小白菊内酯对5HT2A受体的活性。
Activity of Parthenolide at 5HT2A receptors.
作者信息
Weber J T, O'Connor M F, Hayataka K, Colson N, Medora R, Russo E B, Parker K K
机构信息
Department of Pharmaceutical Sciences, School of Pharmacy, University of Montana, Missoula 59812-1075, USA.
出版信息
J Nat Prod. 1997 Jun;60(6):651-3. doi: 10.1021/np960644d.
PMID:9214741
Abstract
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.
摘要
小白菊内酯可从大鼠和兔脑的5HT2A受体以及克隆的5HT2A受体上取代[3H]酮色林。其抑制常数（Ki）在100 - 250微摩尔范围内。这些结果表明，小白菊内酯可能是5HT受体的低亲和力拮抗剂；其整个作用机制不太可能仅通过其适度的5HT2A受体亲和力来解释。
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