Radiosynthesis and preliminary evaluation of 5-[123/125I]iodo3-(2(S)-azetidinylmethoxy)pyridine:: A radioligand for nicotinic acetylcholine receptors

被引：44

作者：

Horti, AG

Koren, AO

Lee, KS

Mukhin, AG

Vaupel, DB

Kimes, AS

Stratton, M

London, ED

机构：

[1] NIDA, Brain Imaging Ctr, Intramural Res Program, Baltimore, MD 21224 USA

[2] NIMH, Clin Brain Disorders Branch, Washington, DC 20032 USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 1999年 / 26卷 / 02期

关键词：

radiotracer; A-85380; I-123; I-125; radioiodination; nicotinic receptors; acetylcholine; receptor binding; SPECT;

D O I：

10.1016/S0969-8051(98)00086-9

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

The radiochemical syntheses of 5-[I-125]iodo-3-(2 (S)-azetidinylmethoxy)pyridine (5-[I-125]iodo-A-85380, [I-125]1) and 5-[I-123]-iodo-A-85380, [I-123]1, were accomplished by radioiodination of 5-trimethylstannyl-3-( (1-tert-butoxycarbonyl-2 (S)-azetidinyl)methoxy)pyridine, 2, followed by acidic deprotection. Average radiochemical yields of [I-125]1 and [I-123]1 were 40-55%; and the average specific radioactivities were 1,700 and 7,000 mCi/mu mol, respectively. Binding affinities of [I-125]1 and [I-123]1 in vitro (rat brain membranes) were each characterized by a K-d value of 11 pM. Preliminary in vivo assay and ex vivo autoradiography of mouse brain indicated that [I-125]1 selectively labels nicotinic acetylcholine receptors (nAChRs) with very high affinity and specificity. These studies suggest that [I-123]1 may be useful as a radioligand for single photon emission computed tomography (SPECT) imaging of nAChRs. NUCL MED BIOL 26;2:175-182, 1999. Published by Elsevier Science Inc.

引用

页码：175 / 182

页数：8

共 44 条

[1] Novel 3-pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors [J].