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Documentos Principais

5.08162

Sigma-Aldrich

Loperamide Hydrochloride

Sinônimo(s):

Loperamide Hydrochloride, µ-Opioid Receptor Agonist, Loperamide Hydrochloride, Imodium

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About This Item

Fórmula empírica (Notação de Hill):
C29H33ClN2O2 · xHCl
Número CAS:
Peso molecular:
477.04 (free base basis)
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Ensaio

≥99% (HPLC)

Nível de qualidade

Formulário

solid

potência

2 nM Ki

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

white

solubilidade

DMSO: 50 mM
ethanol: 50 mM

temperatura de armazenamento

2-8°C

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

chave InChI

PGYPOBZJRVSMDS-UHFFFAOYSA-N

Descrição geral

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.

Ações bioquímicas/fisiológicas

Primary Target
u opioid receptor

Advertência

Toxicity: Toxic (F)

Nota de preparo

Warming is required for complete solubilization in ethanol.

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

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.
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.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Pictogramas

Skull and crossbones

Palavra indicadora

Danger

Frases de perigo

Declarações de precaução

Classificações de perigo

Acute Tox. 3 Oral

Código de classe de armazenamento

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


Certificados de análise (COA)

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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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