CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity

5-HT2 Receptor Regulation of Mitochondrial Genes: Unexpected Pharmacological Effects of Agonists and Antagonists

“…It should be noted that the pK i values for CP-809,101 and SB-242,084 for the 5-HT 2C receptor are 0.1 nM and 10 nM, respectively (Table 1). CP-809101 is 1,000-fold more selective at the 5-HT 2C receptor compared with 5-HT 2A and 5-HT 2B receptors (Table 1) (Siuciak et al, 2007). Similarly, SB-242,084 is 10-100-fold more selective at the 5-HT 2C receptor compared with 5-HT 2A and 5-HT 2B receptors, respectively (Table 1) .…”

“…)methoxy]-6-(1-piperazinyl) pyrazine] (Siuciak et al, 2007), oxy]-3-pyridinyl]-1H-indole-1-carboxyamide dihydrochloride] , eplivanserin (Rinaldi-Carmona et al, 1992), and NBOH-2C-CN [4-[2-[[(2-hydroxyphenyl) (Hansen et al, 2014) were purchased from Tocris Bioscience (Ellisville, MO). All other chemicals were purchased from Sigma-Aldrich (St. Louis, MO).…”

“…Mice were individually housed in a temperature-controlled room under a 12-hour light/dark cycle and were randomly assigned to either a vehicle control group or one of two treatment groups. and SB-242,084 were chosen based on previously published studies Siuciak et al, 2007;Strong et al, 2009). At 24 hours after treatment, mice were euthanized by CO 2 asphyxiation followed by cervical dislocation.…”

Design, Synthesis, and Pharmacology of Fluorescently Labeled Analogs of Serotonin: Application to Screening of the 5-HT2C Receptor

“…24 following the discovery of 5a and establishing the fp binding assay for 5-ht 2c , we have generated fp binding data at 5-ht 2c , covering a range of chemical series with numerous examples from each series, which supports this claim (cornelius et al, unpublished data).…”

The pipeline and future of drug development in schizophrenia

“…Interestingly, a moderately selective 5-HT 2C agonist was recently shown to have antipsychotic-like effects on a battery of preclinical rodent models, including inhibition of conditioned avoidance response and amphetamine-induced hyperactivity, without inducing EPS. 88 Additionally, the weight gain and metabolic syndrome seen with administration of many of the atypical antipsychotics is thought to be due in part to antagonism of 5-HT 2C , as well as histamine H 1 receptors (Table 2). 89,90 Indeed, 5-HT 2C agonists have been shown to reduce food intake and body weight in humans.…”