Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4)-Reference-Cited by-同舟云学术

Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4)

Published:2019-09-18 Issue:20 Volume:62 Page:9270-9280
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Brooks Carl A.¹^ORCID,Barton Linda S.¹,Behm David J.¹,Brnardic Edward J.¹^ORCID,Costell Melissa H.¹,Holt Dennis A.¹,Jolivette Larry J.¹,Matthews Jay M.¹,McAtee John J.¹,McCleland Brent W.¹,Patterson Jaclyn R.¹,Pero Joseph E.¹^ORCID,Rivero Ralph A.¹,Roethke Theresa J.¹,Sanchez Robert M.¹,Shenje Raynold¹,Terrell Lamont R.¹,Lawhorn Brian G.¹^ORCID

Affiliation:

1. Heart Failure Discovery Performance Unit and Flexible Discovery Unit, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.9b01247

Reference30 articles.

1. An Orally Active TRPV4 Channel Blocker Prevents and Resolves Pulmonary Edema Induced by Heart Failure

2. Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4

3. Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema

4. Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4)

5. “A Phase I Study to Assess the Pharmacokinetics of GSK2798745 Tablets, A First Time in Human Study to Evaluate the Safety”, “Tolerability, Pharmacokinetics, and Pharmacodynamics of GSK2798745 in Healthy Subjects and Stable Heart Failure Patients”, and “A Study to Evaluate the Effect of the Transient Receptor Potential Vanilloid 4 (TRPV4) Channel Blocker, GSK2798745, on Pulmonary Gas Transfer and Respiration in Patients With Congestive Heart Failure”. NCT02925546, NCT02119260, NCT02497937. https://clinicaltrials.gov/ct2/results?cond=&term=GSK2798745&cntry1=&state1=&recrs.

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