COMPARATIVE PHARMACOLOGICAL ACTIVITY OF THE VINCANINE ALKALOID AND ITS PIRAZOLINE DERIVATIVE IN A SINGLE ADMINISTRATION Yu.R. Mirzaev, E.M. Ruzimov, T.T. Khamroev, Sh.M. Adizov, B.B. Abduazimov, B.N. Khandamov. S.Yu. Yunusov Institute of the Chemistry of Plant Substances Academy of sciences of the Republic of Uzbekistan st. Mirzo-Ulugbek, 77, 100170 Tashkent e-mail: tolmas4th@mail.ru
From the strychnine-like alkaloid vincanin isolated from the Vinca erecta plant, a
new derivative pirazoline in ICPS was obtained. For the first time, comparative
pharmacological studies have confirmed that vincanin belongs to convulsive agents or
analeptics of the central nervous system, while pirazoline, according to the results of the
studies carried out, can be attributed to psychostimulants.
The purpose of the study.
To study the effect of the vincanine alkaloid and its
pirazoline derivative with a single administration, on the motor and search activity of
experimental animals in an experimental condition.
All the studies were conducted on mongrel laboratory white mice with a body weight
of 20-22 g, which were kept and kept in standard quarantine conditions for 14 days. The
vincanine alkaloid and its pirazoline derivative were with asingle administered orally to
experimental animals in the form of an aqueous solution in doses of 0,1; 1,0 and 10
mg/kg, and distilled water in appropriate volumes to animals of the control group. The
psychopharmacological indications of the substance under study were studied by the
methods of I. Lapin on motor activity and C. Hall on motor and research activity
according to the recommendations given in the guides and literature.
The results obtained and their discussion.
1. The vincanine hydrochloride, increased
of motor activity caused by the action of phenamine at a dose of 7 mg/kg under the skin
of white mice by Lapin by 1,3; 1,4 and 1,6 times, and pirzoline hydrochloride increased
it by 2,21; 2,17 and 1,74 times respectively, compared with the control group. Usually,
using this research method, the central α – adrenoreceptor stimulating effect of
substances is studied against the background of the introduction of a special analyzer of
phenamine. And the results of the preliminary screening study allow us to conclude that
the studied substances showed an effect stimulating these receptors.
2. It was also noticed that the vincanine hydrochloride reduces the motor and
research activity of white mice in all doses in the Hall method “open field” by 1,1-1,24
times and pirazoline hydrochloride increased them by 1,43 times compared to the
control group, respectively and proportionally. This makes it necessary to conduct
studies of the sedative (hypnotic) activity of vincanine hydrochloride and the
psychostimulating activity of pirazoline hydrochloride.
Thus, in the screening studies carried out, it was found that the substance consisting
of the vincanine alkaloid and its pirazoline derivative with a single administration, have
a stimulating effect on the central α – adrenoreceptors. At the same time, with the ”open
field" method, vincanine hydrochloride significantly decreased motor and research
activity, and pirazoline hydrochloride increased more, respectively, compared with the
control group.