Pharmacological and Behavioral Profile of N-(4-Fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl) Carbamide (2R,3R)-Dihydroxybutanedioate (2:1) (ACP-103), a Novel 5-Hydroxytryptamine2A Receptor Inverse Agonist

@article{Vanover2006PharmacologicalAB,
  title={Pharmacological and Behavioral Profile of N-(4-Fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl) Carbamide (2R,3R)-Dihydroxybutanedioate (2:1) (ACP-103), a Novel 5-Hydroxytryptamine2A Receptor Inverse Agonist},
  author={K. Vanover and D. Weiner and M. Makhay and I. Veinbergs and L. Gardell and J. Lameh and Andria L. Del Tredici and F. Piu and H. Schiffer and T. Ott and E. Burstein and A. Uldam and M. Thygesen and N. Schlienger and C. Andersson and Thomas Son and S. C. Harvey and S. Powell and M. Geyer and Bo Tolf and M. Brann and R. Davis},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2006},
  volume={317},
  pages={910 - 918}
}
The in vitro and in vivo pharmacological properties of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103) are presented. A potent 5-hydroxytryptamine (5-HT)2A receptor inverse agonist ACP-103 competitively antagonized the binding of [3H]ketanserin to heterologously expressed human 5-HT2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. ACP-103 displayed potent inverse agonist… Expand
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