57477-39-1
57477-39-1 结构式
基本信息
3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇
BRL 54443
BRL 54443 HCl
BRL 54443, >=98%
BRL-54443
BRL54443
BRL 54443 USP/EP/BP
BRL54443
BRL 54443
BRL-54443
3-(1-methylpiperidin-4-yl)-1H-indol-5-ol
3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol
1H-Indol-5-ol, 3-(1-Methyl-4-piperidinyl)-
物理化学性质
常见问题列表
|
5-HT 1E Receptor 1.1 nM (Ki) |
5-HT 1F Receptor 0.7 nM (Ki) |
5-HT 1A Receptor 63 nM (Ki) |
5-HT 1B Receptor 126 nM (Ki) |
5-HT 1D Receptor 63 nM (Ki) |
5-HT 2A Receptor 1259 nM (Ki) |
5-HT 2B Receptor 100 nM (Ki) |
5-HT 2C Receptor 316 nM (Ki) |
5-HT 6 Receptor >10,000 nM (Ki) |
5-HT 7 Receptor >10,000 nM (Ki) |
Despite its low affinity for other receptors [5-HT
1A
(63 nM), 5-HT
1B
(126 nM), 5-HT
1D
(63 nM), 5-HT
2A
(1259 nM), 5-HT
2B
(100 nM), 5-HT
2C
(316 nM), 5-HT
6
(>10,000 nM), 5-HT
7
(>10,000 nM), D
2
(501 nM), D
3
(631 nM), and α
1B
-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT
1F
receptors.
In DG membranes, BRL54443 selectively stimulates 5-HT
1E
receptors and potently inhibits forskolin-dependent cAMP production (IC
50
=14 nM). BRL 54443 also induces contraction (-log EC
50
=6.52).
Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats.