Nootropic drugs

Kristofikova Z, Benesova 0, Tejkalova H. (1992). Changes in high-affinity choline uptake in the hippocampus of old rats after long-term administration of two nootropic drugs (tacrine and Ginkgo biloba extract). Dementia. 3 304-7. 

Petkov VD, Cao Y, Todorov I, Lazarova M, Getova D, Stancheva S, Alova L. (1992). Behavioral effects of stem-leaves extract from Panax ginseng C.A. Meyer. Acta Physiol Pharmacol Bulg. 18(2) 41-48. Petkov VD, Getova D, Mosharrof AH. (1987). A study of nootropic drugs for anti-anxiety action. Acta Physiol Pharmacol Bulg. 13(4) 25-30. 

Petkov VD, Mosharrof AH, Petkov W, Kehayov RA. (1990). Age-reiated differences in memory and in the memory effects of nootropic drugs. Acta Physiol Pharmacol Bulg. 16(2) 28-36. 

Semlitsch HV, Anderer P, Saletu B, Binder GA, Decker KA. (1995). Cognitive psychophysiology in nootropic drug research effects of Ginkgo biloba on event-related potentials (P300) in age-associated memory impairment. Pharmacopsychiatry. 28(4) 134-42. 

CNS stimulants can be classified as Psychomotor stimulants compounds that display a stimulatory effect primarily on brain functions and which activate mental and physical activity of the organism. They are made up of methylxanthines (caffeine, theophylline, pentoxifyllin), amphetamines (dextroamphetamine, methamphetamine), and also methylphenidate and pemoline. Respiratory stimulants or analeptics compounds, which cause certain activations of mental and physical activity of the organism, and primarily excite the vasomotor and respiratory centers of the medulla (doxapram, almitrine).Drwgi that suppress appetite or anorectics drags that activate mental and physical activity of the organism, but primarily accentuate the excitatory center of satiation in the hypothalamus (phentermine, diethylpropion).In order to increase mental capability, nootropics — drugs that increase the functional state of the brain — are sometimes used, the effect of which is associated with blood flow and metabolism of the brain. 

Few results are available from experiments in healthy volunteers involving the use of the older nootropic drugs, such as co-dergocrine mesylate, piracetam or... 

Nootropics induce very weak or no EEG effects at all in single-dose experiments m healthy subjects. A lack of significant effects was also found in sleep polygraphic studies with several nootropic drugs (Maggini et id., 1988 ... 

Rashid, M. H., and Ueda, H. (2002). Nonopioid and neuropathy-specific analgesic action of the nootropic drug nefiracetam in mice. J. Pharmacol. Exp. Ther. 303, 226-231. 

Piracetam is a so-called nootropic drug, one of a class of drugs that affect mental function (1). In healthy volunteers it improves the higher functions of the brain involved in cognitive processes, such as learning and memory. Its mechanisms of action are not known but may include increased cholinergic neurotransmission. 

Moriguchi S, Tanaka T, Narahashi T, Fukunaga K (2013) Novel nootropic drug sunifiram enhances hippocampal synaptic efficacy via glycine-binding site of N-methyl-D-aspartate receptor. Hippocampus 23 942-951... 

Compounds that positively modulate the AMPA receptor have been reviewed [146, 147]. The first reports of AMPA receptor modulators, appearing over 20 years ago, were plant lectins (e.g., concanavalin A) that inhibited rapid non-NMDA receptor desensitization [148]. Shortly after, the nootropic drug 12 (aniracetam) (Fig. 3), which was reported to effect learning and memory, was found to selectively... 

Ito I, Tanabe S, Kohda A et al (1990) Allosteric potentiation of quisqualate receptors by a nootropic drug aniracetam. J Physiol 424 533-543... 

Figure 7. Chromatogram of the resolution of the racemic nootropic drug CGS 16920 (2 g) on the column (5 x 45 cm) packed with tribenzoylcellulose beads with recycling and peak shaving [139].

Dihydroxypyrrolidinones, which can be considered as cyclic GABA derivatives, are potential nootropic drug candidates. All four possible diastereomers 794—797, as shown in Scheme 174, can be prepared from tartaric acid. Treating L-tartaric acid sequentially with acetyl chloride, methyl glycinate, and then acetyl chloride provides in 81% overall yield the C2-symmetric succinimide 790. In order not to reduce the methyl ester, the very mild treatment with sodium borohydride at —40 °C is employed to prepare the cw-hydroxylactam 791 in an 80% isolated yield. Esterification of 791 with trifiuoroacetic anhydride followed by triethylsilane reduction yields to the extent of 79% the pyrrolidinone 792. This is deprotected with sodium methoxide to provide in 97% yield (3i ,45)-3,4-dihydroxy-A -methoxy-carbonylmethyl-2-pyrrolidinone (793). Ammonolysis of 793 affords (3i ,4 S)-3,4-dihydroxy-2-oxopyrrolidine-A -acetamide (794) in 60% yield. Subsequent modifications to 793 allow for the preparation of (35, 4S)-3,4-dihydroxy-2-oxopyrrolidine-A/-acetamide (795), (3R,4R)-3,4-dihydroxy-2-oxopyrrolidine-A -acetamide (796) and (35, 47 )-3,4-dihydroxy-2-oxopyrrolidine-7V-acetamide (797) [234]. 

Five-membered ring lactams also named y-lactams or 2-oxopyrrolidines are present in biologically active naturally occurring products and also found in approved drugs. Compoxmds of the same class derived from N-substituted-y-lactams are known as nootropic drugs such as piracetam 36 or related compoxmds, oxiracetan 37, or pramiracetam 38 (Figure 10). 

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