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L4762

Loperamide hydrochloride

98-102% (USP), powder, Ca2+ channel blocker

동의어(들):

4-(p-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutyramide hydrochloride

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C29H33ClN2O2 · HCl
CAS 번호:
34552-83-5
Molecular Weight:
513.50
NACRES:
NA.77
PubChem Substance ID:
24278042
UNSPSC Code:
12352200
EC Number:
252-082-4
MDL number:
MFCD00058581
Quality level:
200
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제품 이름

Loperamide hydrochloride,

Quality Level

200

originator

Johnson & Johnson

SMILES string

Cl.CN(C)C(=O)C(CCN1CCC(O)(CC1)c2ccc(Cl)cc2)(c3ccccc3)c4ccccc4

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

Gene Information

human ... OPRM1(4988)

Application

Loperamide hydrochloride (HCl) has been used in inflammatory pain experiments and to assess the functionality of proteins. 54

Biochem/physiol Actions

Loperamide hydrochloride (HCl) is a non-selective Ca2+ channel blocker. At nanomolar concentrations, it binds to μ-opioid receptors. Loperamide HCl does not cross the blood-brain barrier.

Features and Benefits

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Preparation Note

Slightly soluble in water and dilute acids, freely soluble in methanol and in chloroform, soluble in ethanol (95%).

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pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

저장 등급

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

wgk

WGK 3

ppe

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

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시험 성적서(COA)

Lot/Batch Number
078K1867
057K1424
106K1679
095K1573
109H0934

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J Church et al.
Molecular pharmacology, 45(4), 747-757 (1994-04-01)
The effects of the antidiarrheal agent loperamide on high-voltage-activated (HVA) calcium channel activity and excitatory amino acid-evoked responses in two preparations of cultured hippocampal pyramidal neurons were examined. In rat hippocampal neurons loaded with the calcium-sensitive dye fura-2, rises in
Raphaël Weibel et al.
PloS one, 8(9), e74706-e74706 (2013-09-27)
Opiates are powerful drugs to treat severe pain, and act via mu opioid receptors distributed throughout the nervous system. Their clinical use is hampered by centrally-mediated adverse effects, including nausea or respiratory depression. Here we used a genetic approach to
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
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