1,1-DIPHENYL-3-DIALKYLAMINO-1-SILACYCLOPENTANE DERIVATIVES - A NEW CLASS OF POTENT AND SELECTIVE 5-HT2A ANTAGONISTS

A new series of 1,1-diphenyl-3-dialkylamino-1-silacyclopentanes was sy nthesized, and most compounds demonstrated moderate to high affinity f or the 5-HT2A receptor. A member of this series, compound 1p displays potent antagonist activity after oral administration against both mesc aline and DOI-induced head-twitches in mice and rats, with a long dura tion of action. The dextrorotatory isomer (+)-1p is highly more potent than the levorotatory isomer (-)-1p in in vitro and in in vivo assays .