Document Detail


Synthesis and in vivo evaluation of 122I- and 131I-labelled iodoperidol, a potential agent for the tomographic assessment of cerebral perfusion.
MedLine Citation:
PMID:  3484351     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Iodoperidol (IP), an iodinated analogue of the antipsychotic drug haloperiodol, was evaluated as a cerebral blood flow radiopharmaceutical for PET or SPECT. IP was labelled with 131I or 122I (76% beta +, t1/2 = 3.6 min) in greater than 75% radiochemical yield via electrophilic aromatic iododestannylation. [131I]IP showed high cerebral uptake (1.9% of injected dose after 5 min) and good brain retention for the rat, with very low blood levels (brain/blood ratio = 35 at 2 h post injection). PET imaging of a dog demonstrated that [122I]IP has high selectivity for brain localization and good retention, and indicates that this class of compounds holds promise for development as perfusion radiopharmaceuticals.
Authors:
S M Moerlein; C A Mathis; K M Brennan; T F Budinger
Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology     Volume:  14     ISSN:  0883-2897     ISO Abbreviation:  Int J Rad Appl Instrum B     Publication Date:  1987  
Date Detail:
Created Date:  1987-08-19     Completed Date:  1987-08-19     Revised Date:  2008-02-21    
Medline Journal Info:
Nlm Unique ID:  8611098     Medline TA:  Int J Rad Appl Instrum B     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  91-8     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Brain / radionuclide imaging*
Cerebrovascular Circulation
Dogs
Female
Haloperidol / analogs & derivatives*,  chemical synthesis,  diagnostic use
Iodine Radioisotopes / diagnostic use*
Magnetic Resonance Spectroscopy
Rats
Rats, Inbred Strains
Tissue Distribution
Grant Support
ID/Acronym/Agency:
P01 HL25840/HL/NHLBI NIH HHS; R01 NS22899/NS/NINDS NIH HHS; S07 RR05918/RR/NCRR NIH HHS
Chemical
Reg. No./Substance:
0/Iodine Radioisotopes; 109852-09-7/iodoperidol; 52-86-8/Haloperidol

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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