Linked Life Data

11160615

Source:http://linkedlifedata.com/resource/pubmed/id/11160615

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2001-2-22
pubmed:abstractText
Dinapsoline is a new potent, full agonist at D1 dopamine receptors with limited selectivity relative to D2 receptors. The efficacy of this compound was assessed in rats with unilateral 6-hydroxydopamine lesions of the medial forebrain bundle, a standard rat model of Parkinson's disease. Dinapsoline produced robust contralateral rotation after either subcutaneous or oral administration. This rotational behavior was attenuated markedly by the D1 receptor antagonist SCH-23390, but not by the D2 receptor antagonist raclopride. During a chronic 14-day treatment period in which rats received dinapsoline either once or twice a day, dinapsoline did not produce tolerance (in fact, some sensitization of the rotational response was observed in one experiment). Because dinapsoline shows less D1:D2 selectivity in vitro than other D1 agonists, the contribution of D2 activity to tolerance was assessed. Chronic daily cotreatment with dinapsoline and raclopride did not enable the development of tolerance to chronic dinapsoline treatment. In contrast, when dinapsoline was administered by osmotic minipump, rapid tolerance was observed. To explore further the contribution of D1 and D2 receptors to tolerance, experiments were performed with the selective D1 agonist A-77636. Daily dosing with A-77636 rapidly produced complete tolerance, as previously observed, whereas coadministration of the D2 agonist quinpirole plus A-77636 failed to either delay or prevent tolerance. Taken together, these results indicate that the development of tolerance to D1 receptor agonists is influenced by the pattern of drug exposure but not by the D1:D2 selectivity of the agonist.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
296
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
338-44
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed-meshheading:11160615-Animals, pubmed-meshheading:11160615-Antiparkinson Agents, pubmed-meshheading:11160615-Chromatography, High Pressure Liquid, pubmed-meshheading:11160615-Dopamine, pubmed-meshheading:11160615-Dopamine Agonists, pubmed-meshheading:11160615-Dose-Response Relationship, Drug, pubmed-meshheading:11160615-Drug Tolerance, pubmed-meshheading:11160615-Hydroxydopamines, pubmed-meshheading:11160615-Isoquinolines, pubmed-meshheading:11160615-Male, pubmed-meshheading:11160615-Naphthols, pubmed-meshheading:11160615-Neostriatum, pubmed-meshheading:11160615-Parkinson Disease, pubmed-meshheading:11160615-Quinpirole, pubmed-meshheading:11160615-Raclopride, pubmed-meshheading:11160615-Rats, pubmed-meshheading:11160615-Rats, Sprague-Dawley, pubmed-meshheading:11160615-Receptors, Dopamine D1, pubmed-meshheading:11160615-Rotation, pubmed-meshheading:11160615-Stereotyped Behavior, pubmed-meshheading:11160615-Sympathectomy, Chemical
pubmed:year
2001
pubmed:articleTitle
Dinapsoline: characterization of a D1 dopamine receptor agonist in a rat model of Parkinson's disease.
pubmed:affiliation
Neuroscience/Genitourinary Drug Discovery, Bristol-Myers Squibb Inc., Wallingford, Connecticut 06492, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't