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Submit ReviewOndansetron hydrochloride is a selective 5-HT3 receptor antagonist (Ki = 6.16 nM). Also an inhibitor of human multidrug and toxin extrusion (MATE) transporter 1 (IC50 = <10-160 nM). Ondansetron blocks 5-HT-evoked transient inward currents (IC50 = 0.1 nM) in human recombinant h5-HT3A receptors. In an animal model of Parkinson's disease, Ondansetron reduces both the severity of dyskinesia and psychosis-like behaviors. Antiemetic; prevents emesis induced by cytotoxic drugs and radiation.
分子量 | 329.83 |
公式 | C18H19N3O.HCl |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 99614-01-4 |
PubChem ID | 68647 |
InChI Key | MKBLHFILKIKSQM-UHFFFAOYSA-N |
Smiles | CN1C3=C(C=CC=C3)C2=C1CCC(CN4C(C)=NC=C4)C2=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 | 16.49 | 50 | |
DMSO | 32.98 | 100 |
以下数据基于产品分子量 329.83。 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 | 3.03 mL | 15.16 mL | 30.32 mL |
5 mM | 0.61 mL | 3.03 mL | 6.06 mL |
10 mM | 0.3 mL | 1.52 mL | 3.03 mL |
50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
参考文献是支持产品生物活性的出版物。
Youssefyeh et al (1992) Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides. J.Med.Chem. 35 895 PMID: 1312602
Ye et al (2001) Ondansetron: a selective 5-HT3 receptor antagonist and its applications in CNS-related disorders. CNS Drug Rev. 7 199 PMID: 11474424
Ginawi et al (2005) Ondansetron, a selective antagonist, antagonizes methamphetamine-induced anorexia in mice. Pharmacol.Res. 51 255 PMID: 15661576
Wittwer et al (2013) Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. J.Med.Chem. 56 781 PMID: 23241029
Brown et al (1998) Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A). J.Physiol. 507 653 PMID: 9508827
Kwan et al (2021) Selective blockade of the 5-HT3 receptor acutely alleviates dyskinesia and psychosis in the parkinsonian marmoset. Neuropharmacology 182 PMID: 33152452
If you know of a relevant reference for Ondansetron hydrochloride, please let us know.
关键词: Ondansetron hydrochloride, Ondansetron hydrochloride supplier, Selective, 5-HT3, antagonists, Serotonin, Receptors, GR38032, antiparkinsons, parkinsons, MATE, transporter, GR, 38032, Multidrug, Transporters, 2891, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Ondansetron hydrochloride 的部分引用包括:
Jin et al (2014) Ginger and its pungent constituents non-competitively inhibit serotonin currents on visceral afferent neurons. Korean J Physiol Pharmacol 18 149 PMID: 24757377
Pezeshki et al (2016) Low protein diets produce divergent effects on energy balance. PLoS One 6 25145 PMID: 27122299
Amorim et al (2015) Galanin-Mediated Behavioural Hyperalgesia from the Dorsomedial Nucleus of the Hypothalamus Involves Two Independent Descending Pronociceptive Pathways. Antioxid Redox Signal 10 e0142919 PMID: 26565961
Spring et al (2019) Methionine Restriction Partly Recapitulates the Sympathetically Mediated Enhanced Energy Expenditure Induced by Total Amino Acid Restriction in Rats. Nutrients 11 PMID: 30917593
Capasso et al (2012) Modulation of mouse gastrointestinal motility by allyl isothiocyanate, a constituent of cruciferous vegetables (Brassicaceae): evidence for TRPA1-independent effects. Br J Pharmacol 165 1966 PMID: 21955242
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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.