生物活性

• 靶点	Angiotensin Receptor IC50:0.26nM

• 描述Candesartan is an angiotensin II receptor antagonist with IC₅₀ of 0.26 nM. In vivo research shows that conducted on 5XFAD mice, 2-months intranasal treatment with candesartan resulted in reduced Aβ deposits and microglial accumulation in the hippocampus but not in the cortex. In vitro, reduced IL-1β levels in 4-hour LPS-stimulated cortical microglia (100 ng/mL) following 2-hour pretreatment with candesartan (10 μM)^[3]. It is a prolonged angiogenic effect, associated with enhanced VEGF-A and VEGF-B expression in vitro and in vivo, in response to a single dose of candesartan treatment^[4].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00863980	Acute Myocardial Infarction ... more >> Angina Pectoris Myocardial Ischemia Acute Coronary Syndrome Hypertension Collapse <<	Not Applicable	Terminated(Principle investiga... more >>tor resigned in 2013) Collapse <<	-	Japan ... more >> Shakaihoken Kobe Central Hospital Kobe, Japan, 651-1145 Akashi Municipal Hospital Kobe, Japan, 673-8501 Kouseikai Takeda Hospital Kyoto, Japan, 600-8558 Aijyukai Dohjin Hospital Kyoto, Japan, 602-0917 Kyoto Second Red Cross Hospital Kyoto, Japan, 602-8026 Kyoto Prefectural University of Medicine Kyoto, Japan, 602-8566 Social Insurance Kyoto Hospital Kyoto, Japan, 603-8151 Kyoto Kojyo Hokenkai Kyoto, Japan, 604-8472 Kyoto City Hospital Kyoto, Japan, 604-8845 Kyoto First Red Cross Hospital Kyoto, Japan, 605-0981 Aiseikai Yamashina Hospital Kyoto, Japan, 607-8086 Tanabe Central Hospital Kyoto, Japan, 610-0334 Rakusai Simizu Hospital Kyoto, Japan, 610-1106 Uji Hospital Kyoto, Japan, 611-0011 Kyoto Yawata Hospital Kyoto, Japan, 614-8114 Seizinkai Simizu Hospital Kyoto, Japan, 615-8237 Saiseikai Kyoto Hospital Kyoto, Japan, 617-0814 Public Yamasiro Hospital Kyoto, Japan, 619-0214 Gakkentoshi Hospital Kyoto, Japan, 619-0238 Fukuchiyama City Hospital Kyoto, Japan, 620-8505 Ayabe City Hospital Kyoto, Japan, 623-0011 Maizuru Red Cross Hospital Kyoto, Japan, 624-0906 National Hospital Organization Maizuru Medical Center Kyoto, Japan, 625-8502 Maizuru Kyosai Hospital Kyoto, Japan, 625-8585 Public Nantan Hospital Kyoto, Japan, 629-0197 Kyoto Prefectural Yosanoumi Hospital Kyoto, Japan, 629-2261 Kumihama Hospital Kyoto, Japan, 629-3403 Sakurakai Takahashi Hospital Kyoto, Japan, 654-0026 Yuuseikai Midorigaoka Hospital Osaka, Japan, 569-1121 Matsushita Memorial Hospital Osaka, Japan, 570-8540 Saiseikai Shiga Hospital Shiga, Japan, 520-3046 Omihachiman Community Medical Center Shiga, Japan, 523-0892 Collapse <<
  NCT00130975	Atrial Fibrillation	Phase 3	Completed	-	Norway ... more >> Ulleval University Hospital Oslo, Norway, 0407 Asker & Baerum Hospital Rud, Norway, 1309 Collapse <<
  NCT00150631	Hypertension	Phase 3	Unknown	December 2014	Denmark ... more >> Karin Skov Aarhus, Denmark, 8000 Collapse <<

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• 参考文献

• [1] Kosugi M, Miyajima A, et al. Angiotensin II type 1 receptor antagonist candesartan as an angiogenic inhibitor in a xenograft model of bladder cancer. Clin Cancer Res. 2006 May 1;12(9):2888-93.

  [2] Ojima M, Inada Y, et al. Candesartan (CV-11974) dissociates slowly from the angiotensin AT1 receptor. Eur J Pharmacol. 1997 Jan 14;319(1):137-46.

  [3] Torika N, Asraf K, Apte RN, Fleisher-Berkovich S. Candesartan ameliorates brain inflammation associated with Alzheimer's disease. CNS Neurosci Ther. 2018 Mar;24(3):231-242. doi: 10.1111/cns.12802. Epub 2018 Jan 24. PMID: 29365370; PMCID: PMC6489976.

  [4] Soliman S, Ishrat T, Pillai A, Somanath PR, Ergul A, El-Remessy AB, Fagan SC. Candesartan induces a prolonged proangiogenic effect and augments endothelium-mediated neuroprotection after oxygen and glucose deprivation: role of vascular endothelial growth factors A and B. J Pharmacol Exp Ther. 2014 Jun;349(3):444-57. doi: 10.1124/jpet.113.212613. Epub 2014 Mar 28. PMID: 24681872; PMCID: PMC4019323.