[Experimental study of the effects of citalopram, olanzapine, and their combinations in tests for antipsychotic, antidepressant and anxiolytic activities of drugs].

The effects of citalopram, olanzapine and their combinations were studied in tests on outbred SHR male mice. The locomotor activity was determined in the open field, the antidepressant effects - in the tail suspension test, the anxiety-like behavior- in the light-dark transition test; in addition, the antidopaminergic effects of drugs and their combination were evaluated using the apomorphine-induced stereotypy. The results indicate that olanzapine inhibits locomotor activity in all behavioral tests, whereas citalopram alone has no significant effect and does not modify the action of olanzapine.

Effect of M2 muscarinic receptor blockade in rats with haloperidol-produced catatonic syndrome.

We studied the functional role of individual subtypes of muscarinic cholinoceptors in the pathogenesis of neuroleptic parkinsonism in rats. Blockade of M4 receptors prevented the development of extrapyramidal disorders, which was abolished by simultaneous blockade of M2 receptors. The data suggest that various subtypes of muscarinic receptors are involved in the regulation of dopamine concentration.

Effect of M4-cholinoceptor blockade on haloperidol-produced catatonic syndrome in rats.

We studied the relationship between the efficiency of muscarinic receptor antagonists in preventing haloperidol-induced catatonia and their activity in tests for the interaction of ligands with various subtypes of muscarinic receptors (M1-M4) in rats. Mathematical modeling showed that affinity of the ligand for M4 receptors positively affects its ability to correct extrapyramidal disorders (catatonic syndrome) produced by haloperidol, while affinity for M2 receptors had a negative effect on this characteristic.

Qualitative assessment of selective blockade of M(4)-cholinoreceptors in the whole organism.

Quantitative assessment of selective blockade of M4-subtype muscarinic receptors was performed by the number of pilocarpine-induced movements of lower jaw in rats. Three antagonists (atropine, cyclodol, and glipin) were used in the experiments. Glipin produced the most potent blockade of M4 receptors in the whole organism compared to other test antagonist.

[Effect of M3-choline receptor blockade on the ability of muscarinic antagonists to prevent catalepsy induced by haloperidol in rats].

A relationship between the indices of efficacy of the muscarinic antagonists in preventing the haloperidol catalepsy and their activity in the tests characterizing the interaction of these ligands with various subtypes of m-cholinoreceptors was studied in rats. A mathematical model was formulated that confirmed the previous conclusion concerning the role of of the m1- and m2-cholinoreceptor blockade in the antiparkinsonian activity of muscarinic antagonists. It was established that blocking of the m3-cholinoreceptors decreases the anticataleptic activity of m-cholinoblockers with respect to haloperidol.

[The evaluation of the specific activity and side effects of the m-cholinergic blocker pentifin compared to other antiparkinson agents].

Experiments on rodents showed that pentifin, a muscarine antagonist belonging to the group of acetylene amines, possesses a pronounced antiparkinsonian activity. Pentifin is superior in the breadth of therapeutic action and tolerance characteristics to the conventional agents used for Parkinson's disease treatment.

[The effect of selective m-cholinopositive substances on the antiparkinson activity of atropine].

The effect of the selectivity of cholinopositive compounds on atropin antiparkinsonian activity was compared in experiments on rats. The selectivity of the effect of two new synthesized cholinopositive compounds of the phenylcarbamate group was evaluated in preliminary experiments. It was determined by means of these compounds that stimulation of m1-cholinoceptors reduces while stimulation of m2-cholinoceptors has no effect on the ability of atropin to prevent haloperidol-induced catalepsy.

[The antiparkinson activity of muscarinic antagonists depending on their selectivity for individual m-cholinoreceptor subtypes].

The dependence between the activity parameters of muscarine antagonists in the prevention of haloperidol catalepsy in rats and those in tests characterizing the interaction of ligands and various subtypes of m-cholinoceptors was studied. It was established by constructing the mathematical dependence that blockade of m1-cholinoceptors increases, while that of m2-cholinoceptors reduces the antiparkinsonian activity of the drugs. The activity of the muscarine antagonist pentiphan in the prevention of haloperidol-induced catalepsy in rats exceeds the activity of such traditional antiparkinsonian drugs as cyclodol and amedin.

[Blakeslea trispora mutants with a disrupted sexual process].

Three groups of Blakeslea trispora (+) and (-) mutants were obtained and their phenotypical characteristics were studied as well as biochemical changes in the course of mating and the ability to synthesize carotenoids when the sexual process of these mutants was disordered. The first group of mutants synthesized carotenoids at the control level, the second group produced them below the control level, and the third group accumulated less than 1% of carotenoids as compared to the control. The difference in the yields of carotenoids among the three groups of mutants in the mated culture is attributed to the presence (or absence) of the ability to synthesize trisporic acids in them.