5-HT transporter

Soudijn, W.; Wijngaarden, I. Van

doi:10.1016/s0165-7208(97)80019-0

Cited by 3 publications

(1 citation statement)

References 93 publications

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“…In search of an improved ligand for SERTs, many compounds have been evaluated (Chart ). − Among these tracers, only [ 123 I]5-iodo-6-nitroquipazine (INQP) − showed promising properties for mapping SERT sites in monkey's brain . No human study of [ 123 I]INQP has been reported.…”

Section: Introductionmentioning

confidence: 99%

New PET Imaging Agent for the Serotonin Transporter: [¹⁸F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)

et al. 2002

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A new F-18-labeled phenylthiophenyl derivative specific for imaging of serotonin transporters (SERT) in the brain by positron emission tomography (PET) is described. Fluorinated phenylthiophenyl derivative, ACF, 2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine, was prepared by first coupling 2,5-dichloro-4-nitroaniline with 2-mercapto-N,N-dimethylbenzamide. The amino group of the coupled adduct was converted to a fluoro group through a Schiemann reaction. Subsequently, a one pot reduction of both nitro and amide groups by BH(3)-tetrahydrofuran yielded the nonradioactive ACF (yield 25%). In vitro binding assays using cell membrane homogenates of LLC cells expressing SERT, dopamine transporters (DAT), or norepinephrine transporters (NET) showed excellent binding affinity and selectivity for SERT (K(i) = 0.05, 3020, and 650 nM for SERT, DAT, and NET, respectively). For preparation of the [(18)F]ACF, the NH(2) group of the initially coupled adduct was converted to the trimethylammonium salt, which was replaced by [(18)F]fluoride in the presence of Kryptofix 222 and potassium carbonate. The final product, [(18)F]ACF, was obtained after a borane and stannous chloride reduction reaction. The combined two step reaction gave a radiochemical yield of 10-15% (EOB) and a radiochemical purity of >99%. Synthesis of the novel PET tracer, [(18)F]ACF, as a probe for binding to SERT in the brain was successfully achieved. The new tracer [(18)F]ACF showed excellent brain penetration and selective localization after an iv injection in rats (brain uptake at 2, 30, 60, 120, and 240 min was 3.27, 1.28, 0.69, 0.21, and 0.06% dose/organ, respectively). The hypothalamus/cerebellum ratio at 60 min post iv injection was 3.55. This specific localization in the hypothalamus was blocked by pretreatment of (+)McN5652. This novel ligand is a potential PET tracer for in vivo evaluation of SERT in the brain.

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Section: Introductionmentioning

confidence: 99%

New PET Imaging Agent for the Serotonin Transporter: [¹⁸F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)

et al. 2002

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A novel serotonin transporter ligand: (5-Iodo-2-(2-dimethylaminomethylphenoxy)-benzyl alcohol

Zhuang

Choi

Hou

et al. 2000

Nuclear Medicine and Biology

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A putative three-dimensional arrangement of the human serotonin transporter transmembrane helices: a tool to aid experimental studies

Ravna

Edvardsen

2001

Journal of Molecular Graphics and Modelling

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5-HT transporter

Cited by 3 publications

References 93 publications

New PET Imaging Agent for the Serotonin Transporter: [¹⁸F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)

New PET Imaging Agent for the Serotonin Transporter: [¹⁸F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)

A novel serotonin transporter ligand: (5-Iodo-2-(2-dimethylaminomethylphenoxy)-benzyl alcohol

A putative three-dimensional arrangement of the human serotonin transporter transmembrane helices: a tool to aid experimental studies

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5-HT transporter

Cited by 3 publications

References 93 publications

New PET Imaging Agent for the Serotonin Transporter: [18F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)

New PET Imaging Agent for the Serotonin Transporter: [18F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)

A novel serotonin transporter ligand: (5-Iodo-2-(2-dimethylaminomethylphenoxy)-benzyl alcohol

A putative three-dimensional arrangement of the human serotonin transporter transmembrane helices: a tool to aid experimental studies

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New PET Imaging Agent for the Serotonin Transporter: [¹⁸F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)

New PET Imaging Agent for the Serotonin Transporter: [¹⁸F]ACF (2-[(2-Amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine)