Discriminative stimulus effects of serotonin agonists, neutral antagonists, and inverse agonists in pigeons: perspectives on intrinsic efficacy measurements in vivo

Abstract

These data and the subsequent analyses suggest that the discriminative cues of MK212, methysergide, and mianserin are different and that the drug discrimination paradigm is a useful functional assay to examine intrinsic efficacy in vivo.

Synthesis and Structure–Activity Relationships of Tool Compounds Based on WAY163909, a 5-HT2C Receptor Agonist

“…Reaction of 16 with triphosgene provided the benzoxazanone, which was reacted with glycine to form the bisamide (18). Exhaustive reduction of both amides then provided the diamine, which was selectively protected as the Cbz carbamate (19). Formation of the nitroso compound (20) followed by reduction with titanium tetrachloride and magnesium metal provided the hydrazine (21) necessary for the Fischer indole synthesis step.…”

“…Our initial paper reported the synthesis and in vitro pharmacology of a homobivalent 5-HT 2A R antagonist . Here, we report the synthesis and structure–activity relationships (SAR) for derivatives of the selective 5-HT 2C R agonist WAY163909 ( 1 ) ,− which can be used to attach tethers [e.g., polyethylene glycol (PEG)] to link these molecules to various other partners. Versions of the basic structure were synthesized in which locations around the molecule, sites a – d ( 2 ), were modified to determine the viability of these locations as points for the attachment of a necessary linker.…”