N

A series of 21 compounds, differing from (382) in the amide region, has been synthesised by Franciso et al. [278] and their biological properties studied.

The biological activity of the compounds was assessed in two binding assays using [3H]-CP 55,940 (see Table 6.36) and [3H]-rimonabant (data not shown), and their functional activity determined using a GTPgS assay. Upon

Table 6.36 MODIFIED AMIDE SUBSTITUENT ANALOGUES OF RIMONABANT

Me CONHR

Me CONHR

Cl

Cpd R CB! Ki (nM) CB2 K (nM) [ 35S] GTP-gS EC50 (nM)

(382)

Piperidine

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