TY - JOUR
T1 - The inhalation convulsants
T2 - a pharmacodynamic approach
AU - Cohen, S.
AU - Goldschmid, A.
AU - Shtacher, G.
AU - Srebrenik, S.
AU - Gitter, S.
PY - 1975
Y1 - 1975
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0016698605&partnerID=8YFLogxK
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AN - SCOPUS:0016698605
SN - 0026-895X
VL - 11
SP - 379
EP - 385
JO - Molecular Pharmacology
JF - Molecular Pharmacology
IS - 3
ER -