Chemistry and pharmacology of nootropics

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Abstract
Nicolaus, B.J.R.: Chemistry and pharmacology of nootropics. Drug Dev. Res. 2: 463–474, 1982.The paper discusses the chemistry and pharmacology of the nootropics, reviewing the new chemical entities to recently emerge and in particular the five‐membered heterocyclic lactams belonging to the pyrrolidinone class, such as piracetam and oxiracetam. These gammalactams are related to the folded conformation of GABA, which seems to play a role in the uptake mechanisms—that is, in the transport of GABA across the membrances into differnt nervous tissue elements. The classification of nootropics is discussed, taking into consideration the six main criteria recently suggested, which are: no direct vasoactivity, no change in basic rhythm of EEG activity, blood brain barrier passage, positive metabolic activity in humans and animals, low incidence of side‐effects, and objective demonstration of clinivicacy. A critical analysis is made of the various pharmacological and biochemical models employed to screen the nootropics, including a new approach based on the impaired learning rate of spontaneously hypertensive rats with cerebrovascular lesions. The activity of the new GABA‐derivative nootropic called oxiracetam is also described and compared with the forerunner of the class, piracetam.