2-[18F]F-A85380:: PET imaging of brain nicotinic acetylcholine receptors and whole body distribution in humans

被引：97

作者：

Kimes, AS

Horti, AG

London, ED

Chefer, SI

Contoreggi, C

Ernst, M

Friello, P

Koren, AO

Kurian, V

Matochik, JA

Pavlova, O

Vaupel, DB

Mukhin, AG

机构：

[1] NIDA, Intramural Res Program, Neuroimaging Res Branch, Baltimore, MD 21224 USA

[2] Univ Calif Los Angeles, David Geffen Sch Med, Inst Neuropsychiat, Los Angeles, CA USA

[3] NIMH, Intramural Res Program, Bethesda, MD 20892 USA

来源：

FASEB JOURNAL | 2003年 / 17卷 / 08期

关键词：

dosimetry; smoking; Alzheimer's disease; Parkinson's disease; non-invasive imaging;

D O I：

10.1096/fj.02-0492fje

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Noninvasive imaging of nicotinic acetylcholine receptors (nAChRs) in the human brain in vivo is critical for elucidating the role of these receptors in normal brain function and in the pathogenesis of brain disorders. Here we report the first in vivo visualization of human brain areas containing nAChRs by using PET and 2-[F-18]fluoro-3-(2(S)azetidinylmethoxy)pyridine (2-[F-18]FA). We acquired scans from six healthy non-smoking volunteers after i.v. bolus administration of 2-[F-18]FA (1.6 MBq/kg or 0.043 +/- 0.002 mCi/kg). This dose was sufficient for visualizing nAChRs in the thalamus up to 5 h after injection. There were no adverse effects associated with administration of no-carrier-added 2-[F-18]FA (1.3-10 pmol/kg). Consistent with the distribution of nAChRs in human brain, accumulated radioactivity was greatest in thalamus, intermediate in the midbrain, pons, cerebellum, and cortex; and least in white matter. As similar to90% of the injected radioactivity was eliminated via the urine (biological half-life ca. 4 h), the urinary bladder wall received the highest radiation dose. The estimate of radiation dose equivalent to the urinary bladder wall (ca. 180 +/- 30 mSv/MBq or 0.7 rem/mCi with a 2.4 h void interval) suggests that multiple studies could be performed in a single subject. The results predict that quantitative PET imaging of nAChRs in human brain with 2-[F-18]FA is feasible.

引用

页码：1331 / +

页数：17

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