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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
5
|
| pubmed:dateCreated |
1988-10-13
|
| pubmed:abstractText |
1. The binding characteristics of [3H]ICS 205-930, a potent and selective 5-hydroxytryptamine 5-HT3 receptor antagonist, were investigated in membranes prepared from murine neuroblastoma-glioma NG 108-15 cells. 2. [3H]ICS 205-930 bound rapidly, reversibly and stereoselectively to a homogeneous population of high affinity recognition sites: Bmax = 58 +/- 3 fmol/mg protein, pKD = 9.01 +/- 0.08 (n = 11). Non linear regression and Scatchard analysis of saturation data suggested the existence of a single class of [3H]ICS 205-930 recognition sites on NG 108-15 cells. The binding was rapid, stable and reversible. The affinity of [3H]ICS 205-930 determined in kinetic studies was in agreement with that obtained under equilibrium conditions. 3. Competition studies performed with a variety of agonists and antagonists also suggested the presence of a homogeneous population of [3H]ICS 205-930 recognition sites. All competition curves were steep and monophasic and were best fit by a 1 receptor site model. [3H]ICS 205-930 binding sites displayed the pharmacological profile of a 5-HT3 receptor. Potent 5-HT3 receptor antagonists showed nanomolar affinities for [3H]ICS 205-930 binding sites with the following rank order of potency: SDZ 206-830 greater than ICS 205-930 greater than SDZ 206-792 greater than BRL 43694 greater than quipazine greater than BRL 24924 greater than SDZ 210-204 greater than MDL 72222 greater than SDZ 210-205. Metoclopramide, mCP and mianserin showed submicromolar affinity.(ABSTRACT TRUNCATED AT 250 WORDS)
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Nucleotides,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/tropisetron
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
May
|
| pubmed:issn |
0028-1298
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
337
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
493-9
|
| pubmed:dateRevised |
2003-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:3412489-Animals,
pubmed-meshheading:3412489-Binding, Competitive,
pubmed-meshheading:3412489-Cell Membrane,
pubmed-meshheading:3412489-Glioma,
pubmed-meshheading:3412489-Indoles,
pubmed-meshheading:3412489-Kinetics,
pubmed-meshheading:3412489-Mice,
pubmed-meshheading:3412489-Neuroblastoma,
pubmed-meshheading:3412489-Nucleotides,
pubmed-meshheading:3412489-Radioligand Assay,
pubmed-meshheading:3412489-Receptors, Serotonin,
pubmed-meshheading:3412489-Serotonin Antagonists,
pubmed-meshheading:3412489-Stereoisomerism,
pubmed-meshheading:3412489-Temperature,
pubmed-meshheading:3412489-Tumor Cells, Cultured
|
| pubmed:year |
1988
|
| pubmed:articleTitle |
Characterisation of 5-HT3 recognition sites in membranes of NG 108-15 neuroblastoma-glioma cells with [3H]ICS 205-930.
|
| pubmed:affiliation |
Department of Veterinary Pharmacology, Pharmacy and Toxicology, University of Utrecht, The Netherlands.
|
| pubmed:publicationType |
Journal Article
|