Bioorganic & Medicinal Chemistry Letters 2010-12-15

Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.

Yun W Alelyunas, James R Empfield, Dennis McCarthy, Russell C Spreen, Khanh Bui, Luciana Pelosi-Kilby, Cindy Shen

文献索引：Bioorg. Med. Chem. Lett. 20 , 7312-6, (2010)

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摘要

We determined the experimental solubility of CNS marketed drugs. Of the 98 drugs measured, greater than 90% had solubility >10 μM in pH 7.4 buffer. Only seven drugs had solubility <10 μM. 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.Copyright © 2010 Elsevier Ltd. All rights reserved.