5.08162
Loperamide Hydrochloride
别名:
Loperamide Hydrochloride, µ-Opioid Receptor Agonist, Loperamide Hydrochloride, Imodium
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关于此项目
经验公式（希尔记法）:
C29H33ClN2O2 · xHCl
化学文摘社编号:
分子量:
477.04 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
[Cl-].Clc1ccc(cc1)C2(CC[N+H](CC2)CCC(c4ccccc4)(c3ccccc3)C(=O)N(C)C)O
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
InChI key
PGYPOBZJRVSMDS-UHFFFAOYSA-N
assay
≥99% (HPLC)
form
solid
potency
2 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 50 mM, ethanol: 50 mM
Quality Level
General description
A very potent and highly selective peripheral resctricted µ-opioid receptor agonist (Ki = 2 nM). Often used as an antidiarrheal, antipruritic, and antihyperalgesic agent. In addition, shown to improve defective post-receptor insulin signaling in skeletal muscle cells and enhance insulin sensitivity in rats.
Biochem/physiol Actions
Primary Target
u opioid receptor
u opioid receptor
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warming is required for complete solubilization in ethanol.
Other Notes
Cheng, K., et al. 2013. Pharmaco. Ther.139, 334.
Di Bosco, M., et al. 2008. Chem. Biol. Drug Des.71, 328.
DeHaven-Hudkins, D., et al. 1999. J. Pharmacol. Exp. Ther.289, 494.
Mackerer, C., et al. 1976. J. Pharmacol. Exp. Ther.199, 131.
Di Bosco, M., et al. 2008. Chem. Biol. Drug Des.71, 328.
DeHaven-Hudkins, D., et al. 1999. J. Pharmacol. Exp. Ther.289, 494.
Mackerer, C., et al. 1976. J. Pharmacol. Exp. Ther.199, 131.
Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Toxic (F)
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors.
Antonio Mazzella di Bosco et al.
Chemical biology & drug design, 71(4), 328-335 (2008-02-21)
Loperamide is a piperidine analogue, acting as agonist on peripheral opioid receptors, exhibiting affinity and selectivity for the cloned mu human opioid receptor compared with the delta human opioid receptor. Automatic docking studies of loperamide, using AutoDock, on human mu-
C R Mackerer et al.
The Journal of pharmacology and experimental therapeutics, 199(1), 131-140 (1976-10-01)
Loperamide, a new antidiarrheal agent, was tested to determine whether its biological activity involves binding to opiate receptor sites. Loperamide and morphine competitively inhibited 3H-naloxone binding to homogenates a guinea-pig brain and myenteric plexus. The Kp values obtain in the
D L DeHaven-Hudkins et al.
The Journal of pharmacology and experimental therapeutics, 289(1), 494-502 (1999-03-23)
The antihyperalgesic properties of the opiate antidiarrheal agent loperamide (ADL 2-1294) were investigated in a variety of inflammatory pain models in rodents. Loperamide exhibited potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta
Kai-Chun Cheng et al.
Pharmacology & therapeutics, 139(3), 334-340 (2013-05-22)
Type-2 diabetes is one of the fastest growing public health problems worldwide resulting from both environmental and genetic factors. Activation of μ-opioid receptor (MOR) could result in reversal of the impairment of insulin-stimulated glucose disposal in genetically obese Zucker rats
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