盐酸曲托喹吩(Trimetoquinol Hydrochloride Hydrate) - 药物靶点：β2-adrenergic receptor_在研适应症：哮喘，支气管炎，尘肺病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Tretoquinol Hydrochloride

+ [2]

靶点

β2-adrenergic receptor

作用机制

β2-adrenergic receptor激动剂(β2-肾上腺素能受体激动剂)

治疗领域

免疫系统疾病感染呼吸系统疾病+ [1]

在研适应症

哮喘支气管炎尘肺病

非在研适应症-

原研机构

Nipro ES Pharma KK

在研机构

Nipro ES Pharma KK

非在研机构-

最高研发阶段批准上市

首次获批日期

日本 (1971-09-09),

哮喘支气管炎尘肺病

最高研发阶段(中国)-

特殊审评-

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结构

分子式C19H23NO5

InChIKeyRGVPOXRFEPSFGH-AWEZNQCLSA-N

CAS号30418-38-3

关联

3

项与盐酸曲托喹吩相关的临床试验

JPRN-JapicCTI-184163 / CompletedN/A

Administration study of preparation containing Trimetoquinol Hydrochloride Hydrate to healthy adults

开始日期2018-10-26

申办/合作机构

LSI Medience Corp.

JPRN-jRCT1080224102 / CompletedN/A

Administration study of preparation containing Trimetoquinol Hydrochloride Hydrate to healthy adults

开始日期2018-10-26

申办/合作机构

LSI Medience Corp.

IRCT201201195623N1 / CompletedN/AIIT

Effects of synbiotic Gaz on fasting plasma glucose and lipid profiles of diabetic subjects

开始日期2010-08-21

申办/合作机构

Qom University of Medical Sciences

100 项与盐酸曲托喹吩相关的临床结果

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100 项与盐酸曲托喹吩相关的转化医学

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100 项与盐酸曲托喹吩相关的专利（医药）

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102

项与盐酸曲托喹吩相关的文献（医药）

2019-11-01·Drug Testing and Analysis2区 · 医学

Analysis of tretoquinol and its metabolites in human urine by liquid chromatography–tandem mass spectrometry

2区 · 医学

Article

作者: Kageyama, Shinji ; Okano, Masato ; Miyamoto, Asami ; Sato, Mitsuhiko

AbstractTretoquinol (trimetoquinol), a β2‐agonist, has been explicitly listed on the World Anti‐Doping Agency Prohibited List 2019 since January 2019; however, it has been distributed as an antiasthmatic on the medical market. This study aimed to develop a liquid chromatography–tandem mass spectrometric method for the quantification of tretoquinol (free form plus glucuronide) in human urine for doping control purposes. An excretion study (n = 6) of tretoquinol hydrochloride hydrate (6 mg) was performed, and urine samples were collected prior to oral administration and during the first 48 h, along with spot urine samples at 7 and 14 days after administration. All the urine samples were analysed using the developed method. The limit of detection for the developed method was 0.03 ng/mL. The inter‐day precision for the target analyte was excellent (2.7% to 9.2%), and the inter‐day accuracy of target analyte was −0.6% to −3.6%. In all subjects, tretoquinol (free form plus glucuronide conjugate) was identified up to 48 h after administration. The maximum concentrations were in the range of 12.4–78.8 ng/mL and the mean concentration was 55.3 ng/mL. The metabolites O‐methylated tretoquinol, tretoquinol sulphate and O‐methylated tretoquinol sulphate could be also identified in human urine after administration. The longest‐lasting urinary metabolite of tretoquinol currently known, O‐methylated tretoquinol, is also likely to be a useful marker in doping controls.

2008-12-01·Journal of Veterinary Pharmacology and Therapeutics3区 · 农林科学

Plasma and urinary concentrations of trimetoquinol by LC‐MS‐MS following intravenous and intra‐tracheal administration to horses with heaves

3区 · 农林科学

Article

作者: N. E. Robinson ; J. May ; A. F. Lehner ; T. Tobin ; C. Hughes ; F. C. Camargo ; F. J. Derksen ; C. Berney ; S. Eberhart ; L. Dirikolu

Trimetoquinol (TMQ) is a very potent and fast acting bronchodilator in horses with heaves. This study assessed the plasma and urinary concentrations of TMQ in horses with heaves following administration via the intravenous (IV, 0.2 μg/kg) and intra‐tracheal (IT, 2 μg/kg) routes. TMQ was administered to six horses affected with heaves (RAO – Recurrent Airway Obstruction, used interchangeably) by the above routes and plasma and urine samples collected and stored at −20 °C until analyzed. Solid Phase Extraction (SPE) of TMQ was followed by highly sensitive ESI(+)‐LC‐MS‐MS (ElectroSpray Ionization, positive mode – Liquid Chromatography – Mass Spectrometry – Mass Spectrometry); with a Limit of Detection (LOD) estimated at 1 pg/mL. Following IV administration, TMQ plasma levels peaked at 1 min at 707 pg/mL, and at 9 min at 306 pg/mL following IT administration. Our results show that TMQ plasma concentrations decline rapidly following IV administration, which is consistent with the fast onset and short duration of TMQ effect that was observed in our previous studies. On the other hand, IT administration showed a very unique plasma concentration pattern. From a regulatory standpoint, the current available TMQ ELISA kit was also used in an attempt to detect TMQ from the plasma and urine samples. We report that the ELISA kit was unable to detect TMQ from any of the samples generated in these studies.

2007-05-01·Equine Veterinary Journal1区 · 农林科学

Trimetoquinol: bronchodilator effects in horses with heaves following aerosolised and oral administration

1区 · 农林科学

Article

作者: N. E. Robinson ; T. Tobin ; S. Baker ; C. Hughes ; A. F. Lehner ; F. J. Derksen ; C. Berney ; F. C. Camargo ; P. Detolve ; S. Eberhart

SummaryReason for performing study: The bronchodilator effects of trimetoquinol (TMQ) have been studied when administered i.v. or intratracheally, but not in an aerosolised form.Objectives: To define the relationship between the therapeutic and adverse responses (therapeutic index) of TMQ when administered as an aerosol or by the oral route.Methods: Increasing doses of TMQ were administered to horses with heaves as an aerosol and by the oral route. Dose ranged 100–1000 μg/horse for aerosolised TMQ and from 6–60 μg/kg bwt for the oral route. Airway and cardiac effects were assessed by measurement of maximal change in pleural pressure (ΔPplmax) and heart rate (HR), respectively. Side effects of sweating, agitation and muscle trembling were scored subjectively. Duration of action of aerosolised (1000 μg/horse) and oral (6–60 μg/kg bwt) TMQ was evaluated over 6 h.Results: Aerosol administration of TMQ caused dose‐dependent bronchodilation but did not change HR or cause other observable side effects. When 1000 μg/horse was administered via aerosol, TMQ produced a 2‐phase bronchodilation; an immediate effect lasting up to 30 min and a second phase between 2 and 4 h. Oral TMQ was therapeutically ineffective.Conclusion: Aerosol administration of TMQ is a safe and effective method of producing bronchodilation in horses.

100 项与盐酸曲托喹吩相关的药物交易

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