Synthesis and biological activity in GPI test of scyliorhinin I and its analogues modified in position 8 by Leu, Sar and Pro residues

1991 ◽  
Vol 56 (9) ◽  
pp. 1957-1962 ◽  
Author(s):  
Krzysztof Rolka ◽  
Gotfryd Kupryszewski ◽  
Piotr Janas ◽  
Jarosław Myszor ◽  
Zbigniew S. Herman
Keyword(s):  
Biological Activity ◽  
Guinea Pig ◽  
Solid Phase ◽  
Phase Method ◽  
Guinea Pig Ileum ◽  
Tachykinin Receptor ◽  
Solid Phase Method ◽  
One Step ◽  
Agonistic Activity ◽  
The Hill

Three analogues of scyliorhinin I with Gly in position 8 substituted with Leu, Sar and Pro residues, were synthesized by the solid-phase method. The agonistic activity was determined on isolated guinea pig ileum. Analogues with Sar and Pro in position 8 appeared to be significantly more active than scyliorhinin I and the analogues with Leu in this position. For all analogues the Hill cooperativity coefficient is much lower than one suggesting that the interaction of these peptides with tachykinin receptor(s) in not a one-step reaction.

Synthesis and biological activity of new metallocenic angiotensin II analogs

1988 ◽  
Vol 53 (11) ◽  
pp. 2914-2919 ◽  
Author(s):  
Pierrette Maes ◽  
Annie Ricouart ◽  
Emmanuel Escher ◽  
André Tartar ◽  
Christian Sergheraert
Keyword(s):  
Amino Acids ◽  
Biological Activity ◽  
Angiotensin Ii ◽  
Solid Phase ◽  
Rabbit Aorta ◽  
Phase Method ◽  
Solid Phase Method

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.

Synthesis and Biological Activity of Agonists for the Neuronal Tachykinin Receptor in Guinea Pig Ileum

1987 ◽  
pp. 144-145
Author(s):  
D. Ron ◽  
R. Laufer ◽  
J. Frey ◽  
C. Gilon ◽  
Z. Selinger ◽  
...  
Keyword(s):  
Biological Activity ◽  
Guinea Pig ◽  
Guinea Pig Ileum ◽  
Tachykinin Receptor

Antagonistic Analogs of Oxytocin with Substituted Phenylalanine or Tyrosine in Position 2

1994 ◽  
Vol 59 (6) ◽  
pp. 1430-1438 ◽  
Author(s):  
Rudolf Ježek ◽  
Miroslava Žertová ◽  
Jiřina Slaninová ◽  
Pavel Majer ◽  
Zdenko Procházka
Keyword(s):  
Amino Acids ◽  
Solid Phase ◽  
Phase Method ◽  
Inhibiting Activity ◽  
Structure Activity ◽  
Low Degree ◽  
Solid Phase Method ◽  
Pressor Activity ◽  
Agonistic Activity

Solid phase method on p-methylbenzhydrylamine resin was used for the synthesis of seven analogs of oxytocin with non-coded amino acids in position 2. [L-Phe(4-Me)2]oxytocin (I), [D-Phe(4-Me)2]oxytocin (II), [L-Phe(2-Me,4-Et)2]oxytocin (III), [D-Phe(2-Me,4-Et)2]oxytocin (IV), [D-Tyr(Me)2]oxytocin (V), [D-Tyr(Et)2]oxytocin (VI) and [L-Tyr(2-Me)2]oxytocin (VII) were synthesized. All analogs with D-stereoisomer of alkyl or alkoxy substituted phenylalanine possess uterus in vitro inhibiting activity. In the case of L-stereoisomers the structure activity relationship is more complicated. As far as the pressor activity is concerned, the analogs have either very low agonistic activity or low degree of antagonism.

Synthesis of Peptides with the Solid Phase Method. II. Octapeptide Analogues of Angiotensin II

1974 ◽  
Vol 52 (2) ◽  
pp. 113-119 ◽  
Author(s):  
W. K. Park ◽  
C. Choi ◽  
F. Rioux ◽  
D. Regoli
Keyword(s):  
Blood Pressure ◽  
Biological Activity ◽  
Angiotensin Ii ◽  
Enzymatic Degradation ◽  
Solid Phase ◽  
Paper Electrophoresis ◽  
Antagonistic Effect ◽  
Phase Method ◽  
Solid Phase Method ◽  
Layer Chromatography

Forty-six analogues of angiotensin II were obtained with the solid-phase method for peptide synthesis. The peptides were purified, using the conventional procedures; homogeneity and purity were established after paper, thin-layer chromatography, paper electrophoresis, amino acid analysis, elemental analysis, and enzymatic degradation by aminopeptidase. The biological activity of all compounds was compared with that of angiotensin II on the blood pressure of anesthetized rats. The same test was used to establish the antagonistic effect of several analogues against angiotensin II.

Synthesis and Structure-Activity Relationship of Scyliorhinin I Analogues Modified in Position 3, 6, 7 and 8

1993 ◽  
Vol 58 (4) ◽  
pp. 918-924 ◽  
Author(s):  
Jolanta Zboinska ◽  
Krzysztof Rolka ◽  
Gotfryd Kupryszewski ◽  
Krzysztof Golba ◽  
Piotr Imiolek ◽  
...  
Keyword(s):  
Substance P ◽  
Solid Phase ◽  
Phase Method ◽  
Structure Activity ◽  
Dependent Activity ◽  
Solid Phase Method ◽  
Agonistic Activity ◽  
Cd Studies ◽  
Relationship Of ◽  
Dose Dependent

Seven analogues of scyliorhinin I modified in positions 3, 6, 7 and 8 were synthesized by the solid-phase method. Their agonistic activity was determined on isolated guinea pig ileum (GPI). Except for the two analogues modified in position 6, all exhibited dose-dependent activity. Analogues with Phe, D-Phe(F) in position 7 and Abu in position 8 appeared significantly more active than scyliorhinin I and substance P, whereas the analogue with NMeLeu in position 8 appeared to be twice as active as the native molecule, but displayed only 12% of the substance P activity. CD studies indicated that the analogues modified in position 8 behaved differently in the surroundings that mimics the biological membranes.

Peculiarities of a solid-phase method for the Al-Fe/SiO2 and Al-Co/SiO2 powder catalysts production

2019 ◽  
pp. 63-68
Author(s):  
V.A. Artyukh ◽  
◽  
V.N. Borsch ◽  
V.S. Yusupov ◽  
S.Ya. Zhuk ◽  
...  
Keyword(s):  
Solid Phase ◽  
Phase Method ◽  
Solid Phase Method ◽  
Sio2 Powder

Synthesis of four new V1 antagonists of arginine-vasopressin (AVP) containing new thioacids at position 1 and their vasoconstrictor activity towards isolated mesenteric arterial vessels of rats

1991 ◽  
Vol 56 (2) ◽  
pp. 491-498 ◽  
Author(s):  
Bernard Lammek ◽  
Izabela Derdowska ◽  
Tomasz M. Wierzba ◽  
Witold Juzwa
Keyword(s):  
Peptide Synthesis ◽  
Arginine Vasopressin ◽  
Solid Phase ◽  
Structural Features ◽  
Phase Method ◽  
Competitive Antagonist ◽  
Vasoconstrictor Effect ◽  
Solid Phase Method

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.

Synthesis of a 21-Residue Fragment of Human Proinsulin by the Polyamide Solid Phase Method

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

scholarly journals Syntheses of two deacetyl-thymosin β4analogs and their anti-inflammatory effect on carrageenin-induced edema in the mouse paw

2001 ◽  
Vol 10 (2) ◽  
pp. 89-92 ◽  
Author(s):  
T. Abiko ◽  
R. Ogawa
Keyword(s):  
Marked Reduction ◽  
Solid Phase ◽  
The Other ◽  
Para Position ◽  
Phase Method ◽  
Antiinflammatory Effect ◽  
Solid Phase Method ◽  
Anti Inflammatory ◽  
Inflammatory Effect

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.

The Gas-Solid-Phase 2,5-Dioxopiperazine Synthesis. Cyclization of Vaporous Dipeptides on Silica Surface

1994 ◽  
Vol 59 (2) ◽  
pp. 461-466 ◽  
Author(s):  
Vladimir A. Basiuk ◽  
Taras Yu. Gromovoy
Keyword(s):  
Silica Surface ◽  
Solid Phase ◽  
Phase Method ◽  
Solid Phase Method

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.

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