促生长激素释放肽(Pralmorelin Hydrochloride) - 药物靶点：GHSR_在研适应症：生长激素缺乏症_专利_临床

概要

基本信息

药物类型

合成多肽

别名

Pralmorelin、Pralmorelin dihydrochloride、生长激素释放肽-2

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靶点

GHSR

作用机制

GHSR激动剂(促生长激素释放激素受体激动剂)

治疗领域

神经系统疾病内分泌与代谢疾病其他疾病

在研适应症

生长激素缺乏症

非在研适应症-

原研机构

Tulane University Hospital & Clinic

在研机构

Kaken Pharmaceutical Co., Ltd.

非在研机构-

最高研发阶段批准上市

首次获批日期

日本 (2004-10-22),

生长激素缺乏症

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构

分子式C45H55N9O6

InChIKeyHRNLPPBUBKMZMT-RDRUQFPZSA-N

CAS号158861-67-7

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序列信息

Sequence Code 16996358

来源: *****

关联

4

项与促生长激素释放肽相关的临床试验

JPRN-jRCTs021180039 / Recruiting临床3期IIT

The usefulness of DDAVP test and GHRP-2 test in patients with Cushing's disease - Cushing_diagnosis

开始日期2018-05-24

申办/合作机构-

JPRN-UMIN000018891 / RecruitingIIT

The usefulness of DDAVP test and GHRP-2 test in patients with Cushing's disease - The usefulness of DDAVP test and GHRP-2 test in patients with Cushing's disease

开始日期2015-10-01

申办/合作机构-

JPRN-jRCT1080220995 / Unknown statusN/A

Administration study as a part of research toward the influence of growth hormone releasing peptide GHRP-2 on detection of rhGH

开始日期2010-02-05

申办/合作机构-

100 项与促生长激素释放肽相关的临床结果

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100 项与促生长激素释放肽相关的转化医学

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100 项与促生长激素释放肽相关的专利（医药）

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177

项与促生长激素释放肽相关的文献（医药）

2021-03-01·Drug Testing and Analysis2区 · 医学

On the road of dried blood spot sampling for antidoping tests: Detection of GHRP‐2 abuse

2区 · 医学

Article

作者: Reverter‐Branchat, Gemma ; Segura, Jordi ; Pozo, Oscar J.

AbstractDried blood spots (DBSs) sampling is gaining support by the antidoping community because of simplicity and cost‐effective characteristics, especially in collection, transport, and storage. Nevertheless, DBS applicability demands specific studies for each of the analytes proposed for testing. Here, GHRP‐2 has been selected as a representing member of the growth hormone‐releasing peptides (GHRPs) family to provide further evidence of DBS suitability for GHRPs abuse detection in sport testing. An analytical procedure to extract GHRP‐2 and its main metabolite (AA‐3) from DBS and to detect them by liquid chromatography–tandem mass spectrometry (LC–MS/MS) has been developed. The method has been validated for the detection of GHRP‐2. Specificity and identification capabilities have been assessed in agreement with antidoping guidelines. The low AA‐3 levels found in DBS samples prevented its effective application for the determination of this metabolite. The limit of detection (LoD) for GHRP‐2 has been established at 50 pg/ml. Long‐term stability (>2 years) has been confirmed. The procedure has been successfully applied to actual DBS samples from an administration study with a single intravenous dose of GHRP‐2 (100 μg) being detected up to 4 h after drug injection. GHRP‐2 concentrations have been higher in venous blood DBS than in capillary blood DBS. Despite the observed differences, a similar detection window has been achieved independently of the type of blood used.In summary, this study provides specific evidence supporting DBS usefulness to detect GHRP‐2, and potentially other GHRPs family members, for antidoping tests.

2021-02-01·Molecular Diversity3区 · 化学

Identification of potential Mpro inhibitors for the treatment of COVID-19 by using systematic virtual screening approach

3区 · 化学

Article

作者: Teli, Divya M ; Patel, Dushyant V ; Kanhed, Ashish M ; Yadav, Mange Ram ; Patel, Nirav R ; Chhabria, Mahesh T

The Corona virus Disease (COVID-19) is caused because of novel coronavirus (SARS-CoV-2) pathogen detected in China for the first time, and from there it spread across the globe creating a worldwide pandemic of severe respiratory complications. The virus requires structural and non-structural proteins for its multiplication that are produced from polyproteins obtained by translation of its genomic RNA. These polyproteins are converted into structural and non-structural proteins mainly by the main protease (Mpro). A systematic screening of a drug library (having drugs and diagnostic agents which are approved by FDA or other world authorities) and the Asinex BioDesign library was carried out using pharmacophore and sequential conformational precision level filters using the Schrodinger Suite. From the screening of approved drug library, three antiviral agents ritonavir, nelfinavir and saquinavir were predicted to be the most potent Mpro inhibitors. Apart from these pralmorelin, iodixanol and iotrolan were also identified from the systematic screening. As iodixanol and iotrolan carry some limitations, structural modifications in them could lead to stable and safer antiviral agents. Screenings of Asinex BioDesign library resulted in 20 molecules exhibiting promising interactions with the target protein Mpro. They can broadly be categorized into four classes based on the nature of the scaffold, viz. disubstituted pyrazoles, cyclic amides, pyrrolidine-based compounds and miscellaneous derivatives. These could be used as potential molecules or hits for further drug development to obtain clinically useful therapeutic agents for the treatment of COVID-19.

2020-06-01·Analytical and Bioanalytical Chemistry2区 · 化学

Fully automated dried blood spot sample preparation enables the detection of lower molecular mass peptide and non-peptide doping agents by means of LC-HRMS

2区 · 化学

Article

作者: Thevis, Mario ; Thomas, Andreas ; Walpurgis, Katja ; Lange, Tobias

AbstractThe added value of dried blood spot (DBS) samples complementing the information obtained from commonly routine doping control matrices is continuously increasing in sports drug testing. In this project, a robotic-assisted non-destructive hematocrit measurement from dried blood spots by near-infrared spectroscopy followed by a fully automated sample preparation including strong cation exchange solid-phase extraction and evaporation enabled the detection of 46 lower molecular mass (< 2 kDa) peptide and non-peptide drugs and drug candidates by means of LC-HRMS. The target analytes included, amongst others, agonists of the gonadotropin-releasing hormone receptor, the ghrelin receptor, the human growth hormone receptor, and the antidiuretic hormone receptor. Furthermore, several glycine derivatives of growth hormone–releasing peptides (GHRPs), arguably designed to undermine current anti-doping testing approaches, were implemented to the presented detection method. The initial testing assay was validated according to the World Anti-Doping Agency guidelines with estimated LODs between 0.5 and 20 ng/mL. As a proof of concept, authentic post-administration specimens containing GHRP-2 and GHRP-6 were successfully analyzed. Furthermore, DBS obtained from a sampling device operating with microneedles for blood collection from the upper arm were analyzed and the matrix was cross-validated for selected parameters. The introduction of the hematocrit measurement method can be of great value for doping analysis as it allows for quantitative DBS applications by managing the well-recognized “hematocrit effect.”

100 项与促生长激素释放肽相关的药物交易

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