2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸
中文名称 | 2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸 |
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中文同义词 | 2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸;美兰纳坦;化合物 T16034;麦克林坦;2-[[[1-(7-氯-4-喹啉)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-三环[3.3.1.13,7]癸烷-2-羧酸;机械师 |
英文名称 | SR 48692 |
英文同义词 | SR 48692;2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid;2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]tricyclo[3.3.1.13,7]decane-2-carboxylic acid;meclinertant, CID 119192;merclinertant;CS-334;Tricyclo[3.3.1.13,7]decane-2-carboxylic acid, 2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-;2-CARBOXYLIC ACID |
CAS号 | 146362-70-1 |
分子式 | C32H31ClN4O5 |
分子量 | 587.07 |
EINECS号 | |
相关类别 | |
Mol文件 | 146362-70-1.mol |
结构式 |
2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸 性质
密度 | 1.50 |
---|---|
储存条件 | -20°C |
溶解度 | 在DMSO中的溶解度≥2mg/mL(加热) |
形态 | 粉末 |
颜色 | 白色至米色 |
Neurotensin receptor 1 (NTS1)
In vitro, Meclinertant (SR 48692) competitively inhibits
125
I-labeled neurotensin binding to the high-affinity binding site present in brain tissue from various species with IC
50
values of 0.99 nM (guinea pig), 4.0 nM (rat mesencephalic cells), 7.6 nM (COS-7 cells transfected with the cloned high-affinity rat brain receptor), 13.7 nM (newborn mouse brain), 17.8 nM (newborn human brain), 8.7 nM (adult human brain), and 30.3 nM (HT-29 cells). Meclinertant also displaces
125
I-labeled neurotensin from the low-affinity levocabastine-sensitive binding sites but at higher concentrations (34.8 nM for adult mouse brain and 82.0 nM for adult rat brain).
In guinea pig striatal slices, Meclinertant blocks K
+
-evoked release of [
3
H]dopamine stimulated by neurotensin with a potency (IC
50
= 0.46 nM) that correlates with its binding affinity.
Meclinertant (SR 48692) treatment reverses at 80 μg/kg the turning behavior induced by intrastriatal injection of neurotensin in mice and with a long duration of action (6 hours).
安全信息
WGK Germany | 3 |
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RTECS号 | YD1988500 |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2022/07/01 | HY-105189 | 2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸 Meclinertant | 146362-70-1 | 5mg | 4800元 |
2022/07/01 | HY-105189 | 2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸 Meclinertant | 146362-70-1 | 10mM * 1mLin DMSO | 6199元 |