Source:http://linkedlifedata.com/resource/pubmed/id/11489455
Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
2
|
| pubmed:dateCreated |
2001-8-7
|
| pubmed:abstractText |
SB-243213 (5-methyl-1-[[-2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-6-trifluoromethylindoline hydrochloride) is a new, selective 5-hydroxytryptamine (5-HT)2C receptor inverse agonist. SB-243213 has high affinity for the human 5-HT2C receptor (pK(i) 9.37) and greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. In in vitro functional studies, SB-243213 acted as an inverse agonist at the human 5-HT2C receptor with a pK(b) of 9.8. In in vivo studies, SB-243213 was a potent inhibitor of central 5-HT2C receptor-mediated function in rats, blocking meta-chlorophenylpiperazine-induced hypolocomotion with an ID50 of 1.1 mg/kg p.o. and a long duration of action (>8 h). In rats, SB-243213 exhibited anxiolytic-like activity in both the social interaction and Geller-Seifter conflict tests. Importantly, unlike diazepam, chronic administration of SB-243213 did not result in the development of either tolerance to the anxiolytic-like effects or withdrawal anxiogenesis. Furthermore, in rodents, SB-243213 did not affect seizure threshold, did not increase body weight or induce catalepsy, but attenuated the haloperidol-induced catalepsy. SB-243213 did not affect amphetamine-, MK-801- or phencyclidine-induced hyperactivity. In conclusion, SB-243213 may possess an improved anxiolytic profile compared to benzodiazepines. SB-243213 also modulates dopaminergic transmission, lacks pro-psychotic properties and may have utility in the treatment of schizophrenia and motor disorders.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Anxiety Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Diazepam,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Inositol Phosphates,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2C,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/SB 243213
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Aug
|
| pubmed:issn |
0028-3908
|
| pubmed:author |
pubmed-author:BlackburnT PTP,
pubmed-author:BromidgeS MSM,
pubmed-author:ForbesI TIT,
pubmed-author:GagerT LTL,
pubmed-author:HollandVV,
pubmed-author:KennettG AGA,
pubmed-author:LightowlerSS,
pubmed-author:MiddlemissD NDN,
pubmed-author:ReavillCC,
pubmed-author:RileyGG,
pubmed-author:SteadBB,
pubmed-author:ThomasDD,
pubmed-author:TrainLL,
pubmed-author:WilsonAA,
pubmed-author:WoodM DMD
|
| pubmed:issnType |
Print
|
| pubmed:volume |
41
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
186-99
|
| pubmed:dateRevised |
2004-11-17
|
| pubmed:meshHeading |
pubmed-meshheading:11489455-Animals,
pubmed-meshheading:11489455-Anti-Anxiety Agents,
pubmed-meshheading:11489455-Anxiety,
pubmed-meshheading:11489455-Catalepsy,
pubmed-meshheading:11489455-Diazepam,
pubmed-meshheading:11489455-Dose-Response Relationship, Drug,
pubmed-meshheading:11489455-Drug Tolerance,
pubmed-meshheading:11489455-Humans,
pubmed-meshheading:11489455-Indoles,
pubmed-meshheading:11489455-Inositol Phosphates,
pubmed-meshheading:11489455-Male,
pubmed-meshheading:11489455-Motor Activity,
pubmed-meshheading:11489455-Pyridines,
pubmed-meshheading:11489455-Rats,
pubmed-meshheading:11489455-Rats, Sprague-Dawley,
pubmed-meshheading:11489455-Receptor, Serotonin, 5-HT2C,
pubmed-meshheading:11489455-Receptors, Serotonin,
pubmed-meshheading:11489455-Social Behavior,
pubmed-meshheading:11489455-Substance Withdrawal Syndrome
|
| pubmed:year |
2001
|
| pubmed:articleTitle |
SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety.
|
| pubmed:affiliation |
Department of Neuroscience Research, SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow Essex, CM19 5AW, UK. martyn_wood-1@sbphrd.com
|
| pubmed:publicationType |
Journal Article
|