[Interaction of opiates and opioid peptides with cerebral mediator systems].
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Acetylcholine↗
Biomedical subjects
K S Raevskiĭ
Publications and source records attributed to K S Raevskiĭ.
[Des-1-tyrosine-gamma-endorphin: an assessment of its neuroleptic properties and effect on dopamine synthesis].
The neuropeptide des-1-tyrosine-gamma-endorphine (DTGE) has been shown to facilitate, similarly to neuroleptics, the extinction of pole-jumping avoidance behavior, to enhance the grasping reflex, and to produce catalepsy. In in vitro experiments, DTGE (10(-4) M) did not change the activity of solubilized rat brain striatal tyrosine hydroxylase. However at the concentration of 10(-4) M and 10(-6) M DTGE has been found to accelerate tyrosine hydroxylation in the striatal synaptosomes. It is suggested that the effect of DTGE on the brain dopamine biosynthesis might be involved in the development of the neuropeptide neuroleptic effect.
Animals↗
[Lithium valproate: its neuropharmacological spectrum and effect on transmitter amino acid content of the brain of rats].
The authors studied lithium valproate synthesized at the Institute of Pharmacology, Academy of Medical Sciences of the USSR, and compared it with sodium valproate (depakin, France). It was discovered that like sodium valproate, lithium valproate has a marked anticonvulsant activity, being also effective in experimental seizures induced by bicucullin, exerts a moderate sedative action (potentiation of sodium thiopental and hexenal anesthesia), and a distinct tranquilizing effect in experimental outward inhibition of the conditioned active avoidance response. At the same time the presence in the molecule of lithium ions led to a change in the neurochemical profile of valproate, manifested by an increase in the rat brain content of GABA and glutamate.
Amino Acids↗
[Neurochemical aspects of the pharmacology of GABAergic substances].
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Aminooxyacetic Acid↗
[Effect of the tetracyclic antidepressants pyrazidol and inkazan on the adrenergic nerve transmission in the rat vas deferens].
The effect of new tetracyclic antidepressants pyrazidol and inkazan on adrenergic neurotransmission in the isolated rat vas deferens was studied by examining vas deferens contractions in response to the transmural electric stimulation of the postganglionic sympathetic nerves and addition of noradrenaline (NA) or BaCl2. Pyrazidol and inkazan were found to be capable to increase vas deferens contractions in response to transmural electric stimulation or addition of NA. When given in high concentrations, these antidepressants inhibit the adrenergic neurotransmission since inkazan possesses low sympatholytic activity and pyrazidol exhibits certain alpha-adrenolytic effect.
Animals↗
[Effect of GABA-ergic substances on the conditioned avoidance reaction in rats].
The effect of GABA-ergic substances on the production and latent period of the conditioned reflex of avoidance in rats has been studied. The inhibitor of GABA-transaminase n-dipropylacetate (depakin) deteriorates the reflex production. Fenibut and amino oxyacetic acid significantly prolong the latent period of the produced conditioned reflex of avoidance. The effect of amino oxyacetic acid on the conditioned reflex is abolished by bicuculline and is likely to be related to the increased brain GABA content.
Animals↗
[A comparative study of the neurochemical profiles of carbidine stereoisomers].
The effects of cis- and trans-isomers of atypical neuroleptic carbidine on the synthesis of dopamine and its autoreceptor regulation in the striatum and nucleus accumbens of rats were examined by blocking decarboxylase of L-aromatic amino acids and interrupting the nerve impulse flow in the dopaminergic neurons. The striatal release and metabolism of dopamine were studied in vitro by employing K(+)-stimulated efflux from isolated striata and in vivo by the microdialysis in freely moving rats. Carbidine trans-isomer, unlike its cis-isomer, was shown to enhance the biosynthesis of dopamine via blockade of presynaptic autoreceptors presumably located on the dopaminergic terminals. The trans-isomer was found to be much more potent by affecting the neurochemical parameters of dopaminergic neurotransmission, which are essential for the drug to produce its antipsychotic effect.
Animals↗
[Effect of azabutyrone and its analogs on catecholamine metabolism in the brains of rats].
The action of the neuroleptic azabutyrone and its analogues on the accumulation and disappearance of 3H-norepinephrine and 3H-dopamine was studied in test on rats by using 3H-thyrosine, a tagged precursor of catecholamines. Azabutyrone is shown to be capable to speed up the dopamine circulation rate, as well as that of norepinephrine in the brain of rats. By comparison with azabutyrone the diazabicyclodekanyl derivative produces a more marked effect on the criculation of amines. A further "weighting" of the diazabicyclic radical and also substitution of chlorine for the fluorine atom in the para-position of the phenyl ring of butyrophenone leads to weakening of this effect.
Animals↗
[The brain dopaminergic systems: receptor heterogeneity, functional role and pharmacological regulation].
Recent advances in molecular neurobiology led to a new understanding on mammalian brain dopaminergic system which play a major role in the regulation of motor, cognitive, emotional, neuroendocrine function as well as in the pathogenesis of several pathological conditions, including neurodegenerative diseases, affective disorders, schizophrenia, drug addiction etc. Functional, biochemical and pharmacological heterogeneity of dopamine receptors, which were divided into D1-like (D1 and D5 subtypes) and D2-like (D2, D3 and D4) families of receptors has been postulated. The article reviews the recent advances including author's own results concerning the structure and function of main dopaminergic brain system, i.e. nigrostriatal and mesolimbic. The problem of autoreceptor regulation of dopaminergic neurotransmission, particularly, the processes of dopamine synthesis, release and metabolism has been specially discussed. An involvement of D2 and D3 dopamine autoreceptors in the control of these processes and differences in the mode of action of typical and atypical neuroleptics demonstrating various affinities to D2 and D3 dopamine receptors are analysed in detail. Dopamine and its metabolites have been determined on freely moving rats using brain microdialysis and high performance liquid chromatography. It is hypothesized that dopamine D3 autoreceptor is preferentially involved in the regulation of dopamine release while D2 one is responsible for the control of dopamine synthesis and metabolism in rat basal ganglia in vivo.
Amino Acid Sequence↗
[The effect of lamotrigine and carbamazepine on the development of the audiogenic seizure reaction in rats of the Krushinskiĭ-Molodkina strain].
The effect of Lamotrigine and carbamazepine on the development and character of the epileptiform seizures after strong sonic stimulation were studied on Krushinskiĭ-Molodkina line of rats. Both drugs manifested a dose-dependent increase in the latency of motor reaction Lamotrigine administration in the dose range of 5-40 mg/kg, i.p., resulted in a moderate decrease in the seizure intensity preventing predominantly the tonic component of the seizure and failed to modify the character of convulsive reaction. Carbamazepine administered in doses of 7.5-30 mg/kg effectively prevented the epileptiform seizures. The "two-wave" motor reaction was observed in 15% of carbamazepine-treated rats.
Acoustic Stimulation↗
[Kinetics of the distribution of azabutyrone in the organism of rats].
Spectrophotometry was employed in enquiring into the pharmacokinetics of azabutyrone in the organs of rats. With its intravenous or peroral administration the drug was found to quickly penetrate the cerebral tissues of rats and to accumulate therein. A direct relation between the dosage, the azabutyrone concentration in the cerebral tissues and the duration of the antiphenamine effect was disclosed. The cataleptic action correlates well with the drug concentration in the brain. No correlation between the level of the drug in the brain and the intensity of thiopental sodium anesthesia is observed.
Animals↗
[Microdialysis study of tolcapone effect during blockage of neuronal dopamine reuptake caused by GBR-12909].
In vivo brain functions analysis was conducted to assess the effect of tolcapone, a novel catechol-O-methyltransferase (COMT) inhibitor on extracellular levels of dopamine (DA) and its metabolites dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in the striatum of awake, freely moving eats during GBR 12909-induced blockade of DA uptake. Tolcapone administration (30 mg/kg, i.p.) failed to change the dopamine output but caused a marked and long-lasting decrease in the extracellular level of HVA and increase in that of DOPAC. In contrast, injection of the DA uptake inhibitor GBR 12909 directly into the striatum (5 microM) or i.p. (20 mg/kg) led to increase in the DA level but had no significant effect on the metabolites. Co-administration of tolcapone (30 mg/kg i.p.) and CBR 12909 (20 mg/kg) increased the DA level further, whereas the changes in HVA and DOPAC levels remained approximately the same as after injection of tolcapone alone. Behavioral observation showed GBR 12909-induced hyperactivity and stereotypy to be potentiated by tolcapone. These findings show that in the rat striatum under conditions of normal nerve activity DA uptake completely inhibits the increase in striatal DA neurotransmission induced by tolcapone (30 mg/kg i.p.) through COMT inhibition.
3,4-Dihydroxyphenylacetic Acid↗
[Brain dopamine receptors: structure, functional role, and modulation by psychotropic substances].
Recent advances in molecular neurobiology led to a new understanding on mammalian brain dopaminergic system which plays a major role in the regulation of motor, cognitive, emotional, neuroendocrine functions as well as in the pathogenesis of several pathological conditions, including neurodegenerative diseases, affective disorders, schizophrenia, drug addiction etc. Functional, biochemical and pharmacological heterogeneity of dopamine receptors, which were divided into D1-like (D1 and D5 subtypes) and D2-like (D2, D3 and D4) families of receptors has been postulated. The article reviews the recent advances including author's own results concerning the structure and function of main dopaminergic brain system, i.e. nigrostriatal and mesolimbic. The problem of autoreceptor regulation of dopaminergic neurotransmission, particularly, the processes of dopamine synthesis, release and metabolism has been specially discussed. An involvement of D2 and D3 dopamine autoreceptors in the control of these processes and differences in the mode of action of typical and atypical neuroleptics demonstrating various affinities to D2 and D3 dopamine receptors are analysed in detail. Dopamine and its metabolites have been determined on freely moving rats using brain microdialysis and high performance liquid chromatography. It is hypothesized that dopamine D3 autoreceptor is preferentially involved in the regulation of dopamine release while D2 one is responsible for the control of dopamine synthesis and metabolism in rat basal ganglia in vivo.
Animals↗
[The seizures induced by N-methyl-D,L-aspartate administration are accompanied by an enhancement of nitric oxide generation and of lipid peroxidation processes in the rat brain].
EPR-spectrometry was performed to study the nitrous oxide (NO) content and the intensity of lipid peroxidation (LPO) in the brain cortex of rats during convulsions induced by intracerebral injection of N-methyl-D,L-aspartate (NMDLA). It was shown that the convulsions were attended with a fourfold increase in the NO content and activation of LPO in the rat brain cortex. Disocilpin injection fully prevented the development of convulsions as well as increase in the NO level and LPO activation caused by NMDLA injection. N-nitro-L-arginine had an anticonvulsive effect and prevented increase in the NO content but did not cause any noticeable effect on LPO intensity in the brain cortex.
Animals↗
[The effect of carbamazepine on the content of monoamines and their metabolites in the brain structures of rats with audiogenic epilepsy].
It was shown that the content of serotonin (5-OT) and 5-oxyindoleacetic acid (5-OIAA) in the temporal cortex, hippocampus and medulla oblongata and the content of dopamine and 3,4-dihydroxyphenilacetic acid in the striatum are increased initially, while the level of norepinephrine in the striatum is reduced in Krushinskiĭ-Molodkina rats genetically predisposed to audiogenic epilepsy in comparison with Wistar rats. Carbamazepine levelled out the changes in the 5-OT and 5-OIAA levels at the peak of the audiogenic attack in the temporal cortex and hippocampus, causing at the same time a sum increase in the content of all monoamines and their metabolites in the medulla oblongata and striatum.
Acoustic Stimulation↗
[The effect of sodium nitroprusside and lamotrigine on D-[3H]aspartate release from mouse cortex slices].
The work deals with the study of the effect of the nitrous oxide and the antiepileptic agent lamotridgin on nonstimulated and K(+)- and veratridine-stimulated release of D-[3H]aspartate from sections of the brain cortex of mice. Sodium nitroprusside (0.1 mM) intensified nonstimulated (by 38-52%) and K(+)-stimulated (by 86%) release of labeled D-aspartate. Lamotridgin (0.1 mM) inhibited nonstimulated and veratridine-stimulated release of the label (by 50 and 70%, respectively). Sodium nitroprusside completely turned the inhibiting affect of lamotridgin on spontaneous and veratridine-stimulated release of D-aspartate. It is suggested that NMDA-subtype presynaptic receptors contribute to the regulation of D-aspartate release and are modulated by nitrous oxide.
Animals↗