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Loperamide HCl(R-18553)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Loperamide HCl(R-18553)图片
CAS NO:34552-83-5
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)513.5
FormulaC29H33ClN2O2.HCl
CAS No.34552-83-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 22 mg/mL (42.8 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (7.8 mM)
Other info

Chemical Name: 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide;hydrochloride

InChi Key: PGYPOBZJRVSMDS-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H33ClN2O2.ClH/c1-31(2)27(33)29(24-9-5-3-6-10-24,25-11-7-4-8-12-25)19-22-32-20-17-28(34,18-21-32)23-13-15-26(30)16-14-23;/h3-16,34H,17-22H2,1-2H3;1H

SMILES Code: CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl

SynonymsR 18553; ADL-2-1294; R-18553; ADL2-1294; R18553; ADL 2-1294; Loperamide Hydrochloride; Loperamide HCl; Imodium; Dissenten; Fortasec; Loperamide Monohydrochloride;
实验参考方法
In Vitro

In vitro activity: Loperamide exhibits potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently stimulates [35S]guanosine-5'-O-(3-thio)triphosphate binding with EC50 of 56 nM, and inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide potently inhibits late-phase formalin-induced flinching after intrapaw injection (A50 = 6 mg). Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC50 = 0.44 mM). Loperamide reversibly blocks rises in [Ca2+]i evoked by high [K+] in a concentration-dependent manner, with an IC50 of 0.9 mM. Loperamide (0.1-50 mM) produces a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM and, at the highest concentration tested, could fully block IBa in the absence of any other pharmacological agent. Loperamide also attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV, with an IC50 of 73 mM.

In VivoLoperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia when s.c. injected, locally over the tibial tumoral mass (7.5-75 mg) or distantly, under the fur of the neck (4 mg/kg) in mice.
Animal modelMice
Formulation & Dosage4 mg/kg
References

J Pharmacol Exp Ther. 1999 Apr;289(1):494-502; J Pharmacol Exp Ther. 2005 Jun;313(3):1011-6; Pharmacol Biochem Behav. 2005 May;81(1):114-21.