1 - (4,4 - 二苯基-3 - 丁烯基)- 3 -哌啶盐酸盐
中文名称 | 1 - (4,4 - 二苯基-3 - 丁烯基)- 3 -哌啶盐酸盐 |
---|---|
中文同义词 | 1 - (4,4 - 二苯基-3 - 丁烯基)- 3 -哌啶盐酸盐;1-(4,4-二苯基-3-丁烯-1-基)-3-哌啶甲酸盐酸盐;4-二苯基-3-丁烯基)-3-哌啶盐酸盐;化合物SKF89976A HYDROCHLORIDE;1-(4,4-二苯基丁-3-烯-1-基)哌啶-3-羧酸盐酸盐 |
英文名称 | 1-(4,4-DIPHENYL-3-BUTENYL)-3-PIPERIDINECARBOXYLIC ACID HYDROCHLORIDE |
英文同义词 | SKF 89976A HYDROCHLORIDE;1-(4,4-DIPHENYL-3-BUTENYL)-3-PIPERIDINECARBOXYLIC ACID HYDROCHLORIDE;SKF89976AHCl;skf-89976a;1-(4,4-Diphenyl-3-buten-1-yl)-3-piperidinecarboxylic acid hydrochloride;1-(4,4-Diphenylbut-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride;d,l-SKF89976A hydrochloride;l-SKF89976A hydrochloride |
CAS号 | 85375-15-1 |
分子式 | C22H26ClNO2 |
分子量 | 371.9 |
EINECS号 | |
相关类别 | 定制化学品;库存;GABA/Glycine receptor;GABA |
Mol文件 | 85375-15-1.mol |
结构式 |
1 - (4,4 - 二苯基-3 - 丁烯基)- 3 -哌啶盐酸盐 性质
储存条件 | Inert atmosphere,2-8°C |
---|---|
溶解度 | 在DMSO中的溶解度为20 mg/mL |
形态 | 固体 |
颜色 | 白色 |
IC50: 0.28 μM (GAT-1), 137.34 μM (GAT-2), 202.8 μM (GAT-3)
SKF89976A has a weak antiallodynic action. SKF89976A weakly inhibits serotonin transporter (SERT), noradrenaline transporter (NET), and dopamine transporter (DAT) in chinese hamster ovary (CHO) cells stably expressing each transporter using a substrate uptake assay, with IC 50 values of 3514 , 202.13, and 728.8, respectively. SKF89976A is a GABA-transport blocker. GABA (1 mM) elicited an inward current that is completely suppressed by the GABA transport inhibitors tiagabine (10 μM) and SKF89976A (100 μM), but is unaffected by 100 μM picrotoxin. 100 μM SKF 89976-A is known to block the transport of GABA into cells, completely eliminated the GABA-elicited current in a reversible fashion. SKF89976A is a nontransportable blockers of GAT-1. SKF89976-A also suppresses baseline inward currents that likely result from tonic GAT activation by background GABA. SKF89976A (100 μM) reversibly reduces GAT currents in every studied cell by 67.9±4.4% (n=19). Intracellular perfusion of 20 μM SKF89976-A progressively reduced and blocked GABA-induced GAT currents without blocking GABAAR-mediated currents (n=4).
SKF89976A produces a weak antiallodynic response when administered i.v. (0.3 mg/kg). The i.t. injection of SKF89976A dose-dependently ameliorates the reduction in the withdrawal threshold in PSL model mice.
安全信息
WGK Germany | 3 |
---|---|
RTECS号 | TM6241000 |
提供商 | 语言 |
---|---|
英文
|
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-100228A | 1 - (4,4 - 二苯基-3 - 丁烯基)- 3 -哌啶盐酸盐 SKF89976A hydrochloride | 85375-15-1 | 5mg | 660元 |
2024/08/19 | HY-100228A | 1 - (4,4 - 二苯基-3 - 丁烯基)- 3 -哌啶盐酸盐 SKF89976A hydrochloride | 85375-15-1 | 10mM * 1mLin DMSO | 726元 |