Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic.

Action Potentials / drug effects Animals Benzofurans / chemistry Blood Pressure / drug effects Diuretics / chemistry Dogs Half-Life Haplorhini Humans Male Natriuretic Agents / chemistry Piperazines / chemistry Potassium / urine Potassium Channel Blockers / chemistry Potassium Channels, Inwardly Rectifying / antagonists & inhibitors Rats Rats, Inbred SHR

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
10 06 2021
Historique:
pubmed: 27 5 2021
medline: 22 6 2021
entrez: 26 5 2021
Statut: ppublish

Résumé

A renal outer medullary potassium channel (ROMK, Kir1.1) is a putative drug target for a novel class of diuretics with potential for treating hypertension and heart failure. Our first disclosed clinical ROMK compound,

Identifiants

DOI: 10.1021/acs.jmedchem.1c00406 PMID: 34038119
pubmed: 34038119
doi: 10.1021/acs.jmedchem.1c00406
doi:

Substances chimiques

Benzofurans 0
Diuretics 0
MK-7145 0
Natriuretic Agents 0
Piperazines 0
Potassium Channel Blockers 0
Potassium Channels, Inwardly Rectifying 0
Potassium RWP5GA015D

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

7691-7701

Auteurs

Jinlong Jiang (J)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.
ORCID: 0000-0002-4889-9292

Fa-Xiang Ding (FX)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Xiaoyan Zhou (X)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Thomas J Bateman (TJ)

Pharmacokinetics Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Shuzhi Dong (S)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Xin Gu (X)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Reynalda Keh deJesus (R)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Barbara Pio (B)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Haifeng Tang (H)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Harry R Chobanian (HR)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Dorothy Levorse (D)

Discovery and Preclinical Sciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Mengwei Hu (M)

Discovery and Preclinical Sciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Brande Thomas-Fowlkes (B)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Michael Margulis (M)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Martin Koehler (M)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Adam Weinglass (A)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Jack Gibson (J)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Kevin Houle (K)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Joel Yudkovitz (J)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Caryn Hampton (C)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Lee-Yuh Pai (LY)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Koppara Samuel (K)

Pharmacokinetics Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Timothy Cutarelli (T)

Discovery Process Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Kathleen Sullivan (K)

Quantitative Biosciences, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Emma R Parmee (ER)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Ian Davies (I)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Alexander Pasternak (A)

Discovery Chemistry, Merck & Co., Inc., Kenilworth, New Jersey 07033, United States.

Articles similaires

[Redispensing of expensive oral anticancer medicines: a practical application].

Lisanne N van Merendonk, Kübra Akgöl, Bastiaan Nuijen
1.00
Humans Antineoplastic Agents Administration, Oral Drug Costs Counterfeit Drugs

Smoking Cessation and Incident Cardiovascular Disease.

Jun Hwan Cho, Seung Yong Shin, Hoseob Kim et al.
1.00
Humans Male Smoking Cessation Cardiovascular Diseases Female

Evaluation of Low-Value Services Across Major Medicare Advantage Insurers and Traditional Medicare.

Ciara Duggan, Adam L Beckman, Ishani Ganguli et al.
1.00
Humans United States Aged Cross-Sectional Studies Medicare Part C

Effectiveness of Virtual Yoga for Chronic Low Back Pain: A Randomized Clinical Trial.

Hallie Tankha, Devyn Gaskins, Amanda Shallcross et al.
1.00
Humans Yoga Low Back Pain Female Male

Classifications MeSH

questionsmedicales.fr › Phénomènes physiologiques de l'appareil locomoteur et du système nerveux › Phénomènes physiologiques du système nerveux › Potentiels de membrane › Potentiels d'action › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Eucaryotes › Animaux › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Benzofuranes › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Phénomènes physiologiques respiratoires et circulatoires › Phénomènes physiologiques cardiovasculaires › Hémodynamique › Pression sanguine › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Diurétiques › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Carnivora › Pinnipedia › Canidae › Chiens › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Phénomènes physiques › Temps › Période › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents cardiovasculaires › Natriurétiques › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pipérazines › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Produits chimiques inorganiques › Métaux › Métaux légers › Potassium › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents cardiovasculaires › Inhibiteurs des canaux potassiques › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Protéines de transport membranaire › Canaux ioniques › Canaux potassiques › Canaux potassiques rectifiants entrants › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Discovery of MK-8153, a Potent and Selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Lignées consanguines de rats › Rats de lignée SHR › Discovery of MK-8153, a Potent and Selective...