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A kind of application of urea channel protein inhibitor

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

Inactive Publication Date: 2017-10-27
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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  • A kind of application of urea channel protein inhibitor
  • A kind of application of urea channel protein inhibitor
  • A kind of application of urea channel protein inhibitor

Examples

Experimental program
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Effect test

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 the application of urea channel protein inhibitor ubit. Its structural formula is as shown. The present invention screens compounds that inhibit urea channel proteins by using erythrocyte models. The experimental results show that such compounds (such as Ubit) can inhibit the urea channel protein UT-B-mediated red blood cell membrane to urea permeability, and its effect is dose-dependent. Dependence relationship; Ubit has no cytotoxic effect on MDCK cells within the effective dose range, indicating that the effect of Ubit on inhibiting cell permeation of urea has nothing to do with its cytotoxicity; Ubit’s inhibitory effect on urea channel protein UT‑B is gradually enhanced; Ubit The inhibitory effect on UT‑B is reversible; in vivo test results show that UBIC can significantly increase the urine output of rats; reduce the concentration of urea in rat urine; and reduce its osmotic pressure, indicating that UBIC produced urea in vivo Sexual diuretic effect.

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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Patent Type & Authority Patents(China)
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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