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Submit ReviewLoperamide hydrochloride is a high affinity μ-opioid receptor agonist with peripheral selectivity (Ki values are 2, 48 and 1156 nM for μ-, δ- and κ-opioid receptors respectively). Antidiarrhoeal and antihyperalgesic agent. Also a Ca2+ channel blocker; at low micromolar concentrations it blocks broad spectrum neuronal HVA Ca2+ channels and at higher concentrations it reduces Ca2+ flux through NMDA receptor operated channels. Inhbits replication of MERS-CoV and SARS-CoV in vitro.
分子量 | 513.51 |
公式 | C29H33ClN2O2.HCl |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 34552-83-5 |
PubChem ID | 71420 |
InChI Key | PGYPOBZJRVSMDS-UHFFFAOYSA-N |
Smiles | Cl.CN(C)C(=O)C(CCN1CCC(O)(CC1)C1=CC=C(Cl)C=C1)(C1=CC=CC=C1)C1=CC=CC=C1 |
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 | |||
ethanol | 10.27 | 20 | |
DMSO | 10.27 | 20 |
以下数据基于产品分子量 513.51。 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 |
---|---|---|---|
0.2 mM | 9.74 mL | 48.68 mL | 97.37 mL |
1 mM | 1.95 mL | 9.74 mL | 19.47 mL |
2 mM | 0.97 mL | 4.87 mL | 9.74 mL |
10 mM | 0.19 mL | 0.97 mL | 1.95 mL |
参考文献是支持产品生物活性的出版物。
Awouters et al (1983) Pharmacology of antidiarrheal drugs. Annu.Rev.Pharmacol.Toxicol. 23 279 PMID: 6307123
Church et al (1994) Loperamide blocks high-voltage activated calcium channels and N-MthD.-aspartate -evoked responses in rat and mouse cultured hippocampal pyramidal neurons. Mol.Pharmacol. 45 747 PMID: 8183255
Daly et al (1995) Maitotoxin-elicited calcium influx in cultured cells - effect of calcium channel block. Biochem.Pharmacol. 50 1187 PMID: 7488233
Dehaven-Hudkins et al (1999) Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J.Pharmacol.Exp.Ther. 289 494 PMID: 10087042
de Wilde et al (2014) Screening of an FDA-approved compound library identifies four small-molecule inhibitors of Middle East Respiratory Syndrome coronavirus replication in cell culture. Antimicrob.Agents.Chemother. 58 4875
If you know of a relevant reference for Loperamide hydrochloride, please let us know.
关键词: Loperamide hydrochloride, Loperamide hydrochloride supplier, Ca2+, channel, blockers, HVA, L/N-type, NMDA, antagonists, reduces, flux, Peripherally, peripheral, μ-opioid, mu-opioid, agonists, Calcium, CaV, Channels, L-Type, N-Type, voltage-gated, voltage-dependent, Glutamate, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, MOP, OP3, Mu, Opioid, Cav1.x, Cav2.x, COVID-19, Coronavirus, 0840, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Loperamide hydrochloride 的部分引用包括:
Sałaga et al (2015) Calea zacatechichi dichloromethane extract exhibits antidiarrheal and antinociceptive effects in mouse models mimicking irritable bowel syndrome. J Pharmacol Exp Ther 388 1069 PMID: 26068703
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