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Synthesis of a radiotracer for studying serotonin uptake sites with positron emission tomography: [11C]McN-5652-Z

✍ Scribed by Makiko Suehiro; Hayden T. Ravert; Robert F. Dannals; Ursula Scheffel; Henry N. Wagner Jr.

Publisher
John Wiley and Sons
Year
1992
Tongue
French
Weight
422 KB
Volume
31
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The highly potent serotonin (5‐HT) uptake blocker, McN‐5652‐Z (trans‐1,2,3,5,6,10b ‐ hexahydro ‐ 6 ‐ [4 ‐ (methylthio)phenyl] pyrrolo ‐ [2,1‐a]‐isoquinoline) was labeled with ^11^C for studying serotonin uptake sites using positron emission tomography (PET). [^11^C]McN‐5652‐Z was synthesized by S‐methylation of the normethyl precursor with [^11^C]iodomethane in DMF at 30 ‐ 35° C. The radiosyntheses including purification by HPLC and formulation for injection were completed in an average of 16 minutes following the end of bombardment (E.O.B.) with an overall radiochemical yield of 12%. The average specific activity determined at the end of synthesis (E.O.S.) was approximately 4250 mCi/μmole; this corresponds to approximately 7350 mCi/μmole at E.O.B. [^11^C]McN‐5655‐Z, a less potent blocker, was also prepared by the same procedure.

📜 SIMILAR VOLUMES

Synthesis of a radiotracer for studying
Synthesis of a radiotracer for studying dopamine uptake sites in vivo using PET: 2β-carbomethoxy-3β-(4-fluorophenyl)-[N-11C-methyl]tropane ([11C]CFT or [11C]WIN-35,428)
✍ Robert F. Dannals; John L. Neumeyer; Richard A. Milius; Hayden T. Ravert; Alan A 📂 Article 📅 1993 🏛 John Wiley and Sons 🌐 French ⚖ 320 KB

## Abstract 2β‐Carbomethoxy‐3β‐(4‐fluorophenyl)‐[N‐^11^C‐methyl]tropane, a potent inhibitor of dopamine transport, was prepared by N‐methylation of the appropriate nor‐methyl precursor in DMF with [^11^C]iodomethane. After derivatization of unreacted precursor with a long chain acyl halide, the rad