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Submit ReviewSB 224289 hydrochloride
说明： Selective 5-HT1B antagonist
化学名： 1'-Methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine hydrochloride
纯度： ≥95% (HPLC)
生物活性 for SB 224289 hydrochloride
SB 224289 hydrochloride is a selective 5-HT1B receptor antagonist (pKi = 8.2). Displays > 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo.
许可信息
Sold with the permission of GlaxoSmithKline
技术数据 for SB 224289 hydrochloride
| 分子量 | 557.09 |
| 公式 | C32H32N4O3.HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 180084-26-8 |
| PubChem ID | 11226716 |
| InChI Key | GKGKBZYMDILCOF-UHFFFAOYSA-N |
| Smiles | O=C(C5=CC=C(C6=CC=C(C7=NOC(C)=N7)C=C6C)C=C5)N2C1=CC3=C(OCC43CCN(CC4)C)C=C1CC2.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SB 224289 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 5.57 | 10 温和加热 |
制备储备液 for SB 224289 hydrochloride
以下数据基于产品分子量 557.09。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 17.95 mL | 89.75 mL | 179.5 mL |
| 0.5 mM | 3.59 mL | 17.95 mL | 35.9 mL |
| 1 mM | 1.8 mL | 8.98 mL | 17.95 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.59 mL |
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产品说明书 for SB 224289 hydrochloride
参考文献 for SB 224289 hydrochloride
参考文献是支持产品生物活性的出版物。
Gaster et al (1998) The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine (SB-224289) potently blocks terminal 5-HT J.Med.Chem. 41 1218 PMID: 9548813
Hagan et al (1997) Stimulation of 5-HT1B receptors causes hypothermia in the guinea-pig. Eur.J.Pharmacol. 331 169 PMID: 9274976
Roberts et al (1998) Differential effects of 5-HT1B/1D receptor antagonists in dorsal and median raphe innervated brain regions. Eur.J.Pharmacol. 346 175 PMID: 9652357
Selkirk et al (1998) SB-224289 - a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity. Br.J.Pharmacol. 125 202 PMID: 9776361
If you know of a relevant reference for SB 224289 hydrochloride, please let us know.
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关键词: SB 224289 hydrochloride, SB 224289 hydrochloride supplier, Selective, 5-HT1B, antagonist, Serotonin, Receptors, SB224289, hydrochloride, GlaxoSmithKline, GSK, 1221, Tocris Bioscience
8 篇 SB 224289 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SB 224289 hydrochloride 的部分引用包括：
Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728
Hirono (2017) Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells. Neuropharmacology 118 79 PMID: 28300552
Cassilly et al (2016) SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A. Mol Ther 11 e0154932 PMID: 27183222
Morecroft et al (2012) Gene therapy by targeted adenovirus-mediated knockdown of pulmonary endothelial Tph1 attenuates hypoxia-induced pulmonary hypertension. Neuron 20 1516 PMID: 22525513
Baillie et al (2012) Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres. PLoS One 63 362 PMID: 22691374
Siddiqui et al (2006) The role of serotonin (5-hydroxytryptamine1A and 1B) receptors in prostate cancer cell proliferation. J Urol 176 1648 PMID: 16952708
Heisler et al (2006) Serotonin reciprocally regulates melanocortin neurons to modulate food intake. J Neurosci 51 239 PMID: 16846858
Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833
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The 5,760 bioactive compound library is a collated compound set of approved drugs and biologically active compound.
By
Anonymous on 02/01/2020
分析类型： In Vitro
种属： Other
Biologically active compounds that have been documented to interact with awide range of targets including SB-224289 (Cat. # 1221), MG-624 (Cat.# 1356), GVIA (Cat. No. 1085), DPAT hydrobromide (Cat. No. 1080) and valinomycin (VA; Cat. # 3373) were ordered from Tocris Bioscience
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