[Binding of [3H] dihydroetorphine to opioid receptors in rat brain membrane]
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1Institute of Pharmacology & Toxicology, Academy of Military Medical Sciences, Beijing, China.
Aim:
To study the binding characteristics of dihydroetorphine (DHE) to opioid receptors.
Methods:
The binding of [3H] DHE to rat brain membrane opioid receptors was observed by radioligand binding study.
Results:
Saturation study showed the binding of [3H] DHE to rat brain membrane presented a single high-affinity class of binding sites with Kd = 0.19 nmol.L-1 and Bmax = 115 pmol/g protein. Kinetics study showed the association rate of [3H] DHE to opioid receptor was very rapid and dissociation very slow. NaCl 100 mmol.L-1 + guanosine triphosphate (GTP) 50 mumol.L-1 inhibited the binding of [3H] DHE and made Kd increase to 7.87 nmol.L-1, without effect on Bmax. Competitive inhibition of agonists and antagonists indicated that the affinity of [3H]DHE to mu opioid receptor was higher than to delta and kappa opioid receptors.
Conclusion:
DHE is a selective agonist of mu opioid receptors.
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