Linked Life Data

6215842

Source:http://linkedlifedata.com/resource/pubmed/id/6215842

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1982-12-21
pubmed:abstractText
Ketanserin, a selective 5-HT2-receptor antagonist, inhibits the reversible aggregation induced by 5-hydroxytryptamine (5-HT) in human platelet-rich plasma (PRP). In this respect, the compound is equipotent to cyproheptadine and more active than methysergide (IC50: 1.66 x 10(-8) M, 1.44 x 10(-8) M and 5.62 x 10(-8) M respectively). Ketanserin is active against 5-HT-induced platelet aggregation after both in vitro and oral administration to human volunteers. At concentrations up to 500 times in excess of the IC50 for 5-HT-induced platelet reactions, ketanserin does not affect the aggregation induced by ADP, epinephrine, collagen or Thrombofax, the prostaglandin biosynthesis of thrombin-stimulated platelets, nor the active uptake of 14C-5-HT by platelets. 5-Hydroxytryptamine amplifies the human platelet aggregation induced by threshold concentrations of ADP, collagen, epinephrine, norepinephrine and induced irreversible aggregation of platelets pre-sensitized with Thrombofax. This amplification by 5-hydroxytryptamine results in a platelet response typical for the potentiated agonist; for the combination of the monoamine with collagen, the serotonergic amplification results in enhanced aggregation, release of beta-TG and PF4 and excessive formation of TXB2. Ketanserin, after both in vitro and oral administration to man reduces the amplified response to the level of the potentiated agonist. The present evidence suggests the presence of functional 5-HT2 receptors on the human platelet, different from those involved in the uptake of the monoamine.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0065-4299
pubmed:author
pubmed:issnType
Print
pubmed:volume
12
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
388-97
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1982
pubmed:articleTitle
Inhibition of 5-hydroxytryptamine-induced and -amplified human platelet aggregation by ketanserin (R 41 468), a selective 5-HT2-receptor antagonist.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't