Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.

Article Details


Raynor K, Kong H, Chen Y, Yasuda K, Yu L, Bell GI, Reisine T

Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.

Mol Pharmacol. 1994 Feb;45(2):330-4.

PubMed ID
8114680 [ View in PubMed

Opioid drugs, such as morphine, and the endogenous opioid peptides, namely the enkephalins, endorphins, and dynorphins, exert a wide spectrum of physiological and behavioral effects, including effects on pain perception, mood, motor control, and autonomic functions. These effects are mediated via membrane-bound receptors, of which the best characterized are the kappa, delta, and mu receptors. The existence of these distinct types of opioid receptors has recently been confirmed by molecular cloning. In the present study, we have examined the pharmacological profiles of the cloned kappa, delta, and mu receptors using a battery of widely employed opioid agents. Our results suggest that the cloned kappa and mu receptors have pharmacological characteristics similar to those of the endogenously expressed kappa 1 and mu receptors, respectively. The cloned delta receptor displays a pharmacological profile consistent with that of a delta 2 receptor. Opioid agents with abuse potential possess high affinities for the mu receptor. The availability of the cloned receptors will facilitate the identification and development of more specific and selective compounds with greater therapeutic potential and fewer undesirable side effects.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DiprenorphineDelta-type opioid receptorKi (nM)0.23N/AN/ADetails
DiprenorphineKappa-type opioid receptorKi (nM)0.01N/AN/ADetails
FentanylDelta-type opioid receptorKi (nM)1000N/AN/ADetails
FentanylKappa-type opioid receptorKi (nM)255N/AN/ADetails
MethadoneDelta-type opioid receptorKi (nM)1000N/AN/ADetails
MorphineDelta-type opioid receptorKi (nM)1000N/AN/ADetails
MorphineKappa-type opioid receptorKi (nM)538N/AN/ADetails
NalbuphineDelta-type opioid receptorKi (nM)1000N/AN/ADetails
NalbuphineKappa-type opioid receptorKi (nM)3.9N/AN/ADetails
NaloxoneDelta-type opioid receptorKi (nM)17N/AN/ADetails
NaloxoneKappa-type opioid receptorKi (nM)2.3N/AN/ADetails
SufentanilDelta-type opioid receptorKi (nM)50N/AN/ADetails
SufentanilKappa-type opioid receptorKi (nM)75N/AN/ADetails