1 TC-2153 [Effect of New Potential Psychotropic Drug,...

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Mol Biol (Mosk). 2011 MarApr;45(2):2828. [Effect of new potential psychotropic drug, 8(trifluoromethyl)1,2,3,4,5benzopentathiepin6amine hydrochloride, on the expression of serotoninrelated genes in mouse brain]. [Article in Russian] Kulikov AV , Tikhonova MA , Kulikova EA , Khomenko TM , Korchagina DV , Volcho KP , Salachutdinov HF , Popova NK . Abstract Study of molecular mechanisms of psychotropic drug action is the main aim of molecular psychopharmacology. New synthetic analog of variacin 8(Trifluoromethyl)1,2,3,4,5benzopentathiepin6amine (TX2153) was shown to produce anxiolytic and anticonvulsant effects on mice. Here the effect of chronic administration of TX2153 on expression of some serotoninrelated genes in mouse brain was investigated. The drug (10 mg/kg, per os, 16 days) was administered to adult males of ASC (Antidepressant Sensitive Catalepsy) mouse strain characterizing by alterations in behavior and brain serotonin system. The expression of genes encoding 1) the key enzyme of serotonin synthesis, tryptophan hydroxylase 2 (TPH2), 2) main enzyme of serotonin degradation, monoamine oxydase A (MAOA), 3) 5HT transporter (SERT) and 4) 5HT(1A) receptor was studied using quantitative RTPCR. TX 2153 significantly reduced mRNA level of 5HT(1A) receptor and MAOA genes in the midbrain without any effect on expression of these genes in the frontal cortex and hippocampus. The drug failed to affect expression of TPH2 and SERT genes in the midbrain. The result indicates involvement of the brain 5HT system in the molecular mechanism underlying the effect of TX2153. PMID: 21634115 [PubMed indexed for MEDLINE] Abstract Publication Types, MeSH Terms, Substances LinkOut more resources PubMed

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Transcript of 1 TC-2153 [Effect of New Potential Psychotropic Drug,...

  • 8/2/2015 [Effectofnewpotentialpsychotropicdrug,8(trifluoromethyl)1,2,3,4,5benzopentathiepin6aminehydrochloride,ontheexpressionofserotoninr...PubMedNCBI

    http://www.ncbi.nlm.nih.gov/pubmed/21634115 1/2

    MolBiol(Mosk).2011MarApr45(2):2828.

    [Effectofnewpotentialpsychotropicdrug,8(trifluoromethyl)1,2,3,4,5benzopentathiepin6aminehydrochloride,ontheexpressionofserotoninrelatedgenesinmousebrain].[ArticleinRussian]KulikovAV,TikhonovaMA,KulikovaEA,KhomenkoTM,KorchaginaDV,VolchoKP,SalachutdinovHF,PopovaNK.

    AbstractStudyofmolecularmechanismsofpsychotropicdrugactionisthemainaimofmolecularpsychopharmacology.Newsyntheticanalogofvariacin8(Trifluoromethyl)1,2,3,4,5benzopentathiepin6amine(TX2153)wasshowntoproduceanxiolyticandanticonvulsanteffectsonmice.HeretheeffectofchronicadministrationofTX2153onexpressionofsomeserotoninrelatedgenesinmousebrainwasinvestigated.Thedrug(10mg/kg,peros,16days)wasadministeredtoadultmalesofASC(AntidepressantSensitiveCatalepsy)mousestraincharacterizingbyalterationsinbehaviorandbrainserotoninsystem.Theexpressionofgenesencoding1)thekeyenzymeofserotoninsynthesis,tryptophanhydroxylase2(TPH2),2)mainenzymeofserotonindegradation,monoamineoxydaseA(MAOA),3)5HTtransporter(SERT)and4)5HT(1A)receptorwasstudiedusingquantitativeRTPCR.TX2153significantlyreducedmRNAlevelof5HT(1A)receptorandMAOAgenesinthemidbrainwithoutanyeffectonexpressionofthesegenesinthefrontalcortexandhippocampus.ThedrugfailedtoaffectexpressionofTPH2andSERTgenesinthemidbrain.Theresultindicatesinvolvementofthebrain5HTsysteminthemolecularmechanismunderlyingtheeffectofTX2153.

    PMID:21634115[PubMedindexedforMEDLINE]

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  • 8/2/2015 [Effectofnewpotentialpsychotropicdrug,8(trifluoromethyl)1,2,3,4,5benzopentathiepin6aminehydrochloride,ontheexpressionofserotoninr...PubMedNCBI

    http://www.ncbi.nlm.nih.gov/pubmed/21634115 2/2

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