ABSTRACT
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.
Subject(s)
Acetylene/analogs & derivatives , Acetylene/therapeutic use , Amines/therapeutic use , Antiparkinson Agents/therapeutic use , Muscarinic Antagonists/therapeutic use , Acetylene/adverse effects , Acetylene/pharmacology , Amines/adverse effects , Amines/pharmacology , Amines/toxicity , Animals , Antiparkinson Agents/adverse effects , Antiparkinson Agents/pharmacology , Antiparkinson Agents/toxicity , Catalepsy/chemically induced , Catalepsy/drug therapy , Convulsants , Disease Models, Animal , Dose-Response Relationship, Drug , Drug Antagonism , Drug Evaluation, Preclinical , Haloperidol , Heart Rate/drug effects , Lethal Dose 50 , Memory, Short-Term/drug effects , Mice , Muscarinic Antagonists/adverse effects , Muscarinic Antagonists/pharmacology , Muscarinic Antagonists/toxicity , Pentylenetetrazole , Rats , Seizures/chemically induced , Seizures/drug therapyABSTRACT
Experiments were performed on rats to study the dynamics of changes in some parameters characterizing the state of the cholinergic part of the nervous system during the development of convulsions induced by various convulsants. It is concluded that, depending on its concentration in the synaptic space, acetylcholine may contribute to the development of convulsions or to their arrest. These effects of the mediator are probably due to its interaction with muscarine receptors of various localization and type.
Subject(s)
Acetylcholine/physiology , Seizures/etiology , Acetylcholine/analysis , Acetylcholinesterase/analysis , Acetylcholinesterase/drug effects , Animals , Brain/drug effects , Brain/enzymology , Brain/physiology , Brain Chemistry/drug effects , Convulsants , Electric Stimulation , Male , Rats , Receptors, Cholinergic/drug effects , Receptors, Cholinergic/physiology , Seizures/physiopathology , Synapses/drug effects , Synapses/physiologyABSTRACT
It was established in experiments on albino rats that blockade of the muscarinic receptors by various M-cholinolytics reduces the dose of corazol necessary for the development of a convulsive state. Preliminary administration of some cholinopositive agents raises the corazol action threshold. It is suggested on the basis of pharmacological analysis that the role of the cholinergic system in the pathogenesis of corasol-induced convulsive state in rats is mediated by the function of cholinoreceptors related to subtype M4 or M1.
Subject(s)
Convulsants/pharmacology , Pentylenetetrazole/pharmacology , Receptors, Muscarinic/physiology , Seizures/etiology , Animals , Dose-Response Relationship, Drug , Drug Interactions , Linear Models , Muscarinic Antagonists/pharmacology , Rats , Receptors, Muscarinic/drug effects , Time FactorsABSTRACT
Under the conditions of the constancy of the postsynaptic effect of two M-cholinolytics atropine and amizil the relationship between the presynaptic and protective effects of the drugs in DDVF intoxication was studied. The indication of the level of the postsynaptic activity was the suppression by the cholinolytics of tremor reaction in rats induced by the action of arecoline. The presynaptic effect of the drugs was judged by the charge of the "bound" acetylcholine content in the brains of the animals. It was found that when administered in the equieffective by the choline-blocking activity doses, atropine to a greater extent reduced the content of the "bound" acetylcholine which was increased due to the action of DDVF and at the same time it possessed the less pronounced protective activity in intoxication with DDVF than amizil. It is supposed that the removal of the presynaptic suppression of acetylcholine release due to the anticholinesterase substance action deteriorates the prognosis of the course of DDVF intoxication.
