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R-(−)-α-Methylhistamine (hydrochloride)

用途

(R) -(-)-α-甲基组胺盐酸盐是一种有效、选择性和脑渗透性的H3组胺受体激动剂,Kd为50.3 nM[1][2]。(R) -(-)-α-甲基组胺盐酸盐能增强记忆保留,减轻大鼠记忆障碍[3][4][5]。

名称

[ CAS 号 ]:
75614-89-0

[ 中文名 ]:
(-)-Alpha-甲基胺盐酸盐

[ 英文名 ]:
(R)-(-)-α-Methylhistamine dihydrochloride

[中文别名 ]:

[英文别名 ]:

R(-)-α-Methylhistamine Dihydrochloride

生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H3 Receptor:50.3 nM (Kd)

[体外研究]

(R) -(-)-α-甲基组胺盐酸盐是一种H3激动剂,其效力是组胺(HA)的10倍以上。其对H3受体的选择性是HA的1000倍以上。(R) -(-)-α-甲基组胺盐酸盐对H1和H2受体的亲和力较弱,pKi分别为4.8和<3.5。(R) -(-)-α-甲基组胺盐酸盐比H4受体[1][2][3]显示出>200倍的选择性。

[体内研究]

用(R)-(-)-α-甲基组胺盐酸盐(RAMH；10 mg/kg；静脉注射；训练前60分钟)预处理可逆转丙泊酚诱导的(25 mg/kg；静脉注射；训练前30分钟)记忆保留[5]。(R) -(-)-α-甲基组胺盐酸盐(6.3 mg/kg；i.p.)显著降低小鼠大脑中的稳态t-MH水平,而这些化合物在HA水平上没有产生显著变化[3]。动物模型：雄性Sprague-Dawley大鼠(10-12周)[3]剂量：10mg/kg给药：IP；训练前60分钟结果：逆转异丙酚诱导的记忆保留。

[参考文献]

[1]. Arrang JM, et al. Highly potent and selective ligands for histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23.

[2]. Mohammad Shahid, et al. Histamine, Histamine Receptors, and their Role in Immunomodulation: An Updated Systematic Review. The Open Immunology Journal, 2009, 2, 9-41.

[3]. Oishi R, et al. Effects of the histamine H3-agonist (R)-alpha-methylhistamine and the antagonist thioperamideon histamine metabolism in the mouse and rat brain. J Neurochem. 1989 May;52(5):1388-92.

[4]. Yamasaki S, et al. The disposition of (R)-alpha-methylhistamine, a histamine H3-receptor agonist, in rats. J Pharm Pharmacol. 1994 May;46(5):371-4.

[5]. Li WW, et al. (R)-alpha-methylhistamine suppresses inhibitory neurotransmission in hippocampal CA1 pyramidal neurons counteracting propofol-induced amnesia in rats. CNS Neurosci Ther. 2014 Sep;20(9):851-9.

物理化学性质

[ 分子式 ]:
C₆H₁₃Cl₂N₃

[ 分子量 ]:
198.09400

[ 精确质量 ]:
197.04900

[ PSA ]:
54.70000

[ LogP ]:
2.77620

[ 储存条件 ]:
室温，干燥，密封

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

Highly potent and selective ligands for histamine H3-receptors.

Nature 327 , 117, (1987)

New drugs selective for histamine H3-receptors can be used to establish that these receptors are involved in the feedback control of histamine synthesis and release, and to demonstrate their distribut...

Effects of the histamine H3-agonist (R)-alpha-methylhistamine and the antagonist thioperamide on histamine metabolism in the mouse and rat brain.

J. Neurochem. 52 , 1388, (1989)

To study the feedback control by histamine (HA) H3-receptors on the synthesis and release of HA at nerve endings in the brain, the effects of a potent and selective H3-agonist, (R)-alpha-methylhistami...

Structure-activity relations of histamine analogs. XX. Absolute configuration and histamine-like activity of enantiomeric α-methyl histamines. Gerhard, et al.

Arch. Pharm. Res. 313 , 709, (1980)

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