SB 271046 Hydrochloride
(Synonyms: 5-氯-N-[4-甲氧基-3-(1-哌嗪基)苯基]-3-甲基苯并[B]噻吩-2-磺酰胺盐酸盐,SB 271046A) 目录号 : GC37597
An orally-available 5-HT6 antagonist
Cas No.:209481-24-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SB-271046 is an orally-available antagonist of the serotonin receptor 5-HT6 (pKi = 9.02-8.92).1,2 It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.2 While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.3 It has been used to evaluate the role of 5-HT6 in learning and memory.4
1.Bromidge, S.M., Brown, A.M., Clarke, S.E., et al.5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): A potent, selective, and orally bioavailable 5-HT6 receptor antagonistJ. Med. Chem.42(2)202-205(1999) 2.Routledge, C., Bromidge, S.M., Moss, S.F., et al.Characterization of SB-271046: A potent, selective and orally active 5-HT6 receptor antagonistBr. J. Pharmacol.1301606-1612(2000) 3.Dawson, L.A., Nguyen, H.Q., and Li, P.In vivo effects of the 5-HT(6) antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, dopamine, 5-HT, glutamate and aspartateBr. J. Pharmacol.13023-26(2000) 4.Woods, S., Clarke, N.N., Layfield, R., et al.5-HT(6) receptor agonists and antagonists enhance learning and memory in a conditioned emotion response paradigm by modulation of cholinergic and glutamatergic mechanismsBr. J. Pharmacol.167436-449(2012)
| Cas No. | 209481-24-3 | SDF | |
| 别名 | 5-氯-N-[4-甲氧基-3-(1-哌嗪基)苯基]-3-甲基苯并[B]噻吩-2-磺酰胺盐酸盐,SB 271046A | ||
| Canonical SMILES | ClC1=CC2=C(C=C1)SC(S(=O)(NC3=CC=C(C(N4CCNCC4)=C3)OC)=O)=C2C.[H]Cl | ||
| 分子式 | C20H23Cl2N3O3S2 | 分子量 | 488.45 |
| 溶解度 | DMSO: 50 mg/mL (102.36 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0473 mL | 10.2365 mL | 20.4729 mL |
| 5 mM | 0.4095 mL | 2.0473 mL | 4.0946 mL |
| 10 mM | 0.2047 mL | 1.0236 mL | 2.0473 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Effects of 5-HT(6) receptor blockade on the neurochemical outcome of antidepressant treatment in the frontal cortex of the rat
J Neural Transm (Vienna) 2003 Jun;110(6):577-90.PMID:12768354DOI:10.1007/s00702-003-0812-1.
Using in vivo microdialysis in the freely moving rat we have examined the effects of 5-HT(6) receptor antagonism on the neurochemical outcome of antidepressant treatment. Acute administration of both desipramine (10 mg/kg s.c.) and venlafaxine (10 mg/kg s.c.) produced a 2 fold increase in extracellular noradrenaline (NA) but no change in frontal cortex dopamine (DaA), 5-HT or glutamate. Fluoxetine (20 mg/kg s.c.) produced no change in extracellular levels of any of the neurotransmitters examined. SB-271046 produced a 3 fold increase in extracellular glutamate. Combination treatment of SB-271046 with each antidepressant produced no change in the antidepressant-induced changes in NA, DA or 5-HT. In contrast, both fluoxetine and venlafaxine attenuated the SB-271046-induced increase in extracellular glutamate, suggesting that 5-HT and possibly NA may be having an inhibitory action on the excitatory pathways enhanced by 5-HT(6) receptor blockade. Furthermore, these data indicate that the neurochemical effects induced by NA and/or 5-HT reuptake inhibitors are not enhanced by 5-HT(6) receptor blockade indicating that 5-HT(6) receptor antagonists are unlikely to augment the therapeutic efficacy of these types of antidepressants.