(R)-(-)-α-Methylhistamine dihydrobromide
(R)-(-)-α-Methylhistamine dihydrobromide 性质
| 储存条件 | Desiccate at RT |
|---|---|
| 形态 | 白色固体。 |
| 水溶解性 | Soluble to 100 mM in water |
(R)-(-)-α-Methylhistamine dihydrobromide 用途与合成方法
|
H 3 Receptor 50.3 nM (Kd) |
(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.
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. |
