3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇性质、用途与生产工艺
3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇即BRL-54443是一种对5-HT1E和5-HT1F血清素受体亚型起选择性激动作用的药物。其制备受到越来越多医药工作者的关注。
BRL 54443 是 5-HT1E/1F 受体激动剂，Ki 分别为 1.1 nM 和 0.7 nM，比对其它 5-HT 和多巴胺受体的抑制性高 30 倍以上。
|
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.
3-(1-甲基-4-哌啶基)-1H-吲哚-5-醇
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