SYNTHESIS AND BINDING-AFFINITY OF ,9A-HEXAHYDRO-9,4-(IMINOMETHANO)-1H-BENZ[F]INDENES - LIGANDS FOR THE PCP SITE OF THE NMDA RECEPTOR

A series of 2,3,3a,4,9,9a-hexahydro-9,4-(iminomethano) was prepared an d their ability to displace [H-3]TCP was measured. The 5-amino derivat ives 5 and 12b were the most potent members of this series with K-i va lues of 14 nM and 8 nM respectively, The orientation of the cyclopenta ne ring was crucial for binding potency, with the endo isomer 12a > 10 times more potent than the exo-isomer 13.