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Pikamilon-a new vasoactive and nootropic preparation (1989)

Pikamilon-a new vasoactive and nootropic preparation (1989)

  1. Calliope
    Pharmaceutical Chemistry Journal, 1989, Vol.23(2), pp.182-186

    Kruglikova-L'vova, R. ; Kovler, M. ; Mirzoyan, R. ; Burov, Yu. ; Gan'shina, T. ; Kopelevich, V. ; Avakumov, V. ; Gunar, V.
    Drugs normalizing the GABA system consist mainly of substances activating GABA receptors, inhibiting GABA utilization, or increasing the permeability of the blood-brain barrier (BBB) to GABA. One way of creating preparations of this kind which are being developed at the "Vitaminy" Scientific-Industrial Association is to use substances that are carriers of the GABA molecule, including vitamins or their derivatives and, in particular, nicotinic acid [9, I0, 12]. Nicotinic acid has been chosen as the carrier because of its valuable pharmacological properties, its low toxicity, and its high biological availability. It has therefore been suggested that a combination of nicotinic acid and GABA in the same molecule would potentiate the action of each component. Compound nicotinoyl-~-aminobutyric acid was first synthesized at the All-Union Vitamin Research Institute in 1970 [ii], and in the subsequent years the product pikamilon, created on its basis, has been widely studied both experimentally and clinically. Pikamilon, a sodium salt of N-nicotinoyl-~-aminobutyric acid, is a white crystalline odorless and hygroscopic powder, readily soluble in water. It was shown when the research had only begun that the compound passes rapidly through the BBB. The essential role of GABA in the central and peripheral regulation of the cerebral circulation [4, 14, 15, 17] and also the presence of a nicotinic acid residue possessing vasoactive properties, determined the priority given to the study of the cerebrovascular properties of pikamilon.