Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 24, Pages 7312-7316Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.10.068
Keywords
CNS; Solubility; Lipophilicity; Toxicity
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We determined the experimental solubility of CNS marketed drugs. Of the 98 drugs measured, greater than 90% had solubility > 10 mu M in pH 7.4 buffer. Only seven drugs had solubility < 10 mu M. Using these data, we established a solubility criterion to support CNS discovery. The implication of poor solubility with potential safety concerns and undesirable side effects are discussed. (C) 2010 Elsevier Ltd. All rights reserved.
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