Synthesis of Tritium Labelled [8-Arginine]-vasopressin

1973 ◽  
Vol 51 (12) ◽  
pp. 1910-1914 ◽  
Author(s):  
H. Hutch Holton ◽  
Luis A. Branda ◽  
Barbara M. Ferrier

Ring tritiated phenylalanine has been incorporated into [8-arginine]-vasopressin synthesized by the solid phase method. The peptide produced has levels of biological activities in agreement with those of the highly purified natural hormone.

1991 ◽  
Vol 56 (2) ◽  
pp. 491-498 ◽  
Author(s):  
Bernard Lammek ◽  
Izabela Derdowska ◽  
Tomasz M. Wierzba ◽  
Witold Juzwa

In an attempt to determine some of the structural features in position 1 that account for V1 antagonism, four new analogues of arginine-vasopressin were synthesized and the effect of the modifications on the vasoconstrictor activity was checked using isolated mesenteric arterial vessels of rats. The protected precursors required for these analogues were synthesized by a solid phase method of peptide synthesis. One of the reported analogues, namely [1-(4-mercapto-4-tetrahydrothiopyraneacetic acid)., 2-O-methyltyrosine, 8-arginine]vasopressin appears to be a potent competitive antagonist of the vasoconstrictor effect by AVP.


1989 ◽  
Vol 54 (10) ◽  
pp. 2795-2801 ◽  
Author(s):  
Krysztof Bankowski ◽  
Alexandra Misicka ◽  
Tomislav Barth ◽  
Jiřina Slaninová

Four new analogs of arginine vasopressin containing β-homo-L-amino acid residue were synthesized by the solid-phase method. The introduced modifications yielded the following peptides:[β-homo Phe3]AVP (I), [β-homoPro7]AVP (II), [Cpp1, Tyr(Me)2, β-homoPhe3]AVP (III), and[Cpp1,Tyr(Me)2, β-homoPro7]AVP (IV). Agonistic properties of I and II, as well as antagonistic properties of III and IV were decreased, more pronouncedly with analogs substituted in the position 3.


2019 ◽  
Vol 20 (2) ◽  
pp. 393 ◽  
Author(s):  
Malgorzata Paduszynska ◽  
Magdalena Maciejewska ◽  
Katarzyna Greber ◽  
Wieslaw Sawicki ◽  
Wojciech Kamysz

The widespread use of biomaterials such as contact lenses is associated with the development of biofilm-related infections which are very difficult to manage with standard therapies. The formation of bacterial biofilms on the surface of biomaterials is associated with increased antibiotic resistance. Owing to their promising antimicrobial potential, lipopeptides are being intensively investigated as novel antimicrobials. However, due to the relatively high toxicity exhibited by numerous compounds, a lot of attention is being paid to designing new lipopeptides with optimal biological activities. The principal aim of this study was to evaluate the potential ophthalmic application of lipopeptide (C10)2-KKKK-NH2. This lipopeptide was synthesized according to Fmoc chemistry using the solid-phase method. The antibiofilm activities of the lipopeptide, antibiotics used in ocular infections, and commercially available lens liquids were determined using the broth dilution method on polystyrene 96-well plates and contact lenses. Resazurin was applied as the cell-viability reagent. The effectiveness of the commercially available lens liquids supplemented with the lipopeptide was evaluated using the same method and materials. (C10)2-KKKK-NH2 exhibited stronger anti-biofilm properties compared to those of the tested conventional antimicrobials and showed the ability to enhance the activity of lens liquids at relatively low concentrations (4–32 mg/L). Estimation of the eye irritation potential of the lipopeptide using Toxtree software 2.6.13 suggests that the compound could be safely applied on the human eye. The results of performed experiments encourage further studies on (C10)2-KKKK-NH2 and its potential application in the prophylaxis of contact lens-related eye infections.


Author(s):  
V.A. Artyukh ◽  
◽  
V.N. Borsch ◽  
V.S. Yusupov ◽  
S.Ya. Zhuk ◽  
...  

1988 ◽  
Vol 53 (11) ◽  
pp. 2914-2919 ◽  
Author(s):  
Pierrette Maes ◽  
Annie Ricouart ◽  
Emmanuel Escher ◽  
André Tartar ◽  
Christian Sergheraert

Analogs of angiotensin II in which phenylalanine in position 8 was replaced with cymantrenylalanine or with its triphenylphosphine photosubstitution product were synthesized by the solid-phase method. On rabbit aorta strips, these peptides were found to be pure antagonists of angiotensin II. Their relative affinities are higher than most other analogs substituted in position 8 with bulky amino-acids.


1981 ◽  
Vol 362 (2) ◽  
pp. 833-840 ◽  
Author(s):  
Eric ATHERTON ◽  
Willy HÜBSCHER ◽  
Robert C. SHEPPARD ◽  
Vivienne WOOLLEY

2001 ◽  
Vol 10 (2) ◽  
pp. 89-92 ◽  
Author(s):  
T. Abiko ◽  
R. Ogawa

Two {Met(0)6}deacetyl-thymosin β4analogs containing Phe(4F) or Tyr(Me) at position 12 were synthesized by the manual solid-phase method, and their anti-inflammatory effect on carrageenin-induced edema in the mouse paw was studied. Fluorination of the para-position of Phe12resulted in a marked antiinflammatory effect on carrageenin-induced edema in the mouse paw compared with that of our synthetic {Met(0)6}deacetyl-thymosin β4, but the other analog, {Met(0)6, Tyr(Me)12}deacetyl-thymosin β4, showed a marked reduction of the anti-inflammatory effect.


1994 ◽  
Vol 59 (2) ◽  
pp. 461-466 ◽  
Author(s):  
Vladimir A. Basiuk ◽  
Taras Yu. Gromovoy

The "gas solid-phase" method is used for the preparation of both symmetric and asymmetric 2,5-dioxopiperazines via cyclization of vaporous linear dipeptides in the presence of silica.


2016 ◽  
Vol 680 ◽  
pp. 208-211
Author(s):  
Lian Lian Wu ◽  
Qiang Li ◽  
Dan Yu Jiang ◽  
Jin Feng Xia

In this paper, La0.65Sr0.35MnO3 (LSM) oxide powder with ultrafine structure has been synthesized by self-propagating combustion method. The powders were characterized by X-ray diffraction, scanning electron microscopy and laser size analysis. Compared to the powders prepared by traditional solid-phase method, the grain size of powders prepared by self-propagating combustion method is relatively small and uniform. Starting from ultrafine LSM powders, sensing electrode (SE) for NO2 mixed-potential sensors based on yttria-stablized zirconia (YSZ) was fabricated. As-obtained NO2 sensor displays fast response and high sensitivity (25.4mV/decade). The response values of the sensor have good linear relationship with the logarithm of NO2 concentration varying from 30ppm to 500ppm.Keywords:Self-propagating combustion method; La0.65Sr0.35MnO3; NOx sensor; YSZ


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