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868698-49-1

中文名稱 (R)-(-)-α-Methylhistamine dihydrobromide
英文名稱 (R)-(-)-α-Methylhistamine dihydrobromide
CAS 868698-49-1
分子式 C6H11N3.2HBr
分子量 206.09
MOL 文件 868698-49-1.mol
868698-49-1 結(jié)構(gòu)式 868698-49-1 結(jié)構(gòu)式

基本信息

中文別名
(R)()-Α-甲基組胺 二鹽酸鹽
英文別名
(R)-(-)-α-Methylhistamine dihydrobromide
(αR)?-α-?Methyl-1H-?imidazole-?5-?ethanamine Hydrobromide

物理化學(xué)性質(zhì)

儲(chǔ)存條件Desiccate at RT
形態(tài)白色固體。
水溶解性溶于水至100mM

常見問題列表

生物活性
(R)-(-)-α-Methylhistamine dihydrobromide 是一種有效的選擇性 H3 組胺受體激動(dòng)劑,Kd 值為 50.3 nM。(R)-(-)-α-Methylhistamine dihydrobromide 可透過血腦屏障,并可增強(qiáng)記憶力,減輕大鼠的記憶力障礙。
靶點(diǎn)

H 3 Receptor

50.3 nM (Kd)

體外研究

(R)-(-)-α-Methylhistamine dihydrobromide is an H3-agonist that is > 10 times as potent as histamine (HA). Its selectivity toward H3-receptors is > 1,000 times as high as that of HA. (R)-(-)-α-Methylhistamine dihydrobromide has only weak affinities for H1 and H2 receptor with a pKi=4.8 and < 3.5, repectively. (R)-(-)-α-Methylhistamine dihydrobromide displays >200-fold selectivity over H4 receptors.

體內(nèi)研究

Pretreatment with (R)-(-)-α-Methylhistamine dihydrobromide (RAMH; 10 mg/kg; i.p.; 60 min before training) reverses propofol‐induced (25 mg/kg; i.p.; 30 min before training) memory retention.
(R)-alpha-Methylhistamine dihydrochloride (6.3 mg/kg; i.p.) significantly decreases the steady-state t-MH level in the mouse brain, whereas these compounds produced no significant changes in the HA level.

Animal Model: Male Sprague‐Dawley rats (10-12 week)
Dosage: 10 mg/kg
Administration: IP; 60 min before training
Result: Reversed propofol‐induced memory retention.
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