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New and convenient synthesis of a tritiated photoactivatable nicotinic agonist: [3H]–AC5

✍ Scribed by A. Mourot; F. Kotzyba-Hibert; E. Doris; M. Goeldner

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
160 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A new synthesis of a tritiated photosensitive nicotinic agonist ([^3^H]–AC5), which uses [^3^H~2~] as the source of radioactivity, is described. Several improvements have been introduced to establish a reliable five‐step synthesis displaying satisfactory overall yields (45%) and requiring a single purification (HPLC) in the final step. This photosensitive radiolabelled probe will enable us to undertake a time‐resolved photolabelling study on the nicotinic acetylcholine receptor in order to analyze at the molecular level the allosteric transitions occurring after agonist stimulation. Copyright © 2002 John Wiley & Sons, Ltd.

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