Discovery of Novel Conformationally Constrained Tropane‐Based Biaryl and Arylacetylene Ligands as Potent and Selective Norepinephrine Transporter Inhibitors and Potential Antidepressants.

Zhou, Jia; Klaess, Thomas; Johnson, Kenneth M.; Giberson, Kelly M.; Kozikowski, Alan P.

doi:10.1002/chin.200538199

Search citation statements

Order By: Relevance

Paper Sections

Select...

Norepinephrine Transporter (Net)1

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2009

Publication Types

Select...

Article1

Relationship

Self Cite0

Independent1

Authors

Journals

Cited by 1 publication

(1 citation statement)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…[289–294] Preliminary microPET evaluation of a 11 C-labeled NET tropane derivative showed both SERT and NET binding and, therefore, a lack of NET selectivity. [295] The NET ligands talopram[296] and talsupram have been radiolabeled with 11 C and evaluated with PET but neither compound entered the brain in sufficient amounts to become a viable PET tracer.…”

Section: Norepinephrine Transporter (Net)mentioning

confidence: 99%

Fluorine-18 Radiolabeled PET Tracers for Imaging Monoamine Transporters: Dopamine, Serotonin, and Norepinephrine

Stehouwer

Goodman

2009

PET Clinics

View full text Add to dashboard Cite

SynopsisThis review focuses on the development of fluorine-18 radiolabeled PET tracers for imaging the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET). All successful DAT PET tracers reported to date are members of the 3β-phenyl tropane class and are synthesized from cocaine. Currently available carbon-11 SERT PET tracers come from both the diphenylsulfide and 3β-phenyl nortropane class, but so far only the nortropanes have found success with fluorine-18 derivatives. NET imaging has so far employed carbon-11 and fluorine-18 derivatives of reboxetine but due to defluorination of the fluorine-18 derivatives further research is still necessary.

show abstract