Literature DB >> 21055935

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

Yun W Alelyunas1, 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.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21055935     DOI： 10.1016/j.bmcl.2010.10.068

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

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3.  A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways.

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Journal:  Mol Divers       Date:  2022-06-23       Impact factor: 2.943

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Authors:  Mingjie Cui; Dominik J Naczynski; Margot Zevon; Craig K Griffith; Larisa Sheihet; Izmarie Poventud-Fuentes; Suzie Chen; Charles M Roth; Prabhas V Moghe
Journal:  Adv Healthc Mater       Date:  2013-03-12       Impact factor: 9.933

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Authors:  Shi Quan Wong; Matthew G Pontifex; Marie M Phelan; Chandra Pidathala; Brian C Kraemer; Jeff W Barclay; Neil G Berry; Paul M O'Neill; Robert D Burgoyne; Alan Morgan
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Review 7.  Carboxylic Acid Counterions in FDA-Approved Pharmaceutical Salts.

Authors:  Sonali S Bharate
Journal:  Pharm Res       Date:  2021-07-23       Impact factor: 4.200

Review 8.  Drug Design for CNS Diseases: Polypharmacological Profiling of Compounds Using Cheminformatic, 3D-QSAR and Virtual Screening Methodologies.

Authors:  Katarina Nikolic; Lazaros Mavridis; Teodora Djikic; Jelica Vucicevic; Danica Agbaba; Kemal Yelekci; John B O Mitchell
Journal:  Front Neurosci       Date:  2016-06-10       Impact factor: 4.677

9.  A perspective on multi-target drug discovery and design for complex diseases.

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  9 in total

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