| CAS NO: | 1049740-32-0 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1049740-32-0 |
| 化学名 | (R)-4'-(3-(3-(dimethylamino)pyrrolidin-1-yl)propoxy)-[1,1'-biphenyl]-4-carbonitrile dihydrochloride |
| Canonical SMILES | CN([C@](C1)([H])CCN1CCCOC2=CC=C(C3=CC=C(C#N)C=C3)C=C2)C.Cl.Cl |
| 分子式 | C22H27N3O.2HCl |
| 分子量 | 422.39 |
| 溶解度 | <42.24mg/ml in Water;<8.45mg/ml in DMSO |
| 储存条件 | Desiccate at RT |
| 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 | A-331440 is described here instead of A-331440 dihydrochloride. A-331440 is an antagonist of non-imidazole histamine H3 receptor with an IC50 value of 22.7 nM for human cortex histamine H3 [1]. Histamine, as a neurotransmitter, is important in homeostasis and physiology. In the CNS, histamine released has the potential to interact with H1, H2, H3 and possibly H4 receptors. All the receptors are G-protein coupled receptors [2]. In HEK 293 cells stably transfected with rat or human histamine H3 receptors, A-331440 was tested for its ability to antagonize increasing calcium mobilization in response to (R)-α-methylhistamine and showed pKb ± S.E.M. values of 7.38 ± 0.10 and 7.37 ± 0.29 for rat histamine H3 and human histamine H3, respectively [1]. In mice, treatment with A-331440 at a dose of 100 mg/kg resulted in piloerection and hypoactivity in the first 2 h, but diminished thereafter. In naive male CD-1 mice, administration with comparable doses of A-331440 i.p. also produced similar data. By day 28, mice treated with A-331440 at the intermediate dose weighed 35.7 ± 0.93 g with an average weight loss of 5.3 ± 0.99 g. The high dose of A-331440 (15 mg/kg, p.o., b.i.d.) produced a marked and sustained weight loss [1]. References: |
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