130972-90-6Relevant articles and documents
The SAR analysis of TRPV1 agonists with the α-methylated B-region
Cho, Yongsung,Kim, Myeong Seop,Kim, Ho Shin,Ann, Jihyae,Lee, Jeewoo,Lee, Jiyoun,Pearce, Larry V.,Pavlyukovets, Vladimir A.,Morgan, Matthew A.,Blumberg, Peter M.
scheme or table, p. 5227 - 5231 (2012/09/07)
A series of TRPV1 agonists with amide, reverse amide, and thiourea groups in the B-region and their corresponding α-methylated analogues were investigated. Whereas the α-methylation of the amide B-region enhanced the binding affinities and potencies as agonists, that of the reverse amide and thiourea led to a reduction in receptor affinity. The analysis indicated that proper hydrogen bonding as well as steric effects in the B-region are critical for receptor binding.
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.