Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2-3
pubmed:dateCreated
2000-8-9
pubmed:abstractText
Multiple populations of pentameric nicotinic acetylcholinergic (nACh) receptors exist and several may be classified as central or neuronal. Neuronal nACh receptors, however, are primarily of the alpha 4 beta 2 and alpha 7 types, and these have been the focus of most recent investigations aimed at the development of novel agents and identification of pharmacophores. Selectivity data are limited. Furthermore, because several populations of nACh receptors might indirectly influence a given functional effect, it is difficult to discuss structure-activity relationships (SAR) in terms of differential SAR, or to formulate SAR on the basis of functional studies. For the most part, studies are limited to the formulation of structure-affinity relationships (SAFIR) for the binding of agents at nACh receptors, and for these the alpha 4 beta 2 population has been the most extensively investigated. SAFIR and newer agents are reviewed here with reference to earlier studies. Novel agents now have been identified that bind with up to 30 times higher affinity than nicotine and these are providing new insight into the understanding of nACh receptors.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0031-6865
pubmed:author
pubmed:issnType
Print
pubmed:volume
74
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
103-14
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
2000
pubmed:articleTitle
Central nicotinic receptor ligands and pharmacophores.
pubmed:affiliation
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298-0540, USA. glennon@hsc.vcu.edu
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Review