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A highly selective serotonin 5‑ht 2c Use of receptor agonist way163909

A WAY163909, receptor agonist technology, applied in the drug field of addiction and withdrawal behavior, can solve problems such as inability to activate

Inactive Publication Date: 2017-11-10
ANHUI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

WAY163909 is a newly synthesized highly selective 5-HT 2C Agonist, WAY163909 for 5-HT 2C The affinity inhibition constant for the receptor ( K i = 11 nM), potency (EC50 = 8 nM; E max =90%), for 5-HT 2B Affinity inhibition constant ( K i = 485nM), potency (EC 50 = 185 nM; E max=40%), but WAY163909 cannot activate 5-HT 2A receptor

Method used

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  • A highly selective serotonin 5‑ht <sub>2c</sub> Use of receptor agonist way163909
  • A highly selective serotonin 5‑ht <sub>2c</sub> Use of receptor agonist way163909
  • A highly selective serotonin 5‑ht <sub>2c</sub> Use of receptor agonist way163909

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Embodiment Construction

[0026] In order to better understand the essence of the present invention, the experimental results of WAY163909 antagonizing morphine addiction will be used below to illustrate its medicinal value in opioid addiction and withdrawal response.

[0027] Research methods

[0028] 1.1 Experimental animals 80 SPF-grade Kunming mice, half male and half female, body weight (18-22) g, purchased from the Experimental Animal Center of Anhui Medical University, production license number: SCXK (Anhui) 2011-002, used as experimental animals License number: SYXK (Anhui) 2011-007. Breeding room temperature: (22±2)°C; humidity: (40-70)%; lighting cycle: 12 h light / 12 h dark.

[0029] Drugs and reagents Morphine: Shenyang No. 1 Pharmaceutical Factory, batch number: 080301; WAY163909: Shanghai Xiarui Pharmaceutical Technology Co., Ltd., batch number: 20140112; Naloxone: China Medical System (Hunan) Pharmaceutical Co., Ltd., batch number: 20120209; Clonidine Hydrochloride Tablets: Jiangsu Yuny...

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Abstract

The invention relates to a novel application of a high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909. A molecular formula of the high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909 is C14H18N2, the molecular weight is 214.30600, and the high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909 is white powder and has good water solubility. The invention discloses the application of the high-selectivity 5-hydroxytryptamine 5-HT2C receptor agonist WAY163909 in preparation of medicines for inhibiting addiction and withdrawl reactions of opioid substances such as morphine, or the application in preparation of the medicines for inhibiting the addiction and withdrawl reactions of morphine substances. According to the novel application disclosed by the invention, the latest researches show that WAY163909 (0.5-1.0mg / kg) can be used for significantly reducing the horizontal movement distance, horizontal movement speed and the withdrawal reactions of mice after morphine-dependent mice are subjected to naloxone precipitation. The novel application disclosed by the invention discovers that WAY163909 can be used for rescuing and treating the addiction and withdrawl reactions produced by the opioid substances such as morphine in clinical treatment and can be used for treating the possible recurrences for the first time.

Description

technical field [0001] The invention belongs to the field of drugs for treating addiction and withdrawal behavior of opioids such as morphine, and in particular relates to a highly selective 5-hydroxytryptamine 5-HT 2C Novel use of agonists in the treatment of addiction and withdrawal behaviors from morphine and other opioids. Background technique [0002] Hazards and Mechanisms of Opioid Addiction [0003] The abuse, dependence and addiction of opioids such as morphine and its chemically synthesized derivative heroin have become increasingly serious social problems in my country and many other countries, especially in Southwest Asia, Central Asia, Southeast Europe and North America (WorldDrug Report 2013 , United Nations Office on Drugs and Crime). Drug users in China mainly abuse heroin and other opioids. By the end of 2013, there were a total of 2.475 million registered drug users nationwide, including 1.358 million opioid abusers and 1.084 million synthetic drug abusers...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/551A61P25/36
Inventor 董六一章功良吴县刘欢陶欣荣王亚男江勤
Owner ANHUI MEDICAL UNIV