91477-84-8Relevant articles and documents
HEDGEHOG ACYLTRANSFERASE INHIBITORS AND USES THEREOF
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Paragraph 00274, (2018/02/24)
Hedgehog acyltransferase (Hhat), a membrane-bound O-acyl transferase (MBOAT) protein, is responsible for the palmitoylation of Shh and is crucial to proper Shh signaling. Hhat inhibitors that are capable of preventing Shh palmitoylation and mitigating Shh
Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists
Tamayo, Nuria A.,Bo, Yunxin,Gore, Vijay,Ma, Vu,Nishimura, Nobuko,Tang, Phi,Deng, Hong,Klionsky, Lana,Lehto, Sonya G.,Wang, Weiya,Youngblood, Brad,Chen, Jiyun,Correll, Tiffany L.,Bartberger, Michael D.,Gavva, Narender R.,Norman, Mark H.
, p. 1593 - 1611 (2012/04/17)
The transient receptor potential melastatin type 8 (TRPM8) is a nonselective cation channel primarily expressed in a subpopulation of sensory neurons that can be activated by a wide range of stimuli, including menthol, icilin, and cold temperatures (25 °C). Antagonism of TRPM8 is currently under investigation as a new approach for the treatment of pain. As a result of our screening efforts, we identified tetrahydrothienopyridine 4 as an inhibitor of icilin-induced calcium influx in CHO cells expressing recombinant rat TRPM8. Exploration of the structure-activity relationships of 4 led to the identification of a potent and orally bioavailable TRPM8 antagonist, tetrahydroisoquinoline 87. Compound 87 demonstrated target coverage in vivo after oral administration in a rat pharmacodynamic model measuring the prevention of icilin-induced wet-dog shakes (WDS).
SUBSTITUTED SULFONAMIDE DERIVATIVES
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Page/Page column 111, (2009/11/29)
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.