210918-31-3Relevant academic research and scientific papers
AMINOTETRALIN-DERIVED UREA MODULATORS OF VANILLOID VR1 RECEPTOR
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, (2010/11/30)
This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to β-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas, a promising class of vanilloid receptor agonists and analgesics
Lee, Jeewoo,Lee, Jiyoun,Kang, Myung-Sim,Kim, Kang-Pil,Chung, Suk-Jae,Blumberg, Peter M.,Yi, Jung-Bum,Park, Young Ho
, p. 1171 - 1179 (2007/10/03)
In order to improve the analgesic activity and pharmacokinetics of thioureas 2 and 3, which we previously developed as potent vanilloid receptor (VR) agonists, we prepared and characterized phenolic modifications of them and of their amide surro-gates (7, 8). The aminoethyl analogue of the amide template 13 was a potent analgesic with an EC50 =0.96 μg/kg in the AA-induced writhing test and with better in vivo stability than the parent phenol. Copyright
