Document Detail


In vitro and in vivo testing of the dopamine D1 ligand [123I]SCH 23982 with respect to its potential application in SPET investigations.
MedLine Citation:
PMID:  8358346     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
[123I]SCH 23982, a dopamine D1 ligand, was labelled in a large scale process and then tested in vitro for binding to rat brain sections and membranes. Because of the promising values of KD = 1.5 x 10(-10) M and Bmax = 0.7 x 10(-11) mol/g, in vivo evaluation was performed on rats and normal volunteers to test its possible usefulness for SPET imaging. In competition experiments, a higher binding in the presence of sulpiride was found while ketanserin displaced [123I]SCH 23982 only at a 10,000-fold excess. Differences between rats and men were seen with respect to their metabolism. SPET investigations failed because the washout of [123I]SCH 23982 was too rapid.
Authors:
H F Beer; S Lin; P Bläuenstein; P Hasler; P A Schubiger; A Maier; W Lichtensteiger; R Oettli; A Bekier; B Weder
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Nuclear medicine and biology     Volume:  20     ISSN:  0969-8051     ISO Abbreviation:  Nucl. Med. Biol.     Publication Date:  1993 Jul 
Date Detail:
Created Date:  1993-09-27     Completed Date:  1993-09-27     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9304420     Medline TA:  Nucl Med Biol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  607-16     Citation Subset:  IM    
Affiliation:
Division of Radiopharmacy, Paul Scherrer Institute, Villigen, Switzerland.
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MeSH Terms
Descriptor/Qualifier:
Aged
Animals
Benzazepines / analogs & derivatives*,  diagnostic use,  metabolism,  pharmacokinetics
Female
Humans
Iodine Radioisotopes
Male
Middle Aged
Rats
Rats, Wistar
Receptors, Dopamine D1 / antagonists & inhibitors*
Tissue Distribution
Tomography, Emission-Computed, Single-Photon / methods*
Chemical
Reg. No./Substance:
0/8-iodo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol; 0/Benzazepines; 0/Iodine Radioisotopes; 0/Receptors, Dopamine D1

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


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