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American Chemical Society, ACS Medicinal Chemistry Letters, 12(2), p. 929-932, 2011

DOI: 10.1021/ml200206z

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Rational Drug Design Leading to the Identification of a Potent 5-HT2C Agonist Lacking 5-HT2B Activity

Journal article published in 2011 by Gang Chen, Sung Jin Cho, Xi-Ping Huang ORCID, Niels H. Jensen, Andreas Svennebring, Maria F. Sassano, Bryan L. Roth, Alan P. Kozikowski
This paper is available in a repository.
This paper is available in a repository.

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Abstract

The 5-HT(2C) receptor is an attractive drug target in the quest for new therapeutics to treat a variety of human disorders. We have previously undertaken a structural optimization campaign that has led to some potent and moderately selective 5-HT(2C) receptor agonists. After expanding our structure-function library, we were able to combine our datasets so as to allow the design of compounds of improved selectivity and potency. We disclose herein the structural optimization of our previously reported 5-HT(2B)/5-HT(2C) agonists, which has led to the identification of a highly selective 5-HT(2C) agonist, (+)-trans-[2-(2-cyclopropylmethoxyphenyl)cyclopropyl]methylamine hydrochloride, with an EC(50) of 55 nM and no detectable agonism at the 5-HT(2B) receptor.