Linked Life Data

7902869

Source:http://linkedlifedata.com/resource/pubmed/id/7902869

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
24
pubmed:dateCreated
1994-1-11
pubmed:abstractText
A series of N-(1-arylpropionyl)-4-aryl-1,2,3,6-tetrahydropyridines, prepared by simple Mannich condensations, have been found by radioligand binding assays to have moderate to high affinity (IC50 0.5-500 nM) for bovine cerebellar sigma receptor/binding sites and no measurable affinity (IC50 > 5000 nM) for bovine striatal D2 receptors. The most active of these compounds rival in potency the most active sigma ligands previously reported. Three of these sigma-active compounds were screened for pharmacological activity under the NIMH-NovaScreen program and showed moderate affinity only for D2 and 5-HT2 receptors among the 40 sites assayed. Since these N-(1-arylpropionyl)-4-aryltetrahydropyridines are structurally related to other potent sigma receptor ligands, in particular haloperidol and 4-phenylpiperidines, these data provide insights into the nature of the essential pharmacophore of the sigma receptor. The selective affinity of these materials for sigma receptors indicates they have potential as prototypes of novel psychotherapeutic medicinal agents, particularly as antipsychotic drugs which would be devoid of debilitating side effects associated with blockade of D2 receptors.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
26
pubmed:volume
36
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3923-8
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1993
pubmed:articleTitle
N-(1-arylpropionyl)-4-aryltetrahydropyridines, a new class of high-affinity selective sigma receptor ligands.
pubmed:affiliation
Department of Chemistry, New York University, New York 10003.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.