Abstract：
:Three new radiolabeled compounds, [(11)C]SNC80 ((+)-4-[(αR)-α-{(2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl}-3-[(11)C]methoxybenzyl-N,N-diethylbenzamide), N,N-diethyl-4-[3-methoxyphenyl-1-[(11)C]methylpiperidin-4-ylidenemethyl)benzamide and N,N-diethyl-4-[(1-[(11)C]methylpiperidin-4-ylidene)phenylmethyl]benzamide, were prepared as potential in vivo radiotracers for the δ-opioid receptor. Each compound was synthesized by alkylation of the appropriate desmethyl compounds using [(11)C]methyl triflate. In vivo biodistribution studies in mice showed very low initial brain uptake of all three compounds and no regional specific binding for [(11)C]SNC80. A monkey positron emission tomography study of [(11)C]SNC80 confirmed low brain permeability and uniform regional distribution of this class of opioid agonists in a higher species. Opioid receptor ligands of this structural class are thus unlikely to succeed as in vivo radiotracers, likely due to efficient exclusion from the brain by the P-glycoprotein efflux transporter.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Pichika R,Jewett DM,Sherman PS,Traynor JR,Husbands SM,Woods JH,Kilbourn MRdoi
10.1016/j.nucmedbio.2010.06.002subject
Has Abstractpub_date
2010-11-01 00:00:00pages
989-96issue
8eissn
0969-8051issn
1872-9614pii
S0969-8051(10)00307-0journal_volume
37pub_type
杂志文章abstract：:By variation of reaction parameters iodination of 3-(9,10-didehydro-6-methyl-8 alpha-ergolinyl)-1,1-diethylurea (lisuride) was performed with the radiohalogen [123I]iodine (t1/2 = 13.3 h). For comparative experiments and stability studies the beta(-)-emitting radioisotope [131I]iodine (t1/2 = 8.04 d) was also used. Re...
journal_title：Nuclear medicine and biology
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journal_title：Nuclear medicine and biology
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journal_title：Nuclear medicine and biology
pub_type： 杂志文章
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pub_type： 杂志文章
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更新日期：2003-02-01 00:00:00
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pub_type： 杂志文章
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更新日期：2000-08-01 00:00:00
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pub_type： 杂志文章
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journal_title：Nuclear medicine and biology
pub_type： 杂志文章
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更新日期：2016-06-01 00:00:00
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doi：10.1016/s0969-8051(01)00253-0
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更新日期：2007-01-01 00:00:00
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更新日期：1998-10-01 00:00:00
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更新日期：2009-02-01 00:00:00
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journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2008.07.001
更新日期：2008-10-01 00:00:00
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doi：10.1016/j.nucmedbio.2012.12.004
更新日期：2013-05-01 00:00:00
abstract：:Quantification of alpha(4)beta(2)* nicotinic acetylcholine receptors using 2-[(18)F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[(18)F]FA) and positron emission tomography (PET) imaging requires measurement of nonmetabolized radioligand in blood plasma, which was previously accomplished using high-performance liquid ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2006.12.001
更新日期：2007-02-01 00:00:00
abstract：INTRODUCTION:Nanoscale perfluorocarbon (PFC) droplets have been used to create imaging agents and drug delivery vehicles. However, development and characterization of new formulations of PFC droplets are hindered because of the lack of simple methods for quantitative and sensitive assessment of whole body tissue distri...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2017.07.001
更新日期：2017-11-01 00:00:00
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journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2008.02.011
更新日期：2008-05-01 00:00:00
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journal_title：Nuclear medicine and biology
pub_type： 临床试验,杂志文章
doi：10.1016/j.nucmedbio.2003.10.005
更新日期：2004-04-01 00:00:00
abstract：INTRODUCTION:Thermal neutron activation of 152Sm [152Sm(n,γ)153Sm] using natural or isotopically enriched (by 152Sm) samarium target is the established route for production of 153Sm used for preparation of 153Sm-EDTMP for pain palliation in cancer patients with disseminated bone metastases. However, some long-lived rad...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2017.11.010
更新日期：2018-03-01 00:00:00
abstract：:The chemical purity and stability of a radio pharmaceutical 99mTc-N-(2,6-diethyl-3-iodo-phenylcarbamoylmethyl)-iminodiacetic acid (IODIDA) has been studied using HPLC. The HPLC results indicate that IODIDA decomposed into at least three species after 99mTc labelling, and the amount of these varied with time. Mass spec...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(94)00120-9
更新日期：1995-05-01 00:00:00
abstract：INTRODUCTION:3'-Deoxy-3'-[(18)F]fluorothymidine ([(18)F]FLT) shows great potential as a tracer for proliferative studies with PET. However, its regular application is often limited by low radiochemical yields and the use of a troublesome HPLC separation. Moreover, a high content of ethanol, at least one-fold higher tha...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2011.10.005
更新日期：2012-05-01 00:00:00
abstract：INTRODUCTION:Nuclear and optical imaging are complementary in many aspects and there would be many advantages when optical imaging probes are prepared using radionuclides rather than classic fluorophores, and when nuclear and optical dual images are obtained using single imaging probe. METHODS:The luminescence intensi...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2010.09.003
更新日期：2011-04-01 00:00:00
abstract：INTRODUCTION:Comparative imaging of multiple radiotracers in the same animal can be invaluable in elucidating and validating their respective mechanisms of localization. Comparative imaging of PET tracers, particularly in small animals, is problematic, however: such tracers must be administered and imaged separately be...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2005.07.011
更新日期：2006-01-01 00:00:00
abstract：INTRODUCTION:Choline, acetate and glucose ([2-(18)F]fluoro-2-deoxyglucose, [(18)F]FDG) analogs are under investigation as positron emission tomography (PET) tracers for the imaging of prostate cancer; however, their response to tumor hypoxia has not been clarified. METHODS:The uptake of [methyl-(3)H]choline, [1-(14)C]...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2006.08.002
更新日期：2006-11-01 00:00:00
