Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1-2
|
| pubmed:dateCreated |
1994-10-10
|
| pubmed:abstractText |
In a human astrocytoma cell line U373 MG, the activation of the neurokinin 1 (NK1) receptor by substance P (SP) increase, in a concentration-related manner (1 nM to 10 microM), the basal release of interleukin-6 (IL-6) as assayed by an ELISA method, in cell supernatants after 18 h of incubation. Septide, a selective NK1 receptor agonist, is equipotent to SP in inducing the IL-6 release showing similar Emax (2644 +/- 285 and 2830 +/- 271 pg/ml) and EC50 (15.6 +/- 3.6 and 13.8 +/- 3.2 nM). However, in binding assays on intact cells, septide was an about 50-fold weaker displacer of the binding of [3H][Sar9,Met(O2)11]SP than SP (Ki's were 0.28 +/- 0.1 nM and 14.2 +/- 5.0 nM for SP and septide, respectively). NK2- and NK3-selective agonists (up to 1 microM) had no binding or functional effect. Highly selective non-peptide (CP96,345) or peptide (GR82,334) NK1 receptor antagonists were more effective in antagonizing septide-(IC50's 0.2 +/- 0.06 nM and 70 +/- 18 nM) than SP-(IC50's 6.7 +/- 1.3 nM and 1.95 +/- 0.4 microM) induced IL-6 secretion. These data support the existence, also in human U373 MG cells, of a septide-sensitive NK1 receptor subtype(s) and/or epitope(s) blocked with high affinity by NK1 antagonist.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Interleukin-6,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrrolidonecarboxylic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neurokinin-1,
http://linkedlifedata.com/resource/pubmed/chemical/Substance P,
http://linkedlifedata.com/resource/pubmed/chemical/septide
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Apr
|
| pubmed:issn |
0304-3940
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
25
|
| pubmed:volume |
171
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
221-4
|
| pubmed:dateRevised |
2004-11-17
|
| pubmed:meshHeading |
pubmed-meshheading:7521949-Astrocytoma,
pubmed-meshheading:7521949-Binding, Competitive,
pubmed-meshheading:7521949-Brain Neoplasms,
pubmed-meshheading:7521949-Humans,
pubmed-meshheading:7521949-Interleukin-6,
pubmed-meshheading:7521949-Peptide Fragments,
pubmed-meshheading:7521949-Pyrrolidonecarboxylic Acid,
pubmed-meshheading:7521949-Receptors, Neurokinin-1,
pubmed-meshheading:7521949-Substance P,
pubmed-meshheading:7521949-Tumor Cells, Cultured
|
| pubmed:year |
1994
|
| pubmed:articleTitle |
Different susceptibility to neurokinin 1 receptor antagonists of substance P and septide-induced interleukin-6 release from U373 MG human astrocytoma cell line.
|
| pubmed:affiliation |
Menarini Ricerche Sud, Pharmacology Department, Pomezia, Roma, Italy.
|
| pubmed:publicationType |
Journal Article
|