Balancing Cardiac Liabilities and PK Properties:Discovery of Triazolopyridine Based Growth Hormone S

来源 :中国上海第七届国际新药发明科技年会 | 被引量 : 0次 | 上传用户:xczsb
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
  The growth hormone secretagogue receptor (GHSR) is a GPCR whose natural ligand is the 28 amino acid peptide ghrelin.Ghrelin agonism of the GHSR in the CNS leads to growth hormone (GH) secretion and increased IGF-1 production in the liver.Orally active Growth Hormone Secretagogues (GHSs) have a potential application for treating frailty in the elderly,osteoporosis,perisurgical or parenteral nutrition.More recent studies have indicated that GHSs may be beneficial in the treatment of cancer cachexia and HIV wasting syndrome.Additionally,new pre-clinical data have demonstrated the potential utility of GHSs for treating multiple GI hypomotility-related disorders.These discoveries have renewed interest in agonists of the GHS receptor.Although the area of growth hormone secretagogue research has been explored for years,only a few compounds were successfully advanced into clinical evaluation.
其他文献
①目的:通过建立"医疗器械查房"制度,提高医疗设备完好率,切实保障临床医疗安全,合理购置设备.②方法:每周一次由器械科科长带领相关人员到各科室沟通医疗设备需求、检查医疗设备运行情况,发现问题,及时解决.③结果:全面提升了工作主动性和设备完好率,提高了工作效率,为设备购置提供更多参考.④结论: "医疗器械查房"制度是提高医疗设备管理工作的有效措施.
本文介绍了医院里几种常见的医疗仪器的非电安全性问题状况,并从特性、危害性及注意点等方面加以讨论。
The formation of the vascular system is an early step in organogenesis that involves the participation of various signalling pathways.Integration of the extracellular signals decoded by their cognate
会议
Breast cancer is a highly heterogeneous disease that includes HER2/NEU+,basal-like and ER+ tumors.The most aggressive subtypes,basal-like and HER2/NEU+,are treated with chemotherapy or chemotherapy pl
会议
Nanoparticles are serving as contrast agents in different biomedical imaging modalities such as magnetic resonance imaging (MRI),computed tomography (CT),ultrasound tomography,positron emission tomogr
会议
The first publication on intravenous immunoglobulin (IVIG) administration for children with immune thrombocytopenia ITP (Imbach et al.,The Lancet 1981; 1:1228-1231) evoked targeted immunomodulation in
会议
Glomerulonephritis (GN) is an important cause of chronic kidney disease and renal failure.Current treatments consist of non-specific immunosuppressive medications which often associate with significan
会议
Obesity and its co-morbidities such as diabetes,coronary heart disease and cancer are a fast growing health threat in today s society.Despite great efforts,pharmacotherapy of obesity has achieved litt
会议
Insulin resistance is a central metabolic defect of type 2 diabetes.As our studies strongly indicate ectopic accumulation of lipids as a primary cause of insulin resistance,we investigated different a
会议
Decline in skeletal muscle mass and function occurs in older men and women.Age-associated loss of muscle increases risk of functional limitations,falls,fractures,loss of independence and poor quality
会议