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121524-09-2

中文名稱 121524-09-2
英文名稱 SR 58611A
CAS 121524-09-2
分子式 C22H27Cl2NO4
分子量 440.36
MOL 文件 121524-09-2.mol
更新日期 2024/12/23 10:32:14
121524-09-2 結(jié)構(gòu)式 121524-09-2 結(jié)構(gòu)式

基本信息

中文別名
(7S)-7-[[(2R)-2-(3-氯苯基)-2-羥乙基]氨基]-5,6,7,8-四氫-2-萘基]氧基]-乙酸乙酯鹽酸鹽
英文別名
SR 58611A
Amibegron hydrochloride
SR 58611A hydrochloride
[[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydro-2-naphthalenyl]ox]yaceticacidethylesterhydrochloride
Acetic acid, [[(7S)?-?7-?[[(2R)?-?2-?(3-?chlorophenyl)?-?2-?hydroxyethyl]?amino]?-?5,?6,?7,?8-?tetrahydro-?2-?naphthalenyl]?oxy]?-?, ethyl ester, hydrochloride (1:1)

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C
溶解度在DMSO中的溶解度為20mg/mL,澄清
形態(tài)粉末
顏色白色至米色
旋光性 (optical activity)[α]/D -75 to -95°, c = 0.5 in methanol

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS09
警示詞警告
危險(xiǎn)性描述H410
防范說明P273-P501
危險(xiǎn)品標(biāo)志N
危險(xiǎn)類別碼50/53
安全說明61
危險(xiǎn)品運(yùn)輸編號(hào)UN 3077 9 / PGIII
WGK Germany3

常見問題列表

生物活性
Amibegron hydrochloride 是一種選擇性的 β3-adrenoceptor 激動(dòng)劑,對(duì)大鼠結(jié)腸 β-adrenoceptor 的 EC50 值為 3.5 nM;Amibegron hydrochloride 具有抗焦慮和抗抑郁的活性。
靶點(diǎn)

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)

體外研究

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).

體內(nèi)研究

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.

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