✦ LIBER ✦

Labeling of (S)-DES-4-amino-3-[125I]iodozacopride (DAIZAC), a high-affinity radioligand for the 5-HT-3 receptor

✍ Scribed by N. Scott Mason; William A. Hewlett; Michael H. Ebert; Dennis E. Schmidt; Tomas de Paulis

Publisher: John Wiley and Sons
Year: 1996
Tongue: French
Weight: 388 KB
Volume: 38
Category: Article
ISSN: 0022-2135
DOI: 10.1002/(sici)1099-1344(199611)38:11<955::aid-jlcr912>3.0.co;2-#

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✦ Synopsis

We have prepared (S)-5-chloro-3-[ 1251]iodo-2-methoxy-N-( l-azabicyclo[2.2.2]oct-3-yl)benzamide ([125I]DAIZAC, [ 1254-3) as a radioligand for characterization of the 5-HT-3 receptor. Preparation of the 3-tri-n-butylstannyl precursor was accomplished from the corresponding unlabeled DAIZAC by reaction with bis(tributy1tin). Treatment of the precursor with 5 mCi of Na125I and chloramine-T in dilute HCl gave 2.58 f 0.22 mCi (52%) of [l25IIDAIZAC with >98% radiochemical purity and 1500 Ci/mmol specific activity. Saturation analysis of the binding of [125I]DAIZAC to rat brain homogenates showed a single binding site with a receptor density Em, of 0.66 f 0.03 pmol/g and a receptor affinity KD of 0.15 f 0.01 nM. Compared to [ 1254iodozacopride, we find the 20-fold higher affinity and easy preparation of [ 1251]DAIZAC to be advantageous for in vitro identification of brain 5-HT-3 receptors.

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