BRL-54443是一种5-HT1E和5-HT1F受体激动剂,pKi分别为8.7和9.25,对5-HT1A, 5-HT1B, 5-HT1D受体具有弱的结合亲和力。A potent agonist at SR-1E and SR-1F.
Information
BRL 54443 is a5-HT1Eand5-HT1Freceptor agonist withpKiof 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. In vitro
BRL 54443 has also measurable affinity for the 5-HT2A receptor. BRL 54443 induces contraction with a −logEC50 of 6.52. Contraction caused by BRL 54443 is likely mediated through stimulation of 5-HT5-HT2A receptors.
In vivo
BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline. Cell Data
cell lines:Renca or 786-O cells, mouse endothelial cells and splenic CD11b+/c-myeloid cells, HUVECs