

生物活性
产品描述 |
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective agonist of H3 histamine receptor( Kd of 50.3 nM). |
靶点活性 |
H3 Receptor,50.3 nM (kd) |
体外活性 |
(R)-(-)-α-Methylhistamine dihydrobromide is an H3-agonist that is > 10 times as potent as histamine (HA).(R)-(-)-α-Methylhistamine dihydrobromide has only weak affinities for H1 and H2 receptor with a pKi=4.8 and < 3.5, repectively. Its selectivity toward H3-receptors is > 1,000 times as high as that of HA. (R)-(-)-α-Methylhistamine dihydrobromide displays >200-fold selectivity over H4 receptors[1]. |
体内活性 |
(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[2].Pretreatment with (R)-(-)-α-Methylhistamine dihydrobromide reverses propofol‐induced memory retention[4]. |
化学信息
分子量 |
287 |
分子式 |
C6H13Br2N3 |
CAS |
868698-49-1 |
溶解度 |
( < 1 mg/ml refers to the product slightly soluble or insoluble ) |
储存条件 |
store at -80°C |
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
1 mg | 5 mg | 10 mg | |
1 mM | 3.484 ml | 17.422 ml | 34.843 ml |
5 mM | 0.697 ml | 3.484 ml | 6.969 ml |
10 mM | 0.348 ml | 1.742 ml | 3.484 ml |
50 mM | 0.07 ml | 0.348 ml | 0.697 ml |
参考文献
- 1. Mohammad Shahid, et al. Histamine, Histamine Receptors, and their Role in Immunomodulation: An Updated Systematic Review. The Open Immunology Journal, 2009, 2, 9-41.
- 2. 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.
- 3. 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.
- 4. 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.