Synthesis of a dopamine uptake inhibitor for PET studies: 1-[1-(2-benzo(b)thiophenyl)cyclohexyl]-4-(2-[18F]fluoroethyl) piperazine
✍ Scribed by I. Loustau-Then; M. Ponchant; J. M. Kamenka; C. Crouzel
- Publisher
- John Wiley and Sons
- Year
- 1996
- Tongue
- French
- Weight
- 415 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
The BTCP derivative l-[l-(2-benzo(b)thiophenyl) cyclohexyll-4-(2-hydroxyethyl) piperazine 2 showed, in uitro, high affinity and selectivity for the Dopamine transporter. In order to evaluate the potential of such a compound as an imaging tool for studying the dopaminergic system by Positron Emission Tomography (PET) the cold fluoroethyl BTCP piperazine 6 was synthesized. After checking the biological activity of the cold compound a , the analogue 1 was synthesized. The radiosynthesis was carried out by the nucleophilic substitution of 1-[1-(2-benzo(b)thiophenyl) cyclohexyll-4-(2-chloroethyl) piperazine fi with cyclotron-produced n.c.a. 18F-, obtained by the (p,n) reaction on l80 enriched water.