The inhalation convulsants: a pharmacodynamic approach

S. Cohen, A. Goldschmid, G. Shtacher, S. Srebrenik, S. Gitter

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

Abstract

Certain fluorinated ethers, e.g., (CF 3CH 2) 2O, are potent stimulants of the central nervous system. The presence of fluorine in the molecule is not necessarily indicative of this type of activity, since (CF 3) 2CHOCH 3, an isomer, is anesthetic. The authors found that the only reliable experimental parameter that could predict the type of activity in fluorinated ethers is the partial molal volume (v) in a model solvent. Knowledge of v allows derivations of the solubility parameter (δ) and of the partition coefficient that are more dependable than had been hitherto possible. All the inhalation convulsants studied are characterized by low δ values (6.5-7.5) and incur large rates of expansion in molal volume (4-8%) in benzene solution (δ = 9.2). Their stimulatory activity could be ascribed to excess free energy in the biophase large enough to surmount the energetic barrier against the spontaneous influx of Na +, to a preference for accumulating in that phase of a target organ that is compatible with their low δ, or to a combination of these effects.

Original languageEnglish
Pages (from-to)379-385
Number of pages7
JournalMolecular Pharmacology
Volume11
Issue number3
StatePublished - 1975

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