143937-74-0Relevant articles and documents
Effect of TRPV1 Antagonist SC0030, a Potent Painkiller, on RANKL-mediated Osteoclast Differentiation Involved in Bone Resorption
More, Kunal N.,Lee, Yong-Jin,Kim, Kwang-Jin,Suh, Young-Ger,Son, Young-Jin,Chang, Dong-Jo
, p. 488 - 491 (2020)
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Synthesis and Reactivity of 18F-Labeled α,α-Difluoro-α-(aryloxy)acetic Acids
Khotavivattana, Tanatorn,Calderwood, Samuel,Verhoog, Stefan,Pfeifer, Lukas,Preshlock, Sean,Vasdev, Neil,Collier, Thomas L.,Gouverneur, Véronique
supporting information, p. 568 - 571 (2017/02/10)
In this work, we describe the 18F-labeling of α,α-difluoro-α-(aryloxy)acetic acid derivatives and demonstrate that these building blocks are amenable to post-18F-fluorination functionalization. Protodecarboxylation offers a new entry to 18F-difluoromethoxyarene, and the value of this approach is further demonstrated with coupling processes leading to representative 18F-labeled TRPV1 inhibitors and TRPV1 antagonists.
Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands
Kim, Myeong Seop,Ki, Yooran,Ahn, Song Yeon,Yoon, Suyoung,Kim, Sung-Eun,Park, Hyeung-Geun,Sun, Wei,Son, Karam,Cui, Minghua,Choi, Sun,Pearce, Larry V.,Esch, Timothy E.,Deandrea-Lazarus, Ian A.,Blumberg, Peter M.,Lee, Jeewoo
, p. 382 - 385 (2014/01/17)
The chiral isomers of the two potent simplified RTX-based vanilloids, compounds 2 and 3, were synthesized employing highly enantioselective PTC alkylation and evaluated as hTRPV1 ligands. The analysis indicated that the R-isomer was the eutomer in binding affinity and functional activity. The agonism of compound 2R was comparable to that of RTX. Docking analysis of the chiral isomers of 3 suggested the basis for its stereospecific activity and the binding mode of 3R.
