Linked Life Data

12014970

Source:http://linkedlifedata.com/resource/pubmed/id/12014970

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
2002-5-16
pubmed:abstractText
A series of 4'-substituted phenyl-4-piperidinylmethanol and benzoyl-4-piperidine derivatives was synthesized as potential novel serotonin 5-HT2A receptor ligands that can be radiolabeled for in vivo brain imaging. Compounds were prepared by alkylation of 4-substituted benzoyl-4-piperidine with an iodo- or fluoro-substituted phenylalkyl halide followed by reduction with sodium borohydride. Potency of novel compounds was determined by in vitro radioreceptor affinity assays selective for serotonin 5-HT2A receptors. Potent compounds were further evaluated for selectivity at serotonin-2A versus 2C, 6, and 7, as well as dopamine D2 and adrenergic alpha1 and alpha2 receptors. The novel compound (4-fluorophenyl)-(1-[2-(4-fluorophenyl)ethyl]piperidin-4-yl])methanol was particularly promising with high 5-HT2A potency (K(i) = 1.63 nM) and >300-fold selectivity over other 5-HT receptor types.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
23
pubmed:volume
45
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2319-24
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed-meshheading:12014970-Animals, pubmed-meshheading:12014970-COS Cells, pubmed-meshheading:12014970-Humans, pubmed-meshheading:12014970-Ligands, pubmed-meshheading:12014970-Piperidines, pubmed-meshheading:12014970-Prosencephalon, pubmed-meshheading:12014970-Radioligand Assay, pubmed-meshheading:12014970-Rats, pubmed-meshheading:12014970-Receptor, Serotonin, 5-HT2A, pubmed-meshheading:12014970-Receptor, Serotonin, 5-HT2C, pubmed-meshheading:12014970-Receptors, Adrenergic, alpha-1, pubmed-meshheading:12014970-Receptors, Adrenergic, alpha-2, pubmed-meshheading:12014970-Receptors, Dopamine D2, pubmed-meshheading:12014970-Receptors, Serotonin, pubmed-meshheading:12014970-Structure-Activity Relationship, pubmed-meshheading:12014970-Tomography, Emission-Computed, pubmed-meshheading:12014970-Tomography, Emission-Computed, Single-Photon
pubmed:year
2002
pubmed:articleTitle
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging.
pubmed:affiliation
Department of Psychiatry, Yale University School of Medicine and VA Connecticut Health Care Service, West Haven, Connecticut 06516, USA.
pubmed:publicationType
Journal Article, In Vitro, Research Support, U.S. Gov't, P.H.S., Research Support, U.S. Gov't, Non-P.H.S., Research Support, Non-U.S. Gov't