N. Tanaka et al., [2-(OMEGA-PHENYLALKYL)PHENOXY]ALKYLAMINES - SYNTHESIS AND DUAL DOPAMINE(2) (D-2) AND 5-HYDROXYTRYPTAMINE(2) (5-HT2) RECEPTOR ANTAGONISTIC ACTIVITIES, Chemical and Pharmaceutical Bulletin, 46(4), 1998, pp. 639-646
A series of [2-(omega-phenylalkyl)phenoxy]alkylamines was synthesized
and their 5-hydroxytryptamine(2) (5-HT2) and/or dopamine(2) (D-2) rece
ptor antagonistic activities were examined in vitro. [2-(4-Phenylbutyl
)phenoxy]alkylamines showed strong inhibition of both 5-HT2 and D-2 re
ceptors, In particular, [2-(4-phenylbutyl)phenoxy]methylpiperidine der
ivatives. 10b, 10i and 10q, exhibited potent inhibition. The structure
-activity relationships in this series of compounds are discussed.