Synthesis and Pharmacology of 3-Isoxazolol Amino Acids as Selective Antagonists at Group I Metabotropic Glutamic Acid Receptors

2001 ◽  
Vol 44 (7) ◽  
pp. 1051-1059 ◽  
Author(s):  
Ulf Madsen ◽  
Hans Bräuner-Osborne ◽  
Karla Frydenvang ◽  
Lise Hvene ◽  
Tommy N. Johansen ◽  
...  

ChemInform ◽  
2010 ◽  
Vol 32 (27) ◽  
pp. no-no
Author(s):  
Ulf Madsen ◽  
Hans Braeuner-Osborne ◽  
Karla Frydenvang ◽  
Lise Hvene ◽  
Tommy N. Johansen ◽  
...  


2019 ◽  
pp. 63-68
Author(s):  
T. V. Zavalskaya ◽  
V. V. Bogdan

The patients with unstable angina (UA) were examined using the method of ion exchange liquid-column chromatography. The content of the substitutable amino acids (AA) in blood serum was determined: ornithine, taurine, aspartic acid, serine, glutamic acid, proline, glycine, alanine, cysteine, tyrosine, glutamine. The patients were divided into two groups: І – 37 people who received cardicet, bisoprolol, atoris, enap, acetylsalicylic acid, clopidogrel; ІІ – 38 people, the therapy of which, in addition to the mentioned drugs, included L-arginine (100 ml intravenous for 10 days). The results of the study indicate a different dynamics of changes in the level of substitute AK in serum in patients with NA, who received anti-anginal therapy and anti-anginal therapy with L-arginine. Attention is drawn to the fact that in patients with Group I after treatment, the total amount of replacement AA significantly decreased in comparison with the II group in 1,2 times, but remained unchanged compared with the indicator before treatment. In patients of the ІІ group, the total amount of substitute AK in serum is significantly reduced in comparison with kontrol group in 1.4 times, and compared with the indicator before treatment – in 1.2 times. That is, the inclusion of L-arginine in anti-anginal therapy promotes the enhancement of their intracellular metabolism in conditions of coronary circulatory destabilization. In patients with UA, antianginal therapy which included L-arginine, there was a normalization of such alternating AAs as ornithine, taurine and glycine, which can be considered as compensatory, protective reactions in myocardial ischemia. Thus, L-arginine effectively affects the balance of substitute AA blood plasma in patients with UA.



2002 ◽  
Vol 45 (4) ◽  
pp. 988-991 ◽  
Author(s):  
Hasse Kromann ◽  
Frank A. Sløk ◽  
Tine B. Stensbøl ◽  
Hans Bräuner-Osborne ◽  
Ulf Madsen ◽  
...  




ChemInform ◽  
2010 ◽  
Vol 25 (40) ◽  
pp. no-no
Author(s):  
S. TAKANO ◽  
T. KAMIKUBO ◽  
M. MORIYA ◽  
K. OGASAWARA
Keyword(s):  


1964 ◽  
Vol 42 (1) ◽  
pp. 139-142 ◽  
Author(s):  
S. J. Patrick ◽  
L. C. Stewart

The effects of hypoglycin A on the metabolism of L-leucine-C14, L-alanine-C14, and L-glutamic-acid-C14 by rat liver slices have been investigated. Hypoglycin exerted markedly inhibitory effects on the conversion of leucine-C14 to fatty acid, cholesterol, and CO2. Conversion of alanine-C14 and glutamic acid-C14 to fatty acids was also inhibited by hypoglycin. No effects of hypoglycin on the conversion of C14-amino acids into protein or glycogen were demonstrated.



1966 ◽  
Vol 101 (3) ◽  
pp. 591-597 ◽  
Author(s):  
R M O'Neal ◽  
R E Koeppe ◽  
E I Williams

1. Free glutamic acid, aspartic acid, glutamic acid from glutamine and, in some instances, the glutamic acid from glutathione and the aspartic acid from N-acetyl-aspartic acid were isolated from the brains of sheep and assayed for radioactivity after intravenous injection of [2-(14)C]glucose, [1-(14)C]acetate, [1-(14)C]butyrate or [2-(14)C]propionate. These brain components were also isolated and analysed from rats that had been given [2-(14)C]propionate. The results indicate that, as in rat brain, glucose is by far the best precursor of the free amino acids of sheep brain. 2. Degradation of the glutamate of brain yielded labelling patterns consistent with the proposal that the major route of pyruvate metabolism in brain is via acetyl-CoA, and that the short-chain fatty acids enter the brain without prior metabolism by other tissue and are metabolized in brain via the tricarboxylic acid cycle. 3. When labelled glucose was used as a precursor, glutamate always had a higher specific activity than glutamine; when labelled fatty acids were used, the reverse was true. These findings add support and complexity to the concept of the metabolic; compartmentation' of the free amino acids of brain. 4. The results from experiments with labelled propionate strongly suggest that brain metabolizes propionate via succinate and that this metabolic route may be a limited but important source of dicarboxylic acids in the brain.





1990 ◽  
Vol 258 (6) ◽  
pp. E907-E917 ◽  
Author(s):  
M. Frexes-Steed ◽  
M. L. Warner ◽  
N. Bulus ◽  
P. Flakoll ◽  
N. N. Abumrad

This study examines the independent effects of insulin and amino acids on protein metabolism after a 12-h and 4-day fast in healthy volunteers. Leucine (Leu) kinetics were examined during sequential insulin infusions of 0 (group I) or 0.0125 (groups II and III), 1.2, and 10 mU.kg-1.min-1. Plasma Leu was maintained at 12-h fasted levels in groups I and II and at 84-h fasted levels in group III. Four-day fast (vs. 1 day, P less than 0.01) was associated with a 79% drop in plasma insulin and elevations in plasma Leu (122%), Leu rates of appearance (Ra) (21%), and Leu oxidation (56%), and no change in nonoxidative rates of disappearance (Rd). Insulin resulted in a dose-dependent suppression of endogenous Leu Ra with group III = I greater than II. Leu oxidation rose 1.7-fold in group III at the highest insulin dose but remained stable in the two other groups. In conclusion, 4-day fasting is associated with enhanced proteolysis and Leu oxidation with no change in nonoxidative Rd (protein synthesis). Elevated branched-chain (and other) amino acids were required to restore tissue sensitivity and specificity to the effects of insulin on protein metabolism after 4 days of fasting.



1994 ◽  
Vol 267 (6) ◽  
pp. E877-E885 ◽  
Author(s):  
I. Tauveron ◽  
D. Larbaud ◽  
C. Champredon ◽  
E. Debras ◽  
S. Tesseraud ◽  
...  

The experiment was carried out to clarify the roles of insulin and amino acids on protein synthesis in fed lactating goats (30 days postpartum). Protein synthesis in the liver and various skeletal muscles was assessed after an intravenous injection of a large dose of unlabeled valine containing a tracer dose of L-[2,3,4-3H]valine. The animals were divided into three groups. Group I was infused with insulin (1.7 mumol/min) for 2.5 h under glucose, potassium, and amino acid replacement. Group A was infused with an amino acid mixture to create stable hyperaminoacidemia for 2.5 h. Group C animals were controls. The fractional synthesis rates (FSR) were 31.5 +/- 2.2, 6.5 +/- 0.4, 4.3 +/- 0.8, 4.0 +/- 1.2, 3.9 +/- 1.2, and 3.6 +/- 0.4%/day (SD) in liver, masseter, diaphragm, anconeus, semitendinosus, and longissimus dorsi, respectively, for group C. Neither hyperinsulinemia in group I nor hyperaminoacidemia in group A had not affected by hyperinsulinemia but was stimulated by hyperaminoacidemia (+30%, P < 0.05). In contrast to previous experiments in which a labeled amino acid was constantly infused, this study revealed a stimulating effect of amino acids on protein synthesis in the liver but not in skeletal muscles. As previously observed in studies with the constant-infusion method, insulin had no effect on protein synthesis.



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