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Preparation of N(1-ethyl-2-pyrrolidyl-methyl)2-methoxy-4-iodo-125I- 5-ethyl sulfonyl benzamide: A radioligand for the radioimmunoassay of sulpiride-related compounds

✍ Scribed by Maria Teresa Cardoso; Philippe Pradelles


Publisher
John Wiley and Sons
Year
1982
Tongue
French
Weight
194 KB
Volume
19
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

We describe the preparation of ^125^I labelling with a higher specific radioactivity of N(1‐ethyl ‐2‐pyrrolidyl‐methyl)2‐ methoxy ‐5‐ethyl sulfonyl benzamide, a potent biological analogue for sulpiride. The incorporation of iodine in the molecule was achieved by the substitution of aromatic amino groups via the diazo compound. Binding and immunological parameters of iodinated and tritiated tracers were compared.


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## Abstract 4‐Fluoro‐__N__‐{2‐[4‐(6‐trifluoromethylpyridin‐2‐yl)piperazin‐1‐yl]ethyl}benzamide is a full 5‐HT~1A~ agonist with high affinity (__pK__~__i__~=9.3), selectivity and a __c__ log __P__ of 3.045. The corresponding PET radioligand 4‐[^18^F]fluoro‐__N__‐{2‐[4‐(6‐trifluoromethylpyridin‐2‐yl)