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Application of a urea transporter (UT) inhibitor Youbi

A urea channel protein and inhibitor technology, applied in the field of urea channel protein inhibitors, can solve the problem of no increase in urine osmotic pressure

Inactive Publication Date: 2015-08-12
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

And after 5 days of strictly controlled fluid intake, their urine osmolality did not increase

Method used

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  • Application of a urea transporter (UT) inhibitor Youbi
  • Application of a urea transporter (UT) inhibitor Youbi
  • Application of a urea transporter (UT) inhibitor Youbi

Examples

Experimental program
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Embodiment 1

[0047] Example 1, Screening and Pharmacodynamic Evaluation of UT-B Inhibitors

[0048] 1. Screening test method

[0049] 1) Take blood, put it in a 15ml graduated centrifuge tube (suspended in PBS containing sodium heparin), centrifuge at 3000r / min for 10min, discard the supernatant;

[0050] 2) Add the same amount of PBS as the blood, centrifuge at 3000r / min for 10min, discard the supernatant;

[0051] 3) Dilute red blood cells with hypertonic PBS containing 1.25M acetamide to a cell suspension with a specific volume of 2%;

[0052] 4) The erythrocyte suspension was incubated at room temperature for 2 hours to balance the concentration of acetamide inside and outside the cells, and mixed with a pipette at regular intervals;

[0053] 5) Take 99 μl of the above erythrocyte suspension and place it in each well of a 96-well round-bottom microplate, then add 1 μl of the compound to be tested (such as Ubit), mix well, and incubate at room temperature for 6 minutes (the final conc...

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Abstract

The invention discloses an application of a urea transporter (UT) inhibitor Youbi, of which the structural formula is represented as follows. In the invention, by means of erythrocyte model screening, the compound inhibiting UT is obtained. An experimental result proves that the compounds, such as the Youbi, can inhibit the permeability, induced by the UT-B, of urea through erythrocytes membrane, wherein the effect of the Youbi has a dosage dependent relationship. In an effective dosage range, the Youbi is free of cyto-toxicity on MDCK cells, which proves that the effect of inhibition the permeability of the urea through cells by the Youbi is independent of the cyto-toxicity. The Youbi is gradually enhanced in the inhibition effect on the UT-B and the inhibition effect of the Youbi on the UT-B is reversible. An in-vivo test result proves that the Youbi can significantly increase the urine output of mice, can reduce the concentration of urea in the urine of mice and can reduce the osmotic pressure, so that it is proves that the Youbi has a urea-selective diuretic effect in-vivo.

Description

technical field [0001] The invention relates to the application of urea channel protein inhibitor ubit. Background technique [0002] 1. Current applications and R&D hotspots of diuretics [0003] Diuretics act on the kidneys to increase water excretion. Clinically, it is mainly used to treat edema caused by various reasons, and it can also be used to treat some non-edematous diseases. For example, as a first-line drug, it can be used alone or in combination with other drugs to treat hypertension, reduce the incidence of cardiovascular and cerebrovascular diseases and mortality Rate. Currently, the commonly used diuretics are mainly divided into three categories: high-potency diuretics, moderate-potency diuretics, and low-potency diuretics. High-potency diuretics and moderate-potency diuretics mainly inhibit Na + / K + / 2Cl - common transporter and distal convoluted tubule Na + / Cl - Common transporter, inhibits the reabsorption of NaCl, reduces the urine concentratin...

Claims

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Application Information

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IPC IPC(8): A61K31/517A61K31/5377C07D405/12C07D239/90C07D239/91C07D409/12C07D401/12A61P7/10
Inventor 杨宝学李飞周虹雷天落李敏
Owner PEKING UNIV
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