Use of bimatoprost as TRPA1 channel agonist in drug preparation

A technology of bimatoprost and agonist, applied in the application field of bimatoprost as a TRPA1 channel agonist in the preparation of medicines, can solve problems such as mechanical sensitivity behavior defects, achieve enhanced mechanical sensitivity, and reduce intraocular pressure , The effect of information sensitivity to changes in intraocular pressure

Inactive Publication Date: 2015-10-28
TONGJI HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mutations in the TRPA1 gene lead to deficits in mec...

Method used

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  • Use of bimatoprost as TRPA1 channel agonist in drug preparation
  • Use of bimatoprost as TRPA1 channel agonist in drug preparation
  • Use of bimatoprost as TRPA1 channel agonist in drug preparation

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Experimental program
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Embodiment 1

[0026] 1. Retrograde labeling of Dil neurons

[0027] Receptors or channels exist in both the cell body and the terminal of neurons, so the cell body is usually used instead of the too small terminal for research, and the conclusions drawn on the cell body are also applicable to the terminal. We used Dil injection in the anterior chamber to label the trigeminal neuron cell bodies innervating the inner wall of the anterior chamber in rats instead of nerve endings for research. 3-5 μl fluorescent tracer Dil (2.5 mg / ml) was injected into the anterior chamber of the rat eyes through the glass microelectrode through the cornea. After the injection, the rats were deprived of water for one day and ate normally.

[0028] 2. Immunofluorescence staining of trigeminal ganglion

[0029] On the 3rd day after Dil was injected into the anterior chamber, the rats were anesthetized by intraperitoneal injection of 10% chloral hydrate (4ml / kg), and fixed by perfusion of 4% paraformaldehyde thr...

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Abstract

The invention discloses a use of bimatoprost as a TRPA1 channel agonist in drug preparation. The bimatoprost as a TRPA1 channel agonist can be used in drug preparation, produces treatment effects by action on TRPA1 and is used for treating hearing disorder, adjusting gastrointestinal tract power and expediting child delivery. The bimatoprost as a TRPA1 channel agonist can be used in preparation of an intraocular pressure reduction drug, can produce intraocular pressure reduction effects on TRPA1 as a target point and realizes effective treatment on related diseases. Through activating the TRPA1 channel, the bimatoprost improves mechanical sensitivity of machinery sensitive peripheral branch of trigeminal nerve. The bimatoprost is sensitive for intraocular pressure variation information so that feedback adjustment is promoted and intraocular pressure is reduced.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the application of bimatoprost as a TRPA1 channel agonist in the preparation of medicines. Background technique [0002] Bimatoprost (17-Phenyl-tri-norprostaglandin F 2α -ethyl amide, bimatoprost) Molecular formula: C 25 h 37 NO 4 , molecular weight: 415.57, molecular structure: [0003] [0004] Bimatoprost is a synthetic prostamide F(2α) derivative, which reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor from trabecular meshwork channels and uveoscleral channels, and is considered to have the strongest effect on lowering intraocular pressure. topical antiglaucoma drugs. Bimatoprost is mainly used for patients with open-angle glaucoma (POAG) or ocular hypertension (OHT), with less systemic adverse reactions. Studies have shown that bimatoprost can neither activate FP receptors nor EP receptors, and its mechanism of lowering intraocular pressure may b...

Claims

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Application Information

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IPC IPC(8): A61K31/5575A61P1/14A61P15/04A61P27/02A61P27/16
Inventor 刘海霞凌云胡壮丽孟庆丽方鹏
Owner TONGJI HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI TECH
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