| 产品描述: | SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM) |
| 靶点: |
5-HT6 Receptor:8.92-9.02 (pKi);5-HT1D Receptor:6.55 (pKi);5-HT1A Receptor:6.35 (pKi);5-HT1B Receptor;6.05 (pKi);5-HT1F Receptor:5.95 (pKi);5-HT2A Receptor:5.62 (pKi);5-HT2B Receptor:5.41 (pKi);5-HT7 Receptor:5.39 (pKi);5-HT4 Receptor:5.27 (pKi);5-HT1E Receptor:<4.99 (pKi);Human 5-HT2C Receptor:5.73 (pKi);5-HTReceptor |
| 体外研究: |
SB 271046 Hydrochloride (SB 271046A) shows pKi values of 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively. SB-271046 Hydrochloride competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71 |
| 体内研究: |
SB 271046 Hydrochloride (10 mg/kg; p.o.) produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg/kg p.o. and maximum effect at 4 h post-dose Animal Model: Male Sprague Dawley rats Dosage: 10 mg/kg Administration: P.o. Result: Produced an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg kg−1 p.o. and maximum effect at 4 h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB-271046 (EC50 of 0.16 μM) and brain concentrations of 0.01-0.04 μM at Cmax. |
| 参考文献: |
1. Routledge C, et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000;130(7):1606-1612. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
2-8℃;干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.047 ml |
10.236 ml |
20.473 ml |
| 5 mM |
0.409 ml |
2.047 ml |
4.095 ml |
| 10 mM |
0.205 ml |
1.024 ml |
2.047 ml |
| 50 mM |
0.041 ml |
0.205 ml |
0.409 ml |
|
| 注意: |
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