Opioid receptor interaction and adenylyl cyclase inhibition of dihydroetorphine: direct comparison with etorphine.

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Niwa M, al-Essa LY, Ohta S, Kohno K, Nozaki M, Tsurumi K, Iwamura T, Kataoka T

Opioid receptor interaction and adenylyl cyclase inhibition of dihydroetorphine: direct comparison with etorphine.

Life Sci. 1995;56(21):PL395-400.

PubMed ID

7739347 [ View in PubMed

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Abstract

To find out the reason of weak addiction property of dihydroetorphine, we compared the affinities of dihydroetorphine to the type selective opioid receptor and inhibition effect on the adenylyl cyclase activity with those of etorphine. Dihydroetorphine and etorphine have almost the same binding affinities to all types (mu, delta, and kappa) of opioid receptors and antagonist binding sites, and have similar inhibition activities to forskolin stimulated adenylyl cyclase. However, dihydroetorphine showed significantly smaller value of DTNB-index compared with that of etorphine. This differentiation may explain partly the high analgesic with low dependence properties of dihydroetorphine.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Etorphine	Delta-type opioid receptor	Protein	Humans	Yes	Agonist	Details
Etorphine	Kappa-type opioid receptor	Protein	Humans	Yes	Agonist	Details