Výsledky vyhledávání

Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists

Autor: Vu Van Ma, Maosheng Zhang, Nuria A. Tamayo, Vijay Keshav Gore, Weiya Wang, Phi Tang, Holger Monenschein, Daniel B. Horne, Mark H. Norman, Michael D. Bartberger, Yunxin Bo, Jeffrey Clarine, Thomas T. Nguyen, Carl Davis, Beth D. Youngblood, Matthew R. Kaller, Sonya G. Lehto, Narender R. Gavva, Nobuko Nishimura

Publikováno v: Journal of medicinal chemistry. 57(7)

Transient receptor potential melastatin 8 (TRPM8) is a nonselective cation channel expressed in a subpopulation of sensory neurons in the peripheral nervous system. TRPM8 is the predominant mammalian cold temperature thermosensor and is activated by

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31259e241c7b92b3f659ee0304d6bff2
https://pubmed.ncbi.nlm.nih.gov/24597733

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Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility

Autor: Liping H. Pettus, Vassil I. Ognyanov, James J. S. Treanor, Phi Tang, Mark H. Norman, Xianghong Wang, Narender R. Gavva, Helming Tan, Rami Tamir, Partha P. Chakrabarti

Publikováno v: Bioorganicmedicinal chemistry letters. 17(23)

A series of trisubstituted pyrimidines were synthesized to improve aqueous solubility of our first TRPV1 clinical candidate (1; AMG 517), while maintaining potent TRPV1 inhibitory activity. Structure–activity and structure–solubility studies led

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38960115873ad338c2f59a2cdf4584f4
https://pubmed.ncbi.nlm.nih.gov/17937985

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Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties

Autor: Charles Bernard, Vijay Keshav Gore, Rami Tamir, Anthony W. Bannon, Hui-Ling Wang, Phi Tang, Sekhar Surapaneni, Jodie Katon, Oliver R. Thiel, Narender R. Gavva, Chenera Balan, Mark H. Norman, Nobuko Nishimura, Celia Dominguez, Vu Van Ma, Elizabeth M. Doherty, James J. S. Treanor

Publikováno v: Journal of medicinal chemistry. 50(15)

Based on the previously reported clinical candidate, AMG 517 (compound 1), a series of related piperazinylpyrimidine analogues were synthesized and evaluated as antagonists of the vanilloid 1 receptor (VR1 or TRPV1). Optimization of in vitro potency

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::519c2957e1742243aa04fd73fa4aec44
https://pubmed.ncbi.nlm.nih.gov/17585751

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