Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors.

Article Details

Citation

di Bosco AM, Grieco P, Diurno MV, Campiglia P, Novellino E, Mazzoni O

Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors.

Chem Biol Drug Des. 2008 Apr;71(4):328-35. doi: 10.1111/j.1747-0285.2008.00637.x. Epub 2008 Feb 12.

PubMed ID
18284554 [ View in PubMed
]
Abstract

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- and delta-opioid receptors is described. Whilst no meaningful difference was detected concerning the docking of the arylpiperidine moiety, mu/delta selectivity could be explained as a different accommodation of the two phenyl groups in two lipophylic pockets of receptors.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
LoperamideDelta-type opioid receptorProteinHumans
Unknown
Agonist
Details
LoperamideMu-type opioid receptorProteinHumans
Yes
Agonist
Details