Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
|
pubmed:dateCreated |
1996-9-19
|
pubmed:abstractText |
There is evidence that neuropeptide FF (NPFF) has antiopiate activity and may play a role in opiate dependence and subsequent abstinence syndrome. A fragment of NPFF was modified at the C-terminal in an effort to convert it to an NPFF antagonist. It was also dansylated at the N-terminal in an effort to render it more lipophilic and increase its penetration of the blood-brain barrier. Third ventricle administration of the resulting compound, dansyl-PQRamide (0.75 microgram and 1 microgram), dose-dependently antagonized the quasi-morphine abstinence activity of NPFF (10 micrograms) in opiate-naive rats. Subcutaneous injection of dansyl-PQRamide (13 mg/kg) in chronically morphine-infused rats attenuated opiate dependence as indicated by prevention of naloxone-precipitated abstinence syndrome. Dansyl-PQRamide displaced radiolabelled ligand from NPFF receptors in a concentration-dependent manner with a Ki of 13 microM, and had a half-life over 300 times longer than NPFF under aminopeptidase digestion.
|
pubmed:grant | |
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Dansyl Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Naloxone,
http://linkedlifedata.com/resource/pubmed/chemical/Narcotic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/phenylalanyl-leucyl-phenylalanyl-glu...
|
pubmed:status |
MEDLINE
|
pubmed:month |
Nov
|
pubmed:issn |
0376-8716
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
40
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
N
|
pubmed:pagination |
37-42
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:8746922-Animals,
pubmed-meshheading:8746922-Dansyl Compounds,
pubmed-meshheading:8746922-Dose-Response Relationship, Drug,
pubmed-meshheading:8746922-Injections, Intraventricular,
pubmed-meshheading:8746922-Injections, Subcutaneous,
pubmed-meshheading:8746922-Male,
pubmed-meshheading:8746922-Morphine Dependence,
pubmed-meshheading:8746922-Naloxone,
pubmed-meshheading:8746922-Narcotic Antagonists,
pubmed-meshheading:8746922-Neurologic Examination,
pubmed-meshheading:8746922-Oligopeptides,
pubmed-meshheading:8746922-Rats,
pubmed-meshheading:8746922-Rats, Sprague-Dawley,
pubmed-meshheading:8746922-Structure-Activity Relationship,
pubmed-meshheading:8746922-Substance Withdrawal Syndrome
|
pubmed:year |
1995
|
pubmed:articleTitle |
Subcutaneous injection of an analog of neuropeptide FF prevents naloxone-precipitated morphine abstinence syndrome.
|
pubmed:affiliation |
University of Houston-Clear Lake, TX 77058, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
|