18337424

Source:http://linkedlifedata.com/resource/pubmed/id/18337424

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Predicate	Object
rdf:type	pubmed:Citation
lifeskim:mentions	umls-concept:C0030685, umls-concept:C0036751, umls-concept:C0258875, umls-concept:C0391871, umls-concept:C0680255, umls-concept:C1283071, umls-concept:C1514873, umls-concept:C1515655, umls-concept:C1533691, umls-concept:C1546857, umls-concept:C1556066, umls-concept:C1619636, umls-concept:C1963578
pubmed:issue	11
pubmed:dateCreated	2008-3-13
pubmed:abstractText	The "club drug" 3,4-methylenedioxymethamphetamine (MDMA; also known as ecstasy) binds preferentially to and reverses the activity of the serotonin transporter, causing release of serotonin [5-hydroxytryptamine (5-HT)] stores from nerve terminals. Subsequent activation of postsynaptic 5-HT receptors by released 5-HT has been shown to be critical for the unique psychostimulatory effects of MDMA. In contrast, the effects of direct activation of presynaptic and/or postsynaptic receptors by MDMA have received far less attention, despite the agonist actions of the drug itself at 5-HT(2) receptors, in particular the 5-HT(2B) receptor. Here we show that acute pharmacological inhibition or genetic ablation of the 5-HT(2B) receptor in mice completely abolishes MDMA-induced hyperlocomotion and 5-HT release in nucleus accumbens and ventral tegmental area. Furthermore, the 5-HT(2B) receptor dependence of MDMA-stimulated release of endogenous 5-HT from superfused midbrain synaptosomes suggests that 5-HT(2B) receptors act, unlike any other 5-HT receptor, presynaptically to affect MDMA-stimulated 5-HT release. Thus, our findings reveal a novel regulatory component in the actions of MDMA and represent the first demonstration that 5-HT(2B) receptors play an important role in the brain, i.e., modulation of 5-HT release. As such, 5-HT(2B) receptor antagonists may serve as promising therapeutic drugs for MDMA abuse.
pubmed:language	eng
pubmed:journal	http://linkedlifedata.com/resource/pubmed/journal/8102140
pubmed:citationSubset	IM
pubmed:chemical	http://linkedlifedata.com/resource/pubmed/chemical/N-Methyl-3,4-methylenedioxyamphetami..., http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2B, http://linkedlifedata.com/resource/pubmed/chemical/Serotonin, http://linkedlifedata.com/resource/pubmed/chemical/Serotonin 5-HT2 Receptor Antagonists, http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists
pubmed:status	MEDLINE
pubmed:month	Mar
pubmed:issn	1529-2401
pubmed:author	pubmed-author:CallebertJacquesJ, pubmed-author:DolyStéphaneS, pubmed-author:HervéDenisD, pubmed-author:LaunayJean-MarieJM, pubmed-author:MaroteauxLucL, pubmed-author:SetolaVincentV, pubmed-author:ValjentEmmanuelE
pubmed:issnType	Electronic
pubmed:day	12
pubmed:volume	28
pubmed:owner	NLM
pubmed:authorsComplete	Y
pubmed:pagination	2933-40
pubmed:dateRevised	2010-11-18
pubmed:meshHeading	pubmed-meshheading:18337424-Animals, pubmed-meshheading:18337424-Female, pubmed-meshheading:18337424-Hyperkinesis, pubmed-meshheading:18337424-Male, pubmed-meshheading:18337424-Mice, pubmed-meshheading:18337424-Mice, Mutant Strains, pubmed-meshheading:18337424-N-Methyl-3,4-methylenedioxyamphetamine, pubmed-meshheading:18337424-Protein Binding, pubmed-meshheading:18337424-Receptor, Serotonin, 5-HT2B, pubmed-meshheading:18337424-Serotonin, pubmed-meshheading:18337424-Serotonin 5-HT2 Receptor Antagonists, pubmed-meshheading:18337424-Serotonin Antagonists
pubmed:year	2008
pubmed:articleTitle	Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro.
pubmed:affiliation	Inserm, U839 and Université Pierre et Marie Curie-Paris 6, Institut du Fer à Moulin, Unité Mixte de Recherche-S0839, Paris 75005, France.
pubmed:publicationType	Journal Article, Comparative Study, Research Support, Non-U.S. Gov't