Linked Life Data

16190770

Source:http://linkedlifedata.com/resource/pubmed/id/16190770

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
20
pubmed:dateCreated
2005-9-29
pubmed:abstractText
In previous studies we demonstrated that lipophilic (99m)Tc-labeled LTB4 antagonist 1 (RP517) accumulated in infectious foci in rabbits, but hepatobiliary clearance hampered imaging of abdominal lesions. We now report the use of cysteic acid as a pharmacokinetic modifier to improve the water solubility and renal clearance of three hydrophilic analogues of 1. Divalent LTB4 antagonist 17 (DPC11870-11) is a DTPA conjugate for radiolabeling with In-111. Monovalent LTB4 antagonists 15 (BMS57868-88) and divalent LTB4 antagonist 18 (BMS57868-81) are conjugated to bifunctional chelator HYNIC for radiolabeling with (99m)Tc. The three compounds labeled efficiently with 111In or (99m)Tc with high radiochemical purity and specific activities. Scintigraphic images obtained in New Zealand White rabbits having acute intramuscular E. coli infection demonstrated that all agents were able to clearly visualize the abscess, and clearance was exclusively renal. The biodistribution of the (99m)Tc-labeled LTB4 antagonists was affected by the coligands used with the HYNIC chelator and by the monovalent or divalent nature of the receptor binding moiety. The best scintigraphic images were obtained with monovalent HYNIC conjugate 15 using tricine and isonicotinic acid as coligands with HYNIC for coordination with (99m)Tc.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
6
pubmed:volume
48
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
6442-53
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:16190770-Abscess, pubmed-meshheading:16190770-Animals, pubmed-meshheading:16190770-Binding, Competitive, pubmed-meshheading:16190770-Chelating Agents, pubmed-meshheading:16190770-Escherichia coli Infections, pubmed-meshheading:16190770-Female, pubmed-meshheading:16190770-Glycine, pubmed-meshheading:16190770-Granulocytes, pubmed-meshheading:16190770-Humans, pubmed-meshheading:16190770-Hydrazines, pubmed-meshheading:16190770-Indium Radioisotopes, pubmed-meshheading:16190770-Isonicotinic Acids, pubmed-meshheading:16190770-Isotope Labeling, pubmed-meshheading:16190770-Leukotriene B4, pubmed-meshheading:16190770-Muscle, Skeletal, pubmed-meshheading:16190770-Nicotinic Acids, pubmed-meshheading:16190770-Organotechnetium Compounds, pubmed-meshheading:16190770-Rabbits, pubmed-meshheading:16190770-Radioligand Assay, pubmed-meshheading:16190770-Radiopharmaceuticals, pubmed-meshheading:16190770-Solubility, pubmed-meshheading:16190770-Structure-Activity Relationship, pubmed-meshheading:16190770-Tissue Distribution
pubmed:year
2005
pubmed:articleTitle
Synthesis of leukotriene B4 antagonists labeled with In-111 or Tc-99m to image infectious and inflammatory foci.
pubmed:affiliation
Bristol-Myers Squibb Medical Imaging, North Billerica, Massachusetts 01862, USA.
pubmed:publicationType
Journal Article, In Vitro