Adenylate cyclase substituted-phenyl

Table IV. Stimulation of Adenylate Cyclase and Arthropod Behavior by Substituted-Phenyl N-Methylformamidines.

Active site, model, 308f Adenylate cyclase stimulation, 118 substituted-phenyl... 

Thioxanthenes lack the ring nitrogen of phenothiazine, and the side chain is attached by a double bond. In all cases, the cis isomer (relative to the substituted phenyl ring) is more active. Electron-attracting substituents seem to have a cumulative effect. For instance, pifluthixol (4.89), with a fluorine and a trifluoromethyl substituent, is 5-10 times more potent than its parent flupenthixol (4.90), and has an inhibitory effect (IC50 = 9.7 X 10 ° M) on the DA-sensitive adenylate cyclase of the striatum. 

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