Activity of Parthenolide at 5HT2A receptors.
Parthenolide displaces [3H]ketanserin from 5HT2A receptors from rat and rabbit brain and cloned 5HT2A receptors. Ki's are in the 100-250 microM range. These results suggest that parthenolide may be a low-affinity antagonist at 5HT receptors; it is unlikely that the entire mechanism of action can be explained by its modest 5HT2A receptor affinity.
Weber
J T
JT
Department of Pharmaceutical Sciences, School of Pharmacy, University of Montana, Missoula 59812-1075, USA.
O'Connor
M F
MF
Hayataka
K
K
Colson
N
N
Medora
R
R
Russo
E B
EB
Parker
K K
KK
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D002478:Cells, Cultured; D066298:In Vitro Techniques; D007650:Ketanserin / Q000493:pharmacokinetics; D007700:Kinetics; D011817:Rabbits; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000494:pharmacology*; D012717:Sesquiterpenes / Q000494:pharmacology*
D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D012717:Sesquiterpenes; C002669:parthenolide; D007650:Ketanserin