compound in
this series is the conformationally restricted derivative WIN-55212-2 [75]. A
binding assay in rat cerebellum membranes has been developed. It makes use
of the stereospecific radioligand [ 3 H](R)-(+)-WIN-55212-2.
The first potent and selective antagonist of the central cannabinoid receptor
(CB 1), SR-141716A, was reported in 1994 by a group at Sanofi [76]. This
compound is not active on the peripheral cannabinoid receptor (CB 2) and has
rapidly become a new tool in the study of cannabinoid receptor mechanisms
and in research on new therapeutic agents. Another novel CB 1 antagonist,
LY320135, which is not as selective as the previous one, was reported soon