目录号: HY-14779
GPCR/G Protein-
Riociguat 是一种可口服的可溶性鸟苷酸环化酶(sGC) 刺激剂，常用于治疗肺动脉高压症。
Guanylate Cyclase
相关产品
Lificiguat-Linaclotide-Cinaciguat-BAY 41-2272-Vericiguat-
生物活性
Description
Riociguat is an oral stimulator of soluble guanylate cyclase (sGC), and used in the treatment of pulmonary hypertension.
In Vitro
Riocigua stimulates the recombinant sGC concentration dependently from 0.1 to 100?μM with a two-fold to 73-fold effect by an NO-independent but haem-dependent mechanism[1].?Riociguat inhibits platelet function in washed platelets but not in whole blood, and exerts no direct effects on contractility and relaxation of cardiac myocytes[2].
In Vivo
Riociguat (10 mg/kg/d, p.o.) partially reverses the pulmonary arterial hypertension, the right heart hypertrophy and the structural remodelling of the lung vasculature in chronic treatment of hypoxic mice and MCT-injected rats[1].
Clinical Trial
NCT02915835
Dinesh Khanna, MD, MS-Bayer-University of Michigan
Scleroderma-Digital Ulcers
September 2016
Phase 2
NCT02117791
Bayer
Hypertension, Pulmonary
July 16, 2014
NCT02024386
Richard Moon-Duke University
Hypertension, Pulmonary-Altitude Sickness
January 2014
Phase 4
NCT02633397
Gregory J. Kato, MD-University of Pittsburgh
Sickle Cell Disease
April 11, 2017
Phase 2
NCT02428985
Bayer
Hypertension, Pulmonary
June 29, 2015
NCT02744339
Medical University of Vienna
Hypertension, Pulmonary-Heart Failure With Normal Ejection Fraction
March 2016
Phase 2
NCT02007629
Bayer
Hypertension, Pulmonary
February 2014
Phase 3
NCT02634203
Assistance Publique - Hôpitaux de Paris-Bayer
Chronic Thromboembolic Pulmonary Hypertension
January 2016
NCT00855660
Bayer
Pharmacology, Clinical
March 2009
Phase 1
NCT02625558
University of Cincinnati
Sarcoidosis
April 2015
Phase 4
NCT02562235
Bayer-Merck Sharp & Dohme Corp.
Hypertension, Pulmonary
October 29, 2015
Phase 3
NCT01179334
Bayer
Pulmonary Hypertension
August 2010
Phase 2
NCT01165931
Bayer
Coronary Artery Disease
May 2012
Phase 2
NCT02283762
Bayer
Scleroderma, Systemic
January 15, 2015
Phase 2
NCT02138825
Bayer
Idiopathic Interstitial Pneumonias / Hypertension,Pulmonary
June 4, 2014
Phase 2
NCT02159326
Bayer
Drug Interactions
June 2014
Phase 1
NCT01065051
Bayer
Hypertension, Pulmonary-Ventricular Dysfunction, Left
November 2010
Phase 2
NCT02759419
Bayer
Hypertension, Pulmonary
June 16, 2016
Phase 4
NCT01784562
Bayer
Hypertension, Pulmonary
NCT02092818
Bayer
Hypertension, Pulmonary
May 31, 2014
NCT02891850
Bayer
Pulmonary Arterial Hypertension
January 12, 2017
Phase 4
NCT01065454
Bayer
Hypertension, Pulmonary-Ventricular Dysfunction, Left
April 14, 2010
Phase 2
NCT00640315
Bayer
Hypertension, Pulmonary-Pulmonary Disease, Chronic Obstructive
August 2008
Phase 1
NCT00855465
Bayer
Pulmonary Hypertension
February 2009
Phase 3
NCT02159313
Bayer
Healthy Volunteers
June 2014
Phase 1
NCT02545465
Bayer
Hypertension, Pulmonary
September 15, 2015
NCT01172756
Bayer
Hypertension, Pulmonary-Ventricular Dysfunction, Left
July 2010
Phase 2
NCT00810693
Bayer
Pulmonary Hypertension
December 2008
Phase 3
NCT02170025
Bayer-Merck Sharp & Dohme Corp.
Cystic Fibrosis
September 30, 2014
Phase 2
NCT00910429
Bayer
Pulmonary Hypertension
July 1, 2009
Phase 3
NCT00863681
Bayer
Hypertension, Pulmonary
March 12, 2009
Phase 3
NCT00694850
Bayer
Hypertension, Pulmonary
August 2, 2008
Phase 2
NCT01926847
Bayer
Raynaud Disease
October 2013
Phase 2
NCT00454558
Bayer
Hypertension, Pulmonary
January 2007
Phase 2
NCT00680654
Bayer
Hypertension, Pulmonary
October 2008
Phase 1
NCT02191137
Bayer
Hypertension, Pulmonary
September 2014
Phase 4
NCT02556268
Bayer
HIV-DDI
February 2016
Phase 1
NCT01489488
Bayer
Pharmacology, Clinical
January 2012
Phase 1
NCT03074539
Medical University of Vienna
Chronic Thromboembolic Pulmonary Hypertension-Sleep Disordered Breathing
February 1, 2017
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References
[1].Schermuly RT, et al. Expression and function of soluble guanylate cyclase in pulmonary arterial hypertension. Eur Respir J. 2008 Oct;32(4):881-91.
[2].Schermuly RT, et al. Riociguat for the treatment of pulmonary hypertension. Expert Opin Investig Drugs. 2011 Apr;20(4):567-76.