R-(-)-α-Methylhistamine (hydrochloride) 是一种有效的、选择性的和脑渗透性 H3 组胺受体激动剂,Kd 为 50.3 nM。
Cas No. | 75614-89-0 |
别名 | (R)-(-)-α-甲基组胺二盐酸盐 |
化学名 | (αR)-methyl-1H-imidazole-5-ethanamine, dihydrochloride |
Canonical SMILES | C[C@@H](N)CC1=CN=CN1.Cl.Cl |
分子式 | C6H11N3.2HCl |
分子量 | 198.1 |
溶解度 | DMF: inbsoluble,DMSO: 20 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 10 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | R-(-)-α-Methylhistamine is a histamine H3 receptor agonist with diverse biological activities. It inhibits the release of histamine induced by antidromic electrical stimulation of the sciatic nerve in rats when administered at doses ranging from 0.25 to 2 mg/kg, an effect that can be reversed by the selective histamine H3 receptor antagonist thioperamide . R-(-)-α-Methylhistamine (0.5-50 nmol) inhibits gastric acid secretion in rats when administered intracerebroventricularly but not intravenously. It reduces isolation-induced vocalizations and aggressive behavior in a resident-intruder test in guinea pig pups and mice, respectively. R-(-)-α-Methylhistamine (30 mg/kg) decreases freezing time in a conditioned fear stress test in rats. It also acts synergistically with fentanyl to reduce nociception and plasma extravasation in a mouse model of chronic inflammation induced by complete Freund's adjuvant. |