盐酸苯环壬酯(L-Phencynonate Hydrochloride) - 药物靶点：mAChRs_在研适应症：晕动病，缺血性卒中，脑梗塞_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(L)-phencynonate、(L)-phencynonate hydrochloride、L-LPC

+ [12]

靶点

mAChRs

作用方式

拮抗剂

作用机制

mAChRs拮抗剂(毒蕈碱型乙酰胆碱受体家族拮抗剂)

治疗领域

其他疾病神经系统疾病心血管疾病+ [1]

在研适应症

晕动病缺血性卒中脑梗塞+ [1]

非在研适应症-

原研机构

在研机构

非在研机构

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)批准上市

特殊审评特殊审批 (中国)

登录后查看时间轴

结构/序列

分子式C22H31NO3

InChIKeyROZOEEGFKDFEFP-JLPZCGHASA-N

CAS号230313-75-4

查看全部结构式(2)

关联

6

项与盐酸苯环壬酯相关的临床试验

NCT02241629

/ Completed临床2期

Levo Phencynonate Hydrochloridefor the Prevention of Motion Sickness (Seasickness): a Randomized, Double-blind, Placebo Controlled, Multicenter,PhaseⅡClinical Study

A double-blind, randomized, placebo controlled, multicenter, dose-finding phaseⅡclinical superiority study.

开始日期2014-08-01

申办/合作机构

四環醫藥控股集團有限公司

CTR20140259

/ Completed临床3期IIT

左旋盐酸苯环壬酯片预防晕动病（晕车）的随机、双盲、安慰剂和阳性药平行对照、多中心Ⅲ期临床试验

以安慰剂和盐酸苯环壬酯片为对照，进一步评价左旋盐酸苯环壬酯片预防晕动病（晕车）的有效性和安全性。

开始日期2014-03-29

申办/合作机构

军事医学科学院毒物药物研究所

NCT02299804

/ Completed临床2期

A Multicenter, Double-Blind, Phase Ⅱ Clinical Trial To Evaluate Efficacy And Safety Of Levophencynonate Hydrochloride In Patient With Vertigo Caused By Posterior Circulation Infarction

A Multicenter, Double-Blind, Placebo Controlled, Phase Ⅱa clinical trial to enroll 120 patients with Vertigo Caused By Posterior Circulation Infarction during 7 days, then to evaluate the efficacy of different dose of Levophencynonate Hydrochloric, and provide the effective dosage for phase IIb clinical study, to study the safety of Levophencynonate Hydrochloric.

开始日期2014-01-01

申办/合作机构

四環醫藥控股集團有限公司

100 项与盐酸苯环壬酯相关的临床结果

登录后查看更多信息

100 项与盐酸苯环壬酯相关的转化医学

登录后查看更多信息

100 项与盐酸苯环壬酯相关的专利（医药）

登录后查看更多信息

23

项与盐酸苯环壬酯相关的文献（医药）

2024-05-01·Chirality

The stereoselective pharmacokinetics of the desmethyl‐phencynonate hydrochloride in beagle dogs

Article

作者: Wang, Xiaoying ; Zhang, Zhenqing ; Xiong, Shan ; Yin, Lan ; Sun, Junying ; Li, Yuexin ; Li, Jinglai

AbstractThe aim of this study was to investigate the chiral inversion and the stereoselective pharmacokinetic profiles of desmethyl‐phencynonate hydrochloride after administration of the single isomer and its racemate to beagle dogs. A liquid chromatography with tandem mass spectrometry (LC–MS/MS) method was established for determination of the stereoisomers on chiral columns in beagle dog plasma, which met all the requirements. The chiral inversion in dogs of the desmethyl‐phencynonate hydrochloride were studied after administration of the single isomer or the racemic modification. The stereoselective pharmacokinetic profiles of the desmethyl‐phencynonate hydrochloride were studied by assays for simultaneous isomers after administration of the racemic modification. The results showed that the absorption of the Rconfiguration dosed as the single isomer was higher than it dosed as the racemic modification. The AUC(0‐t), AUC(0‐∞), and Cmax of the Sconfiguration were much higher than those of Rconfiguration after oral administration of the racemic desmethyl‐phencynonate hydrochloride. The chiral inversion of desmethyl‐phencynonate isomers could not occur in dogs after administration of the Rconfiguration.

2021-12-01·Behavioural Pharmacology4区 · 心理学

Phencynonate hydrochloride exerts antidepressant effects by regulating the dendritic spine density and altering glutamate receptor expression

4区 · 心理学

Article

作者: Zhang, Jing ; Fang, Jie ; Qiao, Hui ; An, Shucheng ; Xu, Chang ; Qu, Yishan ; Hou, Jun ; Shen, Jingxuan ; Zhu, Yingqi ; Huang, Minyi

Phencynonate hydrochloride (PCH) is a drug that crosses the blood–brain barrier. Cellular experiments confirmed that PCH protects against glutamate toxicity and causes only weak central inhibition and limited side effects. As shown in our previous studies, PCH alleviates depression-like behaviours induced by chronic unpredictable mild stress (CUMS). Here we administered PCH at three different doses (4, 8 and 16 mg/kg) to male rats for two continuous days after CUMS and conducted behavioural tests to assess the dose-dependent antidepressant effects of PCH and its effects on the neuroplasticity in the hippocampus and medial prefrontal cortex (mPFC). Meanwhile, we measured the spine density and expression of related proteins to illustrate the mechanism of PCH. PCH treatment (8 mg/kg) significantly alleviated depression-like behaviours induced by CUMS. All doses of PCH treatment reversed the spine loss in prelimbic and CA3 regions induced by CUMS. Kalirin-7 expression was decreased in the hippocampus and mPFC of the CUMS group. The expression of the NR1 and NR2B subunits in the hippocampus, and NR2B in mPFC are increased by CUMS. PCH treatment (8 and 16 mg/kg) reversed all of these changes of Kalirin-7 in PFC and hippocampus, as well as NR1 and NR2B expression in the hippocampus. PCH is expected to be developed as a new type of rapid antidepressant. Its antidepressant effect may be closely related to the modulation of dendritic spine density in the prelimbic and CA3 regions and the regulation of Kalilin-7 and N-methyl-D-aspartic acid receptor levels in the hippocampus.

2017-05-01·Biomedical Chromatography4区 · 医学

A rapid and efficient analytical method for the quantification of a novel anticholinergic compound, R‐phencynonate, by stable isotope‐dilution LC–MS/MS and its application to bioavailability and dose proportionality studies

4区 · 医学

Article

作者: Wang, Xiaoying ; Li, Jinglai ; Zhang, Wenpeng ; Liao, Sha ; Liu, Qian ; Li, Zheng ; Yang, Cuiping ; Zhong, Bohua ; Luo, Huan ; Zhang, Tianhong ; Song, Xinyi ; Meng, Fei ; Zhang, Zhenqing ; Wang, Juan

AbstractA rapid, specific and high‐throughput stable isotope‐dilution LC–MS/MS method was developed and validated with high sensitivity for the quantification of R‐phencynonate (a eutomer of phencynonate racemate) in rat and dog plasma. Plasma samples were deproteinized using acetonitrile and then separated on a C8 column with an isocratic mobile phase containing acetonitrile–water–formic acid mixture (60:40:0.1, v/v/v) at a flow rate of 0.2 mL/min. Each sample had a total run time of 3 min. Quantification was performed using triple quadrupole mass spectrometry in selected reaction monitoring mode with positive electrospray ionization. The method was shown to be highly linear (r2 > 0.99) and to have a wide dynamic range (0.1–100 ng/mL) with favourable accuracy and precision. No matrix effects were observed. The detailed pharmacokinetic profiles of R‐phencynonate at therapeutic doses in rats and dogs were characterized by rapid oral absorption, quick clearance, high volume of distribution and poor absolute bioavailability. R‐Phencynonate lacked dose proportionality over the oral dose range, based on the power model. However, the area under concentration–time curve and the maximum plasma concentration increased linearly in a dose‐dependent manner in both animal models. The absolute bioavailability of R‐phencynonate was 16.6 ± 2.75 and 4.78 ± 1.26% in dogs and rats, respectively.

100 项与盐酸苯环壬酯相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	-	N05CM	DB16011

研发状态

批准上市

10 条最早获批的记录,

登录

后查看更多信息

适应症	国家/地区	公司	日期
晕动病	中国	北京华素制药股份有限公司	-

未上市

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
缺血性卒中	临床2期	中国	北京四环制药有限公司	2016-05-05
缺血性卒中	临床2期	中国	军事医学科学院毒物药物研究所	2016-05-05
脑梗塞	临床2期	中国	军事医学科学院毒物药物研究所	2014-05-07
脑梗塞	临床2期	中国	北京四环制药有限公司	2014-05-07
眩晕	临床2期	中国	军事医学科学院毒物药物研究所	2014-05-07
眩晕	临床2期	中国	北京四环制药有限公司	2014-05-07
脑梗塞	药物发现	中国	中国人民解放军军事科学院军事医学研究院	2014-05-07
眩晕	药物发现	中国	中国人民解放军军事科学院军事医学研究院	2014-05-07
晕动病	药物发现	中国	军事医学科学院毒物药物研究所	2014-03-29