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={Kimberly E. Vanover and David M Weiner and Malath M. Makhay and Isaac Veinbergs and Luis R. Gardell and Jelveh Lameh and Andria L Del Tredici and Fabrice Piu and Hans H. Schiffer and Thomas R. Ott and Ethan S. Burstein and Allan K. Uldam and Mikkel Boas Thygesen and Nathalie Schlienger and Carl Magnus Andersson and Thomas Son and Scott C. Harvey and Susan B. Powell and Mark A. Geyer and Bo Tolf and Mark R. Brann and Robert E 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… 

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