Abstract
The butyrophenones were discovered in 1957 as a result of a systematic investigation of structure-activity relationships of a series of propiophenones derived from nor-pethidine. At that time, our laboratory was using a simple screening procedure in mice, consisting of measurement of mydriatic activity (MD50) (Jageneau and Janssen, 1956), the hot plate test for analgesic activity (AD50) (Janssen and Eddy, 1960), and observation of gross behavioral effects. With this screening technique, morphinelike analgesics, characterized by MD50/AD50 ratios not significantly different from unity, could easely be distinguished from chlorpromazine-like neuroleptics, characterized by MD50/AD50 ratios considerably greater than unity.
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Janssen, P.A.J., van Bever, W.F.M. (1980). Butyrophenones and Diphenylbutylpiperidines. In: Hoffmeister, F., Stille, G. (eds) Psychotropic Agents. Handbook of Experimental Pharmacology, vol 55 / 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-67538-6_2
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