121524-09-2
中文名称 | 121524-09-2 |
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中文同义词 | (7S)-7-[[(2R)-2-(3-氯苯基)-2-羟乙基]氨基]-5,6,7,8-四氢-2-萘基]氧基]-乙酸乙酯盐酸盐;化合物 T10302;AMIBEGRON HCL |
英文名称 | SR 58611A |
英文同义词 | SR 58611A hydrochloride;SR 58611A;[[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydro-2-naphthalenyl]ox]yaceticacidethylesterhydrochloride;Amibegron hydrochloride;Acetic acid, [[(7S)?-?7-?[[(2R)?-?2-?(3-?chlorophenyl)?-?2-?hydroxyethyl]?amino]?-?5,?6,?7,?8-?tetrahydro-?2-?naphthalenyl]?oxy]?-?, ethyl ester, hydrochloride (1:1);Amibegron HCl;Amibegron hydrochloride(SR 58611A) |
CAS号 | 121524-09-2 |
分子式 | C22H27Cl2NO4 |
分子量 | 440.36 |
EINECS号 | |
相关类别 | 制剂-激动剂 |
Mol文件 | 121524-09-2.mol |
结构式 |
121524-09-2 性质
储存条件 | -20°C |
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溶解度 | 在DMSO中的溶解度为20mg/mL,澄清 |
形态 | 粉末 |
颜色 | 白色至米色 |
旋光性 (optical activity) | [α]/D -75 to -95°, c = 0.5 in methanol |
EC50: 3.5 nM (β-adrenoceptor, from rat colon), 499 nM (β-adrenoceptor, from rat uterus), 1.2 μM (β2-adrenoceptor, from cerebellum), 4.6 μM (β1-adrenoceptor1, from cortex)
Amibegron hydrochloride (SR 58611A) is a selective β-adrenoceptor agonist, with an EC 50 of 3.5 nM for β-adrenoceptor in rat colon, and 499 nM in rat uterus. Amibegron hydrochloride (SR 58611A) shows little effect on β1- and β2-adrenoceptors, 5-HT uptake, noradrenaline (NA) uptake, and dopamine (DA) uptake from rat brain tissue, with IC 50 s of 4.6 and 1.2, 0.58, 2.5 and 3.2 μM, respectively; exhibits no effect on 5-HT1A, 5-HT2, MAO-A and MAO-B (IC 50 > 10 μM).
Amibegron hydrochloride (SR 58611A, 0.1 to 0.3 mg/kg, i.p.) potentiates the toxicity produced by yohimbine in mice. Amibegron hydrochloride (0.6 and 2 mg/kg, i.p.) is also active in the learned helplessness model of antidepressant-like activity in rats. However, Amibegron hydrochloride exhibits no effect on the spontaneous locomotor activity of mice at up to 10 mg/kg and of rats at up tp 30 mg/kg. Amibegron hydrochloride (3 and 10 mg/kg, p.o.) increases the synthesis of 5-HT and tryptophan (Trp) levels in several rodent brain areas such as cortex, hippocampus, hypothalamus, striatum. In addition, Amibegron hydrochloride (10 mg/kg, p.o.) promotes the release of 5-HT in rat prefrontal cortex. Systemic (3 mg/kg, i.v.) or chronic administration of SR58611A (10 mg/kg, p.o.) does not affect the activity of serotonergic neurons in the rat dorsal raphe nucleus.
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-103207 | Amibegron hydrochloride | 1 mg | 1977元 | |
2024/04/30 | HY-103207 | 121524-09-2 Amibegron hydrochloride | 121524-09-2 | 10 mg | 6900元 |