Record Display for the EPA National Library Catalog


Main Title Hydrophobicity and Central Nervous System Agents: On the Principle of Minimal Hydrophobicity in Drug Design.
Author Hansch, C. ; Bjoerkroth, J. P. ; Leo., A. ;
CORP Author Pomona Coll., Claremont, CA.;Environmental Research Lab.-Duluth, MN.;Burroughs Wellcome Co., Research Triangle Park, NC.
Publisher c1987
Year Published 1987
Report Number EPA-R-811927 ;EPA-R-809295; EPA/600/J-87/508;
Stock Number PB90-142860
Additional Subjects Central nervous system ; Drugs ; Chemical composition ; Water ; Lethal dosage ; Anesthetics ; Hypnotics and sedatives ; Antihistaminics ; Reprints ; Pharmacokinetics ; Octyl alcohols ; Antidepressive agents
Library Call Number Additional Info Location Last
NTIS  PB90-142860 Some EPA libraries have a fiche copy filed under the call number shown. 07/26/2022
Collation 26p
The problem of getting drugs across the so-called blood-brain barrier has long been under extensive investigation; however, the other side of the problem, that of keeping drugs out of the central nervous system (CNS), has not been studied so intently. The role of lipophilicity has long been recognized as being important in CNS penetration by chemicals, but it is believed that not enough attention has been devoted to just exactly what is meant when it is said that 'a lipophilic drug is needed for CNS penetration.' There are other reasons for making drugs hydrophilic. Hydrophobic drugs, other factors being equal, are more inhibitory of biochemical systems than hydrophilic congeners. The report discusses these problems in terms of the octanol-water (log P) hydrophobic scale.