Biomedical subjects
Publications and source records attributed to A Chodkowska.
In experiments carried out on Albino-Swiss mice we tried to compare some pharmacological properties of standard compound-rubidomycin with its 4 newly synthetized derivatives. DR-16 appeared to be more toxic compound than rubidomycin and DR-19 was found to possess the lowest toxicity.
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In the reaction of 4-phenyl-1,2,4-triazolin-5-one [Ia] and 3,4-diphenyl-1,2,4-triazolin-5-one [Ib] with 1-chloro-2,3-epoksypropane, the respective derivatives of 1-(2,3-epoksypropane)-4-phenyl-1,2,4-triazolin-5-one [IIa] and 1-(2,3-epoksypropane)-3,4-diphenyl-1,2,4-triazolin-5-one [IIb] were obtained. Then these compounds were converted into the corresponding aminoalkanol derivatives of 1,2,4-triazolin-5-one [IIIa, b-VIIIa, b] in reaction with secondary amines. The new compounds affected significantly the central nervous system of mice.
A group of 11 derivatives of chelidonine was obtained by acylations and/or alkylations of the secondary hydroxyl group with the aim of testing their biological activity. This paper focuses on the new derivatives influence on CNS in mice. The highest activity was observed for compounds 2c, 3c and 4, which produced antinociceptive and antiserotoninergic effects, not recorded for the parent alkaloid 1.
The effects of thiophosphoric acid alkaloid derivatives from Chelidonium majus L. (Ukrain, UKSR-222) on the central nervous system (CNS) of mice and rats was studied. Intraperitoneal (ip) administration of Ukrain in doses of 9.5 and 19 mg/kg for mice depressed spontaneous motor activity, decreased body temperature and potentiated the action of hexobarbital. Only in a dose of 19 mg/kg Ukrain produced analgesic action in the hot plate test. It had no protective effect against electroshock or pentetrazol-induced seizures. In rats, ip administration of Ukrain in dose of 14 and 28 mg/kg potentiated the action of amphetamine and apomorphine but had no effect on catalepsy induced by haloperidol. Ukrain used in dose 9.5, 14, 19 and 28 mg/kg antagonized the head twitches induced by 5-HTP and hyperthermia-induced by m-CPP. Biochemical studies indicated that Ukrain did not affect the NA and DA concentrations in the whole rats' brain and did not affect the 5-HT and 5-HIAA concentrations in the whole brain of rats. These findings demonstrate that the central action of Ukrain involves the stimulation of the dopaminergic system and the inhibition of the serotoninergic system.
Six new 5(1H)oxo-2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic ethyl esters bearing an aromatic substituent in position 1 or 2 were obtained. Pharmacological studies on the central action of these derivatives were carried out on mice and rats. The highest activity showed compounds 1 and 2 which produced analgesic effects in mice.
Nifedipine (2.5-10 mg/kg) and verapamil (2.5 and 10 mg/kg) offered some protection against pentylenetetrazol (100 and 130 mg/kg)-induced seizure activity in mice. No protection was provided by diltiazem (1.25-10 mg/kg) in this model of experimental epilepsy. Repeated administration of calcium channel blockers (CCBs) in doses of 5 and 10 mg/kg twice daily for three days resulted in no protective effect against pentylenetetrazol. Regarding electroconvulsions, nifedipine (2.5-10 mg/kg) showed the best anticonvulsive action--for instance, in the dose of 10 mg/kg (60 min--treatment time) it elevated the threshold for electroconvulsions from 7.1 to 10.5 mA. Diltiazem (up to 10 mg/kg) and verapamil (up to 20 mg/kg) were considerably less potent in this respect. After repeated administration, only nifedipine (5-10 mg/kg) retained its protective action against electroconvulsions.
Central pharmacological properties of 38 aminophosphonic acids and their derivatives, mostly newly synthesized, were investigated on mice and rats. Acute toxicity, neurotoxic activity, influence on spontaneous locomotor activity, body temperature, electrogenic and pentetrazol convulsions, on cerebral GABA level were tested. The most active compounds were (in a decreasing order of activity): 2-amino-7-phosphonoheptanoic, 2-amino-5-phosphonovaleric, 2-amino-8-phosphonooctanoic, 2-amino-2-methyl-3-methylphosphonopropionic, and 3-amino-3-hydroxy-5-phosphonovaleric acid.
In the behavioral and biochemical investigations performed on Albino Swiss mice it was found that sanumgerman possessed inhibitory properties on the CNS. The mechanism of this action seems to be connected with depression of central catecholaminergic and a stimulation of central serotoninergic neurons.
In the investigations on male Wistar rats it was demonstrated that histamine (0.05 and 0.5 mg/kg) decreased the serotonin level, without affecting the level of 5-HIAA in the stomach and duodenum. Contrary to this, cimetidine (15, 75 and 150 mg/kg) raised slightly the level of serotonin and decreased the 5-HIAA level in the stomach and duodenum. In the jejunum histamine in the lower dose raised the levels of serotonin and 5-HIAA, and in the higher dose it decreased only the concentration of serotonin. Cimetidine, on the other hand, only in the highest dose increased the serotonin level and decreased significantly the level of 5-HIAA. In the brain a rise of the serotonin level was observed only after histamine. No effects were observed of histamine and cimetidine on the blood serotonin level. Histamine reduced the number of enterochromaffinocytes in the duodenum. These results point to an evident interaction between the histaminergic and the serotoninergic structures in the digestive tract of rats.