| pubmed-article:15256540 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:15256540 | lifeskim:mentions | umls-concept:C0597357 | lld:lifeskim |
| pubmed-article:15256540 | lifeskim:mentions | umls-concept:C1704675 | lld:lifeskim |
| pubmed-article:15256540 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:15256540 | lifeskim:mentions | umls-concept:C1880022 | lld:lifeskim |
| pubmed-article:15256540 | lifeskim:mentions | umls-concept:C1173066 | lld:lifeskim |
| pubmed-article:15256540 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:15256540 | lifeskim:mentions | umls-concept:C0597328 | lld:lifeskim |
| pubmed-article:15256540 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:15256540 | pubmed:dateCreated | 2004-10-15 | lld:pubmed |
| pubmed-article:15256540 | pubmed:abstractText | Clinically used benzodiazepine and nonbenzodiazepine sedative-hypnotic agents for the treatment of insomnia produce their therapeutic effects through allosteric enhancement of the effects of the inhibitory neurotransmitter GABA at the GABA(A) receptor. Indiplon is a novel pyrazolopyrimidine sedative-hypnotic agent, currently in development for insomnia. Using radioligand binding studies, indiplon inhibited the binding of [(3)H]Ro 15-1788 (flumazenil) to rat cerebellar and cerebral cortex membranes with high affinity (K(i) values of 0.55 and 0.45 nM, respectively). [(3)H]Indiplon binding to rat cerebellar and cerebral cortex membranes was reversible and of high affinity, with K(D) values of 1.01 and 0.45 nM, respectively, with a pharmacological specificity consistent with preferential labeling of GABA(A) receptors containing alpha1 subunits. In "GABA shift" experiments and in measurements of GABA-induced chloride conductance in rat cortical neurons in culture, indiplon behaved as an efficacious potentiator of GABA(A) receptor function. In both the radioligand binding and electrophysiological experiments, indiplon had a higher affinity than zolpidem or zaleplon. These in vitro properties are consistent with the in vivo properties of indiplon as an effective sedative-hypnotic acting through allosteric potentiation of the GABA(A) receptor. | lld:pubmed |
| pubmed-article:15256540 | pubmed:language | eng | lld:pubmed |
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| pubmed-article:15256540 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:15256540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15256540 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:15256540 | pubmed:month | Nov | lld:pubmed |
| pubmed-article:15256540 | pubmed:issn | 0022-3565 | lld:pubmed |
| pubmed-article:15256540 | pubmed:author | pubmed-author:FosterAlan... | lld:pubmed |
| pubmed-article:15256540 | pubmed:author | pubmed-author:GrigoriadisDi... | lld:pubmed |
| pubmed-article:15256540 | pubmed:author | pubmed-author:VergeGailG | lld:pubmed |
| pubmed-article:15256540 | pubmed:author | pubmed-author:SullivanSusan... | lld:pubmed |
| pubmed-article:15256540 | pubmed:author | pubmed-author:GrossRaymond... | lld:pubmed |
| pubmed-article:15256540 | pubmed:author | pubmed-author:PetroskiRober... | lld:pubmed |
| pubmed-article:15256540 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:15256540 | pubmed:volume | 311 | lld:pubmed |
| pubmed-article:15256540 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:15256540 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:15256540 | pubmed:pagination | 537-46 | lld:pubmed |
| pubmed-article:15256540 | pubmed:dateRevised | 2008-11-21 | lld:pubmed |
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| pubmed-article:15256540 | pubmed:year | 2004 | lld:pubmed |
| pubmed-article:15256540 | pubmed:articleTitle | Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor. | lld:pubmed |
| pubmed-article:15256540 | pubmed:affiliation | Department of Pharmacology, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA. | lld:pubmed |
| pubmed-article:15256540 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:15256540 | lld:pubmed |
