SB 271046 Hydrochloride
Cat. No.：YN320852
| 产品名称: | SB 271046 Hydrochloride |
| CAS No.: | 209481-24-3 |
| Chemical Name: | 5-chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophene-2-sulfonamide, monohydrochloride |
| Synonyms: | SB 271046A |
| 分子量: | 488.45 |
| 分子式: | C₂₀H₂₃Cl₂N₃O₃S₂ |
| SMILES: | ClC1=CC2=C(C=C1)SC(S(=O)(NC3=CC=C(C(N4CCNCC4)=C3)OC)=O)=C2C.[H]Cl |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | SB 271046 Hydrochloride (SB 271046A) 是一种高效、选择性和具有口服活性的5-HT6受体拮抗剂，对大鼠、猪和人的pKi分别为 9.02、8.55 和 8.81。SB 271046 Hydrochloride 对 5-HT6 受体、结合位点和离子通道的选择性超过 200 倍。具有抗惊厥活性 (EC50=0.16 μM)。 |
| IC50和靶点: | [{name:"5-HT6 Receptor:8.92-9.02 (pKi)"},{name: "5-HT1D Receptor:6.55 (pKi)"},{name: "5-HT1A Receptor:6.35 (pKi)"},{name: "5-HT1B Receptor:6.05 (pKi)"},{name: "5-HT1F Receptor:5.95 (pKi)"},{name: "5-HT2A Receptor:5.62 (pKi)"},{name: "5-HT2B Receptor:5.41 (pKi)"},{name: "5-HT7 Receptor:5.39 (pKi)"},{name: "5-HT4 Receptor:5.27 (pKi)"},{name: "5-HT1E Receptor:<4.99 (pKi)"},{name: "Human 5-HT2C Receptor:5.73 (pKi)"}] |
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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)
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.130,1606-1612(2000)
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.130,23-26(2000)
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.167,436-449(2012)
