|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
4
|
|
pubmed:dateCreated |
2002-5-28
|
|
pubmed:abstractText |
The properties of two prospective positron emission tomography (PET) ligands for the delta-opioid receptor, N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) were investigated. Both were antagonists in the mouse vas deferens, and showed high affinity and selectivity, 1.81 nM and 3.09 nM respectively. [3H]BU97001 binding to rat whole brain was also of high affinity, K(D) of 0.42 nM of and B(MAX) of 59.95 fmol mg of protein(-1). In autoradiographic studies, it was found to bind to brain areas previously shown to be associated with the delta-opioid receptor and good correlations were found to exist with naltrindole and DPDPE. BU97018 and especially BU97001 appear to show good potential as delta-opioid receptor PET ligands with the incorporation of 18F.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
May
|
|
pubmed:issn |
0969-8051
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:volume |
29
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
455-62
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:12031880-Animals,
pubmed-meshheading:12031880-Autoradiography,
pubmed-meshheading:12031880-Binding Sites,
pubmed-meshheading:12031880-Brain,
pubmed-meshheading:12031880-Dose-Response Relationship, Drug,
pubmed-meshheading:12031880-Enkephalin, D-Penicillamine (2,5)-,
pubmed-meshheading:12031880-Male,
pubmed-meshheading:12031880-Mice,
pubmed-meshheading:12031880-Naltrexone,
pubmed-meshheading:12031880-Radiopharmaceuticals,
pubmed-meshheading:12031880-Rats,
pubmed-meshheading:12031880-Rats, Wistar,
pubmed-meshheading:12031880-Receptors, Opioid, delta,
pubmed-meshheading:12031880-Sensitivity and Specificity,
pubmed-meshheading:12031880-Vas Deferens
|
|
pubmed:year |
2002
|
|
pubmed:articleTitle |
N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) potential delta-opioid receptor PET ligands.
|
|
pubmed:affiliation |
Psychopharmacology Unit, School of Medical Sciences, University of Bristol, UK.
|
|
pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|
