Linked Life Data

15145701

Source:http://linkedlifedata.com/resource/pubmed/id/15145701

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2004-5-17
pubmed:abstractText
Previous studies have shown that BD1008 (N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine) and related analogs attenuate the toxicity and stimulant effects of cocaine through antagonism of sigma receptors. In the present study, six analogs of BD1008 (UMB 98-103) were synthesized and evaluated in receptor binding and behavioral studies. Competition binding studies confirmed that all six compounds have high affinity for sigma1 receptors, moderate affinity for sigma2 receptors, and low to negligible affinity for monoamine transporters, opioid, N-methyl-D-aspartate, dopamine, and 5-HT receptors. In behavioral pharmacological studies, pretreatment of mice with UMB 100, UMB 101, or UMB 103 significantly attenuated cocaine-induced convulsions and lethality. Together with earlier studies, the data suggest that analogs of BD1008 are promising medication development leads for reducing the toxicity of cocaine.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
10
pubmed:volume
492
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
21-6
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
2004
pubmed:articleTitle
Novel analogs of the sigma receptor ligand BD1008 attenuate cocaine-induced toxicity in mice.
pubmed:affiliation
Department of Pharmaceutical Sciences, College of Pharmacy, University of Oklahoma Health Sciences Center, P.O. Box 26901, CPB 337 Oklahoma City, OK 73190, USA. rae_matsumoto@ouhsc.edu
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.