80212-12-0Relevant articles and documents
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists
Gomtsyan, Arthur,Schmidt, Robert G.,Bayburt, Erol K.,Gfesser, Gregory A.,Voight, Eric A.,Daanen, Jerome F.,Schmidt, Diana L.,Cowart, Marlon D.,Liu, Huaqing,Altenbach, Robert J.,Kort, Michael E.,Clapham, Bruce,Cox, Phil B.,Shrestha, Anurupa,Henry, Rodger,Whittern, David N.,Reilly, Regina M.,Puttfarcken, Pamela S.,Brederson, Jill-Desiree,Song, Ping,Li, Bin,Huang, Susan M.,McDonald, Heath A.,Neelands, Torben R.,McGaraughty, Steve P.,Gauvin, Donna M.,Joshi, Shailen K.,Banfor, Patricia N.,Segreti, Jason A.,Shebley, Mohamad,Faltynek, Connie R.,Dart, Michael J.,Kym, Philip R.
, p. 4926 - 4947 (2016/06/13)
Transient receptor potential vanilloid 3 (TRPV3) is a Ca2+- and Na+-permeable channel with a unique expression pattern. TRPV3 is found in both neuronal and non-neuronal tissues, including dorsal root ganglia, spinal cord, and keratinocytes. Recent studies suggest that TRPV3 may play a role in inflammation, pain sensation, and skin disorders. TRPV3 studies have been challenging, in part due to a lack of research tools such as selective antagonists. Herein, we provide the first detailed report on the development of potent and selective TRPV3 antagonists featuring a pyridinyl methanol moiety. Systematic optimization of pharmacological, physicochemical, and ADME properties of original lead 5a resulted in identification of a novel and selective TRPV3 antagonist 74a, which demonstrated a favorable preclinical profile in two different models of neuropathic pain as well as in a reserpine model of central pain.
ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANTS
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Paragraph 0161, (2013/03/28)
Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
