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Synthesis of [3H]DIPPA: A potent irreversible antagonist selective for the κ opioid receptor

✍ Scribed by An-Chih Chang; Joseph D. Trometer; Philip S. Portoghese

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

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✦ Synopsis

Abstract

2‐(3,4‐Dichlorophenyl)‐N‐methyl‐N‐[(1S)‐1‐(3‐isothiocyanatophenyl)‐2‐(1‐pyrrolidinyl)ethyl]acetamide (1, DIPPA) has been previously reported to be an opioid receptor affinity label that produces selective and long‐lasting κ opioid receptor antagonism in mice, High specific activity [^3^H]DIPPA (39.7 Ci/mmol) was prepared by bromination and catalytic tritiation of the amino precursor of DIPPA followed by conversion to the isothiocyanate with thiophosgene.

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