DESMETHYL LOPERAMIDE Chemical Properties

Melting point:

219-221?C

Boiling point:

678.3±55.0 °C(Predicted)

Density 

1?+-.0.06 g/cm3(Predicted)

storage temp. 

-20°C Freezer

solubility 

DMF: 2 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 1 mg/ml

form 

A crystalline solid

pka

13.85±0.20(Predicted)

Safety Information

HS Code 

9999999999

DESMETHYL LOPERAMIDE Usage And Synthesis

Chemical Properties

Off-White Solid

Uses

A metabolite of Loperamide; a new and improved PET radiotracer for imaging P-gp function

Uses

Loperamide is an opiate which potently and selectively activates μ opioid receptors (Ki = 0.16 nM) exclusively in the periphery. N-Desmethyl-loperamide (dLop) is a major metabolite of loperamide. Like loperamide, dLop is a substrate of the ATP-dependent efflux transporter, P-glycoprotein. As a result, both the parent compound and the metabolite display restricted passage through the blood-brain barrier. dLop in biological samples can be analyzed by a variety of methods.

Definition

ChEBI: A monocarboxylic acid amide that is the methylamide of 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylbutanoic acid.

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