Pro-Secretory Activity and Pharmacology in Rabbits of an Aminophenyl-1,3,5-Triazine CFTR Activator for Dry Eye Disorders | Zendy

Christian Félix | Zendy; Sujin Lee | Zendy; Marc H. Levin | Zendy; A. S. Verkman | Zendy

Open Access

Pro-Secretory Activity and Pharmacology in Rabbits of an Aminophenyl-1,3,5-Triazine CFTR Activator for Dry Eye Disorders

Author(s) -

Christian Félix,

Sujin Lee,

Marc H. Levin,

A. S. Verkman

Publication year - 2017

Publication title -

investigative ophthalmology and visual science

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.935

H-Index - 218

eISSN - 1552-5783

pISSN - 0146-0404

DOI - 10.1167/iovs.17-22525

Subject(s) - conjunctiva , ex vivo , in vivo , cornea , pharmacology , medicine , cystic fibrosis transmembrane conductance regulator , pharmacokinetics , chemistry , ophthalmology , cystic fibrosis , pathology , biology , microbiology and biotechnology

Pharmacological activation of ocular surface cystic fibrosis transmembrane conductance regulator (CFTR) chloride channels is a potential pro-secretory approach to treat dry eye disorders. We previously reported the discovery of aminophenyl-1,3,5-triazines, one of which, N-methyl-N-phenyl-6-(2,2,3,3-tetrafluoropropoxy)-1,3,5-triazine-2,4-diamine (herein called CFTRact-K267), fully activated human wildtype CFTR with EC50 ∼ 30 nM and increased tear volume for 8 hours in mice. Here, functional and pharmacological studies of CFTRact-K267 were done in adult New Zealand white rabbits.

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