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Submit ReviewSB 258719 hydrochloride is a selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.
Sold for research purposes under agreement from GlaxoSmithKline
SB 258719 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 374.97 |
公式 | C18H30N2O2S.HCl |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 1217674-10-6 |
PubChem ID | 56972181 |
InChI Key | UIZKHTBWJSUGOV-UNTBIKODSA-N |
Smiles | O=S(C1=CC(C)=CC=C1)(N(C)[C@H](C)CCN2CCC(C)CC2)=O.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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 37.5 | 100 | |
DMSO | 37.5 | 100 |
以下数据基于产品分子量 374.97。 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 |
---|---|---|---|
1 mM | 2.67 mL | 13.33 mL | 26.67 mL |
5 mM | 0.53 mL | 2.67 mL | 5.33 mL |
10 mM | 0.27 mL | 1.33 mL | 2.67 mL |
50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
参考文献是支持产品生物活性的出版物。
Forbes et al (1998) (R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl)propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist. J.Med.Chem. 41 655 PMID: 9513592
Thomas et al (1998) Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br.J.Pharmacol. 124 1300 PMID: 9720804
Guscott et al (2003) The hypothermic effect of 5-CT in mice is mediated through the 5-HT7receptor. Neuropharmacology 44 1031 PMID: 12763096
If you know of a relevant reference for SB 258719 hydrochloride, please let us know.
关键词: SB 258719 hydrochloride, SB 258719 hydrochloride supplier, Selective, 5-HT7, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, SB258719, hydrochloride, GlaxoSmithKline, GSK, 2726, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SB 258719 hydrochloride 的部分引用包括:
Johnson et al (2011) Serotonin receptor activity is necessary for olfactory learning and memory in Drosophila melanogaster. Neuroscience 192 372 PMID: 21749913
Domínguez-Soto (2017) Serotonin drives the acquisition of a profibrotic and anti-inflammatory gene profile through the 5-HT7R-PKA signaling axis. Sci Rep 7 14761 PMID: 29116249
Zhao et al (2015) Fisetin exerts antihyperalgesic effect in a mouse model of neuropathic pain: engagement of spinal serotonergic system. Front Synaptic Neurosci 5 9043 PMID: 25761874
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.