Urotensin-II agonists and antagonists

A technology of urotensin and isomers, applied in the field of urotensin-II polypeptide agonists and antagonists, can solve the problem that the receptor is not fully characterized

Inactive Publication Date: 2007-03-14
THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Fish U-II has also been shown to have sphincter activity in mammals, including the rat aorta, but the receptors mediating the activity of these peptides have not been fully characterized

Method used

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  • Urotensin-II agonists and antagonists
  • Urotensin-II agonists and antagonists
  • Urotensin-II agonists and antagonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1: Preparation of Cpa-c[D-Cys-Pal-D-Trp-Lys-Val-Cys)-Cpa-amide

[0050] Step 1: Preparation of Boc-4-chlorophenylalanine-S-methylbenzyl-D-cysteine-3-pyridyl-2-alanine-D-tryptophan-N 8 -Benzyloxycarbonyl-lysine-valine-S-methylbenzyl-cysteine-4-chlorophenylalanine-benzhydrylamine resin.

[0051] Diphenylmethylamine-polystyrene resin (Advanced ChemTech, Inc., Louisville, KY) (1.2g, 0.5mmol) was placed in the reaction vessel Advanced ChemTechpeptide synthesizer (Model 200) in the form of chloride ions, and the following procedures were carried out: Said reaction cycle: (a) methylene chloride; (b) 33% trifluoroacetic acid in methylene chloride (1 minute 2 times, each 25 minutes); (c) methylene chloride; ( d) ethanol; (e) methylene chloride; (f) 10% triethylamine in chloroform.

[0052] Described neutralization resin and Boc-4-chlorophenylalanine and diisopropylcarbodiimide (each 1.5mmole) in methylene chloride 1h, the aminoacid resin of gained is in the above-me...

Embodiment 2

[0056] Example 2: Analysis of U-II Antagonists Using Rat Aortic Ring Dissection

[0057] Male Sprague-Dawley rats (250-350 g) isolated 5-7 days prior to the experiment were sacrificed by decapitation (experiment approved by the Advisory Committee For Animal Resources, Tulane University School of Medicine). The thoracic aorta was dissected, freed from the associated tissue, and cut into approximately 1.5 mm wide rings. Said ring was suspended in 15ml containing high potassium Kreb's solution (9.15g / L potassium chloride, 2.1g / L sodium bicarbonate, 1.0g / L glucose, 0.16g / L monobasic potassium phosphate, 0.14g / L magnesium sulfate (dehydrated), and 0.22 g / L calcium chloride (dihydrated)) in organ baths.

[0058] Optimal tension (0.2 g) was applied to the tissue, and the bath medium was maintained at 37°C and filled with 95% O 2 / 5%CO 2 Mix and bring to a boil. Before fixing the organ bath, the selected preparation was swabbed with a damp cotton wool swab to remove the endothelia...

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Abstract

The present invention features a novel class of cyclic polypeptides that have U-II antagonist and agonist activity. The invention also features methods for treating physiological or psychological conditions characterized by an excess or under expression of Ur4otensin-II.

Description

field of invention [0001] The present invention relates to urotensin-II polypeptide agonists and antagonists and methods of use thereof. Background of the invention [0002] Urotensin-II (U-II) is a cyclic neuropeptide that can effectively affect cardiovascular. Originally isolated from the caudal neurosecretory system of teleosts, the primary structure of U-II has been published in several vertebrates, including various fish species, frogs and humans. Primary structure analysis of various U-II peptides from different species revealed that while the N-terminal region of U-II is highly variable, its C-terminal loop region is highly conserved. In fact, from fish to human, this ring region responsible for U-II biological activity is completely conserved (Coulouran, et al., Proc.Natl.Acad.Sci.USA (physiology), 95:15803-15808 (1998 )). The fact that the biologically active sequence of U-II is still completely conserved under the effect of evolutionary pressure indicates that t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/575A61K38/22A61F9/01A61F9/013
CPCA61F2009/00882A61F9/013A61F2009/00857A61F2009/00859A61F9/00806A61F2009/00846A61F2009/0088A61F9/008A61F2009/00872
Inventor 戴维・H・科伊沃伊切赫・J・罗索夫斯基
Owner THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND
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