Linked Life Data

7658447

Source:http://linkedlifedata.com/resource/pubmed/id/7658447

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
18
pubmed:dateCreated
1995-10-4
pubmed:abstractText
A series of new arylpiperazide derivatives of serotonin has been prepared and evaluated as 5-HT1D receptor agonists. Binding experiments at cloned human 5-HT1D alpha, 5-HT1D beta, and 5-HT1A receptors show that all the compounds are very potent and selective ligands for 5-HT1D receptor subtypes. Functional activity studies (contraction of the New Zealand white rabbit saphenous vein) demonstrate that most of the derivatives behave as full agonists. Among them, the aryl sulfonamide derivative 5q (pD2 = 8.33 compare to 5.75 for sumatriptan) was also identified as a very potent agonist in inhibiting the forskolin-mediated cyclase coupled to 5-HT1D beta receptors (EC50 = 0.52nM).
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
38
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3602-7
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.
pubmed:affiliation
Medicinal Chemistry Division, Centre de Recherche Pierre Fabre, Castres, France.
pubmed:publicationType
Journal Article