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Synthesis and characterization of 7α-O-iodoallyl diprenorphine: A new ligand for potential spect imaging of opioid receptors

✍ Scribed by R. F. Wang; J. A. M. Tafani; M. Bergon; P. Tisnes; Y. Coulais; J. M. Zajac; R. Guiraud

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
552 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The preparation and synthesis of [^125^I]7α‐O‐iodoallyl diprenorphine, a high affinity opioid receptor antagonist, is described using a versatile vinylstannane as prosthetic group for radioiodination at the tertiary alcohol group in the 7α‐side chain. Radioiododestannylation with selective conditions in one step occurs under mild, no‐carrier‐added‐conditions to give the corresponding [^125^I]7α‐O‐iodoallyl diprenorphine analogue in good radiolabelled yields (70‐90%) with specific radioactivity 80 TBq/mmol (2200 Ci/mmol) and radiochemical purity > 95%. Iodoallyl diprenorphine exhibited in vitro a very high affinity (K~i~ = 0.4 nM), so that this radioligand could be suitable for imaging opioid receptors in living humans by Single Photon Emission Computed Tomography (SPECT).

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