BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values: 8.7 and 8.9, respectively).

5-HT1D:7.2(pKi), 5-HT1E:8.7(pKi), 5-HT1A:7.2(pKi), 5-HT1F:9.25(pKi), 5-HT1B:6.9(pKi)

BRL54443相对于盐水,诱导最大胃内体积立即剂量依赖性增加.

BRL 54443诱发收缩,其-logEC50为6.52。 BRL 54443引起的收缩很可能是通过刺激5-HT 5-HT 2A受体介导的。

In Vitro Radiometric PKD Kinase Assay: The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μl of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range. The filter papers are then washed three times in 0.5% phosphoric acid, air-dried, and counted using a Beckman LS6500 multipurpose scintillation counter.