产品说明
应用
SB-277011-A hydrochloride hydrate has been used:
- as a dopamine D3 receptor-selective antagonist in rats to test its effect on 4-propyl-9-hydroxynaphthoxazine ([3H]-(+)-PHNO) radiotracer in cerebellum L9/10 and striatum
- as an acetylcholine inhibitor to test its negative allosteric modulation on Ascaris suum nicotinic acetylcholine receptor (Asu-ACR-16) expressed in Xenopus oocytes and its inhibitory effect on locomotion in Caenorhabditis elegans
- to test its effect on alcohol consumption in mice
SB-277011-A hydrochloride hydrate may be used in D3 dopamine receptor-mediated cell signaling studies.
包装
5, 25 mg in glass bottle
生化/生理作用
The D3 dopamine receptor antagonist, SB-277011-A inhibits the cocaine-seeking behavior and cocaine-enhances brain stimulation reward in in rats. It decreases drug-seeking behavior and may be useful in treatment of cocaine and methamphetamine addiction.
SB-277011-A is a potent, selective brain-penetrant D3 dopamine receptor antagonist; 80-100x selective for D3 over D2; pKi = 7.95 for hD3 receptor.
特点和优势
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
This compound is featured on the Dopamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
基本信息
| 经验(实验)分子式 | C28H30N4O · HCl · xH2O |
| 分子量 | 475.02 (anhydrous basis) |
| MDL编号 | MFCD16875431 |
| PubChem化学物质编号 | 329824542 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 储存条件 | protect from light |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear (warmed) |
| 创始人 | GlaxoSmithKline |
| 储存温度 | 2-8℃ |
| SMILES string | O.Cl.O=C(N[C@@H]1CC[C@H](CC1)CCN2CCc3cc(ccc3C2)C#N)c4ccnc5ccccc45 |
| InChI | 1S/C28H30N4O.ClH.H2O/c29-18-21-5-8-23-19-32(16-13-22(23)17-21)15-12-20-6-9-24(10-7-20)31-28(33)26-11-14-30-27-4-2-1-3-25(26)27;;/h1-5,8,11,14,17,20,24H,6-7,9-10,12-13,15-16,19H2,(H,31,33);1H;1H2/t20-,24-;; |
| InChI key | OOWNBQACGIKNGM-ONAIBGCWSA-N |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
