Linked Life Data

11927170

Source:http://linkedlifedata.com/resource/pubmed/id/11927170

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
2002-4-2
pubmed:abstractText
The neuropharmacological profile of Y-931, 8-fluoro-12- (4-methylpiperazin-1-yl)- 6H-[1]benzothieno [2,3-b][1,5]benzodiazepine maleate, was investigated in comparison with those of typical and claimed atypical antipsychotic drugs. Similar to clozapine and olanzapine, Y-931 interacted with multiple neurotransmitter receptors such as dopaminergic, serotonergic, alpha-adrenergic, muscarinic and histaminergic receptors. Y-931, as well as the other antipsychotics, was active in a dose-dependent manner in established tests which are indicative of potential antipsychotic activity such as inhibition of apomorphine-induced hyperactivity and suppression of conditioned avoidance responses, however, only Y-931 and clozapine were devoid of cataleptogenic potential. In models of N-methyl-D-aspartate (NMDA) receptor hypofunction, Y-931 demonstrated the most potent protective action against the dizocilpine-induced neurotoxicity (neuronal vacuolization) in the rat retrosplenial cortex ([Y-931 (ED(50); 0.20 mg/kg, p.o.), olanzapine (1.1), clozapine (5.7), risperidone (6.9), haloperidol (19)). Furthermore, Y-931 and clozapine, unlike the other antipsychotics used, reversed the dizocilpine-induced social deficits at the same doses at which their neuroprotective action was exhibited. The present results suggest that Y-931 may be a novel potential atypical antipsychotic drug with a low risk of extrapyramidal syndrome (EPS) and the property to ameliorate NMDA receptor hypofunction.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0893-133X
pubmed:author
pubmed:issnType
Print
pubmed:volume
26
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
456-67
pubmed:dateRevised
2011-5-18
pubmed:meshHeading
pubmed-meshheading:11927170-Animals, pubmed-meshheading:11927170-Antipsychotic Agents, pubmed-meshheading:11927170-Apomorphine, pubmed-meshheading:11927170-Avoidance Learning, pubmed-meshheading:11927170-Benzodiazepines, pubmed-meshheading:11927170-Catalepsy, pubmed-meshheading:11927170-Dizocilpine Maleate, pubmed-meshheading:11927170-Dopamine Agonists, pubmed-meshheading:11927170-Excitatory Amino Acid Antagonists, pubmed-meshheading:11927170-Female, pubmed-meshheading:11927170-Male, pubmed-meshheading:11927170-Motor Activity, pubmed-meshheading:11927170-Piperazines, pubmed-meshheading:11927170-Radioligand Assay, pubmed-meshheading:11927170-Rats, pubmed-meshheading:11927170-Rats, Sprague-Dawley, pubmed-meshheading:11927170-Rats, Wistar, pubmed-meshheading:11927170-Receptors, N-Methyl-D-Aspartate, pubmed-meshheading:11927170-Receptors, Neurotransmitter, pubmed-meshheading:11927170-Social Behavior
pubmed:year
2002
pubmed:articleTitle
Neuropharmacological profile of a novel potential atypical antipsychotic drug Y-931 (8-fluoro-12-(4-methylpiperazin-1-yl)- 6H-[1]benzothieno[2,3-b][1,5] benzodiazepine maleate).
pubmed:affiliation
Drug Discovery Laboratories, Pharmaceutical Research Division, Welfide Corporation 7-25, Koyata 3-Chome, Iruma, Saitama 358-0026, Japan.
pubmed:publicationType
Journal Article, Comparative Study