Skip to Content
Merck
CN
  • Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.

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

Bioorganic & medicinal chemistry letters (2010-11-09)
Yun W Alelyunas, James R Empfield, Dennis McCarthy, Russell C Spreen, Khanh Bui, Luciana Pelosi-Kilby, Cindy Shen
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
2-Propylpentanoic acid
Sigma-Aldrich
(±)-Sulpiride
Sigma-Aldrich
Ibuprofen, ≥98% (GC)
Sigma-Aldrich
Riluzole, solid
Sigma-Aldrich
Carbamazepine, meets USP testing specifications
Sigma-Aldrich
Ibuprofen, meets USP testing specifications
Supelco
Ibuprofen
Sigma-Aldrich
(±)-Vigabatrin
Sigma-Aldrich
5,5-Diphenylhydantoin, ≥98%
Sigma-Aldrich
Gabapentin, solid