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Binding characteristics of dihydroetorphine to opioid receptors in rat brain

Dan Wang

Open publisher page 6 citations

Abstract

The inhibitory potency of dihydroe torphine against the binding of [3H]naloxone, [3H]DPDPE and [3H]etorphine (with mu and delta sites having been previously suppressed by 30 nmol / L morphine and 100 nmol / L DADLE) to homogenates of rat brain opioid receptors was studied. The results showed that the inhibitory potency of dihydroetorphine against the binding of [3H]naloxone was much greater than that of [3H]DPDPE and[3H]etorphine. The relative affinity of dihydroetorphine to mu, delta and kappa receptors was 1951 : 2:1. This indicates that dihydroetorphine is a relative mu-receptor selective ligand.

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The inhibitory potency of dihydroe torphine against the binding of [3H]naloxone, [3H]DPDPE and [3H]etorphine (with mu and delta sites having been previously suppressed by 30 nmol / L morphine and 100 nmol / L DADLE) to homogenates of rat brain opioid receptors was studied. The results showed that the inhibitory potency of dihydroetorphine against the binding of [3H]naloxone was much greater than that of [3H]DPDPE and[3H]etorphine. The relative affinity of dihydroetorphine to mu, delta and kappa receptors was 1951 : 2:1. This indicates that dihydroetorphine is a relative mu-receptor selective ligand.

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Available abstract

The inhibitory potency of dihydroe torphine against the binding of [3H]naloxone, [3H]DPDPE and [3H]etorphine (with mu and delta sites having been previously suppressed by 30 nmol / L morphine and 100 nmol / L DADLE) to homogenates of rat brain opioid receptors was studied. The results showed that the inhibitory potency of dihydroetorphine against the binding of [3H]naloxone was much greater than that of [3H]DPDPE and[3H]etorphine. The relative affinity of dihydroetorphine to mu, delta and kappa receptors was 1951 : 2:1. This indicates that dihydroetorphine is a relative mu-receptor selective ligand.

Key concepts: Etorphine, DADLE, Chemistry, Receptor, Opioid, (+)-Naloxone, Pharmacology, Potency

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Binding characteristics of dihydroetorphine to opioid receptors in rat brain — Research Paper | ScholarLens