"目录号: HY-13955
Telmisartan 是一种有效的血管紧张素II 1型受体 (angiotensin II type 1 receptor) 拮抗剂，能够抑制其活性，IC50值为 9.2 nM。
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生物活性
Description
Telmisartan is a potent, long lasting antagonist ofangiotensin II type 1 receptor (AT1), selectively inhibiting the binding of125I-AngII to AT1 receptors withIC50of 9.2 nM.
IC50& Target
IC50: 9.2 nM (angiotensin II type 1 receptor)[1]
In Vitro
In intact RVSMC cells and in membrane preparations, telmisartan inhibits the binding of125I-AngII to AT1 receptors in a concentration-dependent manner, with an IC50of 9.2 ± 0.8 nM. In the same experimental conditions, angiotensin II displaces125I-AngII with an IC50value of 2.9 ± 0.5 nM. The specific binding of [3H]telmisartan to SMC membranes is displaced by unlabeled telmisartan with an IC50of 7.7 ± 1.8 nM and by cold AngII with an IC50of 32.7 ± 5.7 nM[1]. Telmisartan treatment (100 μM) reduces the proliferation of three EAC cell lines (OE19, OE33, and SKGT-4), induces cell cycle arrest in G0/G1 phase and regulates cell cycle-related proteins in EAC cells, and induces the phosphorylation of AMPK and regulates cell cycle-related proteins via the AMPK/mTOR pathway in EAC cells. Telmisartan inhibits the activation of RTKs, downstream effectors and cell cycle-related proteins[5].
In Vivo
In the telmisartan (0.1, 0.3, and 1 mg/kg)-treated rats, the specific binding of [3H]telmisartan to the surface of living RVSMC is saturable and increases quickly to reach equilibrium within 1 h. Telmisartan dissociates very slowly from the receptor with a dissociation half-life (t1/2) of 75 min, which is comparable with candesartan and almost 5 times slower than angiotensin II (AngII). In vivo, telmisartan blunts the blood pressure response to exogenous AngII dose dependently[1]. Telmisartan (10 mg/kg/d) administration effectively suppresses aneurysm pathogenesis after PPE infusion as well, regardless of whether treatment is initiated before or after aneurysm creation or continues for a limited or extended time. Telmisartan treatment is associated with reduced messenger RNA levels for CCL5 and matrix metalloproteinases 2 and 9 in aneurysmal aortae, with no apparent effect on PPARγ-regulated gene expression[2]. Telmisartan (1 mg/kg/day) significantly ameliorates neuronal loss and the spatial acquisition impairment in 5XFAD mice, but without any changes of NeuN expression in the hippocampus layer. Telmisartan (1 mg/kg/day) treatment reduces amyloid burden and microglial accumulation in 5XFAD mice brain, induces microglial polarization towards neuroprotective phenotype, but does not alter the expression levels of NEP and IDE in 5XFAD mice specific brain areas[3]. Telmisartan (0.05, 0.1, 1 mg/kg, p.o.) shows significant reduction in immobility time, antagonizes depression and anxiety, and also significantly attenuates serum cortisol, NO, IL-6 and IL-1β in rats[4]. Telmisartan (50 μg, i.p.) leads to a 73.2% reduction in tumor growth in mice bearing xenografts derived from OE19 cells. Furthermore, miRNA expression is significantly altered by telmisartan in vivo[5].
Clinical Trial
Boehringer Ingelheim
Healthy
July 2002
Phase 1
Boehringer Ingelheim
Healthy
July 2002
Phase 1
Boehringer Ingelheim
Hypertension
August 1998
Phase 2
Boehringer Ingelheim
Hypertension
June 1998
Phase 2
Boehringer Ingelheim
Healthy
September 1998
Phase 1
Boehringer Ingelheim
Healthy
July 2002
Phase 1
Boehringer Ingelheim
Healthy
July 2002
Phase 1
Boehringer Ingelheim
Hypertension
August 1998
Phase 2
Boehringer Ingelheim
Hypertension
June 1998
Phase 2
Boehringer Ingelheim
Healthy
September 1998
Phase 1
Chong Kun Dang Pharmaceutical-Asan Medical Center
Healthy Male Volunteers
June 2011
Phase 1
Hackensack University Medical Center
GVHD
June 2015
Bayer
Hypertension
May 2009
Yale University-National Institute of Neurological Disorders and Stroke (NINDS)-South East Asia Research Collaboration with Hawaii-University of California, San Francisco-Walter Reed Army Institute of Research (WRAIR)-University of Hawaii-National Institute of Mental Health (NIMH)
Acute HIV Infection-HIV Infections
August 2014
Phase 1
Boehringer Ingelheim
Healthy
August 2010
Phase 1
Chong Kun Dang Pharmaceutical
Essential Hypertension-Hyperlipidemia
April 2013
Phase 1
University of California, Los Angeles-California HIV/AIDS Research Program
HIV Infection
May 2010
Phase 2
HanAll BioPharma Co., Ltd.
Hypertension
November 2012
Phase 1
University of California, Los Angeles-The Campbell Foundation
Endothelial Dysfunction
August 2012
Phase 2
Nanfang Hospital of Southern Medical University
Nonalcoholic Fatty Liver Disease (NAFLD)
August 2014
Phase 4
Bayer
Hypertension
September 2006
Takeda
Essential Hypertension Complicated by Type 2 Diabetes Mellitus
March 2014
Phase 4
Boehringer Ingelheim
Healthy
May 2006
Phase 1
Aristotle University Of Thessaloniki
Hypertension
December 2010
Phase 4
Dr. Sandra E Black-Alzheimer’s Drug Discovery Foundation-Sunnybrook Health Sciences Centre
Alzheimer's Disease-Hypertension
March 2014
Phase 2
Bayer
Hypertension
January 2010
University of Erlangen-Nürnberg Medical School
Metabolic Syndrome
November 2006
Phase 3
Yuhan Corporation
Dyslipidemia & Hypertension
July 2013
Phase 1
South East Asia Research Collaboration with Hawaii-National Institute of Neurological Disorders and Stroke (NINDS)
Acute HIV Infection-HIV CNS Involvement
January 2015
Phase 2
Ronald L. Dalman, MD-Palo Alto Veterans Institute for Research
Abdominal Aortic Aneurysm
September 2012
Phase 4
Boehringer Ingelheim
Hypertension
May 1999
Phase 4
AIDS Clinical Trials Group-National Institute of Allergy and Infectious Diseases (NIAID)
HIV-1 Infection
January 2014
Phase 2
Chong Kun Dang Pharmaceutical
Hypertension-Hyperlipidemia
February 2014
Phase 1
Boehringer Ingelheim
Hypertension
October 2010
Phase 3
RWTH Aachen University-CTCA-Heidelberg University-Bayer
Arterial Hypertension-Diabetes Mellitus Type 2 IRC or NIR
December 2007
Phase 4
Coordinación de Investigación en Salud, Mexico
Inflammation-End-stage Renal Disease
August 2009
Phase 4
IlDong Pharmaceutical Co Ltd
Essential Hypertension
May 2015
Phase 3
Jeil Pharmaceutical Co., Ltd.
Hypertension-Hyperlipidemia
February 2015
Phase 1
Bayer-Bang & Olufsen Medicom
Hypertension
April 2007
Boehringer Ingelheim
Healthy
September 2008
Phase 1
Postgraduate Institute of Medical Education and Research
Diabetic Nephropathy
February 2007
Phase 3
Novartis Pharmaceuticals-Novartis
Hypertension
July 2009
Phase 2
The Second Affiliated Hospital of Chongqing Medical University
Atrial Fibrillation
May 2007
Phase 4
Boehringer Ingelheim
Hypertension
August 2000
Phase 3
