Substituted hexahydrobenzodipyrans as 5-HT2A/2C receptor probes.

A pair of substituted hexahydrobenzodipyrans was designed as molecular probes for determining the steric restrictions of the agonist binding site of serotonin 5-HT2A and 5-HT2C receptors. The rationale for the design of these receptor ligands, their chemical synthesis, rat behavioral pharmacology in the two-lever drug discrimination assay using LSD-trained rats, affinity for cloned rat 5-HT2A and 5-HT2C receptors and agonist functional activities are reported.