当前位置： SCI文献检索 > NUCLEAR MEDICINE AND BIOLOGY期刊下所有文献 > Re-evaluation of in vivo selectivity of [(11)C]SA4503 to σ(1) receptors in the brain: contributions of emopamil binding protein.

Re-evaluation of in vivo selectivity of [(11)C]SA4503 to σ(1) receptors in the brain: contributions of emopamil binding protein.

Abstract：

INTRODUCTION:Carbon-11-labeled 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine ([(11)C]SA4503) was shown to be a promising PET ligand for mapping σ(1) receptors, and was applied to human subjects. However, an in vitro study indicated that SA4503 also binds to the emopamil binding protein (EBP), vertebral Δ8-Δ7 sterol isomerase. To our knowledge, no information is available about the possibility of [(11)C]SA4503 binding to EBP in the brain in vivo. METHODS:To confirm the selectivity of [(11)C]SA4503, we carried out an in vivo blocking experiment using high-affinity EBP and σ(1) selective blocker. RESULTS:The brain uptake of [(11)C]SA4503 was dose-dependently decreased by SA4503 and the high-affinity σ(1) blockers haloperidol, ifenprodil, and trifluperidol. On the other hand, the effects of the high-affinity EBP blockers tamoxifen and trifluoperazine were negligible. CONCLUSIONS:Our results confirmed the σ(1)-selective binding of [(11)C]SA4503 in the brain.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Toyohara J,Sakata M,Ishiwata K

doi

10.1016/j.nucmedbio.2012.03.002

subject

Has Abstract

pub_date

2012-10-01 00:00:00

pages

1049-52

issue

7

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(12)00053-4

journal_volume

39

pub_type

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