Discovery of TRPA1 Antagonist


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:
03 Mar 2024
Historique:
medline: 3 3 2024
pubmed: 3 3 2024
entrez: 3 3 2024
Statut: aheadofprint

Résumé

Transient receptor potential ankyrin 1 (TRPA1) is a nonselective calcium ion channel highly expressed in the primary sensory neurons, functioning as a polymodal sensor for exogenous and endogenous stimuli, and has been implicated in neuropathic pain and respiratory disease. Herein, we describe the optimization of potent, selective, and orally bioavailable TRPA1 small molecule antagonists with strong

Identifiants

pubmed: 38431835
doi: 10.1021/acs.jmedchem.3c02121
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Auteurs

Martin Déry (M)

Paraza Pharma, Incorporated, 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.

Robin Larouche-Gauthier (R)

Paraza Pharma, Incorporated, 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.

Marjory Brooks (M)

Department of Population Medicine and Diagnostic Sciences, Cornell University College of Veterinary Medicine, Ithaca, New York 14853, United States.

Alyssa Stablein (A)

Department of Population Medicine and Diagnostic Sciences, Cornell University College of Veterinary Medicine, Ithaca, New York 14853, United States.

Francis Beaumier (F)

Paraza Pharma, Incorporated, 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.

Léa Constantineau-Forget (L)

Paraza Pharma, Incorporated, 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.

Chantal Grand-Maître (C)

Paraza Pharma, Incorporated, 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.

Luce Lépissier (L)

Paraza Pharma, Incorporated, 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.

Stéphane Ciblat (S)

Paraza Pharma, Incorporated, 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.

Claudio Sturino (C)

Paraza Pharma, Incorporated, 2525 Avenue Marie-Curie, Montreal, Quebec H4S 2E1, Canada.

Yong Chen (Y)

Pharmaron-Beijing Company Limited, 6 Taihe Road BDA, Beijing 100176, PR China.

Baihua Hu (B)

Pharmaron-Beijing Company Limited, 6 Taihe Road BDA, Beijing 100176, PR China.

Classifications MeSH