289903-41-9Relevant academic research and scientific papers
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
Vanilloid analogues containing resinferatoxin pharmacophores as potent vanilloid receptor agonists and analgesics, compositions and uses thereof
-
, (2008/06/13)
The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.
