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PubMedDate not supplied

[Topological similarity of antagonist binding sites in biogenic amine receptors].

The influence of physical and chemical properties of some sites of transmembrane receptor domains on the receptors ability to interact with nonspecific antagonists was investigated mathematically. The properties of sites located in 3rd and 7th transmembrane domains are most likely to explain pharmacological characteristics of the receptors. The possibility of receptor blocking by nonspecific antagonists not by competing with agonists but by influencing the receptor conformation is discussed.

Animals↗
PubMed1999

[Effect of the preparation baliz-2 on the integrative brain activity and biogenic amine metabolism in rats under stress].

Effects of balis-2 on exploratory activity in the open field and elevated plus-maze, attention to sensory stimuli of different modalities, elaboration and retention of conditioned reflexes with food reinforcement, were studied in rats under stress. Prolonged treatment of rats with balis-2 seems to normalise integrative activity and metabolism of serotonine and dopamine in the animal brain.

Animals↗
PubMed2000

Genetic control of biogenic-amine systems in Drosophila under normal and stress conditions.

The contents of octopamine and its precursors (tyrosine and tyramine) were studied in adults of two lines of Drosophila virilis with contrasting stress responses. It was demonstrated that in individuals responding to stress by a hormonal stress reaction (line 101), the contents of octopamine and tyrosine are lower than in nonresponding flies (line 147). It was found that there is no difference between the lines in the level of tyramine under normal conditions. The dopamine response to stressor was also studied. Genetic analysis of these differences revealed that they are controlled by a single gene and that the gene is not sex-linked. The gene controlling the response was found to be linked to chromosome 6 of D. virilis.

Animals↗
PubMed2000

Effect of MAO inhibitors on the high-affinity reuptake of biogenic amines in rat subcortical regions.

The noradrenaline (NA), dopamine (DA) and serotonin (5HT) reuptake inhibitory potency of deprenyl, the highly selective and irreversible inhibitor of MAO-B, methamphetamine enantiomers, and some other MAO inhibitors (clorgyline, J-508, J-511, J-512, J-516, LK-63, U-1424, 2-HxMP) was compared. In vitro hypothalamic NA reuptake was inhibited by (+)-, and (-)-methamphetamine, (+)- J-508 and (+)-deprenyl (IC50: 0.35, 3.5, 17.0 and 17.8 mumol/l, respectively), and U-1424, J-512, J-516, LK-63 and 2-Hx-MP showed IC50 > 1000 mumol/l. Striatal DA reuptake was inhibited by (+)-, and (-)-methamphetamine, (+)-, and (-)-deprenyl and clorgyline with IC50 of 0.6, 42.0, 24.0, 98.6 and 27.0 mumol/l, respectively, however the other compounds were ineffective. Hippocampal 5HT reuptake was slightly inhibited by clorgyline (IC50 205.0 mumol/l), while the other MAO-inhibitors were devoid of potency. Data suggest that potency and selectivity of MAO inhibition and reuptake inhibition are independent features of the compounds, and metabolism of deprenyl results in increased noradrenaline and dopamine reuptake inhibition.

Animals↗
PubMedDate not supplied

The effects of neurohormones and biogenic amines on contractile reactivity of the rabbit spleen in vitro.

The effects of adrenaline, noradrenaline, isoproterenol, Alupent, histamine, acetylcholine and serotonin on the isolated rabbit spleen were studied in vitro. The myographic method of recording was used. It was found that all these substances with the exception of Alupent evoked contraction of the rabbit spleen. The contractile response of the spleen was greatest after adrenaline, insignificantly smaller after noradrenaline, very small after isoproterenol and absent after Alupent. A still smaller response was observed after histamine, acetylcholine and serotonin.

Acetylcholine↗
PubMed2001

[Effect of synthetic cationic peptides on activation of the adenylyl cyclase signaling system by biogenic amines in muscle tissue of molluscs and rats].

The hormone-sensitive adenylyl cyclase signaling system (ACS), made of serpentine receptor, heterotrimeric G-protein and enzyme adenylyl cyclase (AC), regulates a wide spectrum of growth and metabolic processes in the cell. Molecular mechanisms of functional coupling of ACS components still remain obscure. We examined the influence of synthetic cationic peptides Ac-Ala-His(Ala)2-His-Ala-NH2 (I), Ac-Ala-His-(Ala)3-His-(Ala)2-His-Ala-NH2 (II), and Ac-(Pro)2-His-(Ala)2-His-(Ala)3-His-(Ala)2-His-Ala-NH2 (III) on the basal AC activity and that stimulated by nonhormonal (NaF) and hormonal reagents (serotonin--molluscs, beta-isoproterenol--rats) in smooth muscles of the freshwater bivalve molluscs Anodonta cygnea and in skeletal muscles of rats. Peptides II and III (the latter more effective) were shown to decrease hormone-stimulated AC activity in both tissues, in a dose-dependent manner. Peptide III strongly reduced NaF stimulating effect to AC, which suggests the involvement of this peptide in the functional coupling of both receptors with G-proteins, and of G-proteins with AC. A correlation was found between the efficacy of peptide action on the functional activity of ACS components and peptide length. As shown by IR-spectroscopy, in water all peptides can form helical structures. However, alpha-helicity of peptides I and II was higher than that of peptide III, which does not conform to a power series in efficacy of these peptides. Thus, it is the length of cationic peptides that plays a key role in hormonal regulation of the functional activity of ACS, especially on the step of receptor-G-protein coupling.

Adenylyl Cyclases↗
PubMed1975

Central action of drugs acting on the cholinergic muscarinic receptor. III. Influence of atropine and scopolamine injected intraventricularly on behavior and levels of biogenic amines in the rat brain.

Atropine (At) and scopolamine (Sc) in low doses intensify basic activity, increase amphetamine stereotypy, and suppress catalepsy induced by injection of haloperidol. High doses lower body temperature, antagonize amphetamine stereotypy, and intensify the hypnotic action of chloral hydrate. Doses of about 1/2 LD50 induce narcotic sleep. Both At and Sc in a wide range of dosage protect against the tonic phase of convulsions produced by electroshock. Sc depresses content of acetylcholine in the brain proportionally to its dosage; At had a similar effect only at the lower of the two doses that were used. Both compounds had no effect on levels of noradrenaline and dopamine in the brain. The results indicate that low doses of blockers of the cholinergic muscarinic receptor, injected intraventricularly, produce strong central stimulation, whereas high doses produce depression of the central nervous system.

Acetylcholine↗