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the cyclohexyl ring did not dramatically alter the affinity. However, moving the methyl group to the 4-position (368) decreased affinity for both can-nabinoid receptors. Conversion of the two phenolic hydroxy groups of (367) to methoxy groups (369) reduced both CB1 and CB2 binding activity, CB1 affinity was decreased more than 700-fold. Further efforts to find more CB2 selective agonists in the dimethoxyphenyl series resulted in discovery of O-1966A (370), which has good affinity and selectivity for CB2 [Ki(CBi) =

AM1703 (371)

Another resorcinol derivative, AM 1703 (371), which has a carbon-carbon triple bond at the end of the alkyl chain, was reported to be a highly potent and selective CB2 agonist (Ki(CB2) = 0.59 pM, with 500-fold selectivity against CB1) [228].

BENZO[C]CHROMEN-6-ONE DERIVATIVES

Benzo[c]chromen-6-one derivatives, such as AM 1710 (372), were found to be CB2 selective agonists [229]. Although these compounds are structurally similar to the THC derivatives, the dimethyl group on 6-position of the

Table 6.35 CYCLOHEXYL RESORCINOL DERIVATIVES [227]

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