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- Nishio,H. etal. (1996) Gen.Pharmacol. 27, 779.
AlomoneLabs Talipexoledihydrochloride(B-HT920) blocks5-HT3AreceptorsexpressedinHEK293Tcells.Currentswereelicitedby10µM5-HT,deliveredevery3minutes.Talipexoledihydrochloride (#B-140)wasapplied30secondsbeforestimulationat10and100µM,asindicatedandinhibitedthe5-HTinducedcurrentinadose-dependentandreversIBLemanner.
- 1.Nishio,H. etal. (1996) Gen.Pharmacol. 27, 779.
- 2.Clarke,P.B. etal. (1990) Br.J.Pharmacol. 99, 509.
- 3.Plosker,G.L.andBenfield,P. (1997) CNSDrugs 7, 410.
- 4.Inoue,Y. etal. (1999) PsychiatryClin.Neurosci. 53, 283.
Talipexoleisanazepinederivative,andactsasanagonistofD2dopaminepre-andpostsynapticreceptors,aswellasan α2-adrenoceptoragonistand5-HT3receptorantagonist1.
ThepurposeofTalipexoleistoincreasedopamineactivityinthecentralnervoussystem.ItinhibitselectricallyevokedreleaseofdopaminethroughactivationofD2synapticautoreceptorslocatedondopaminergicterminals.Italsocausesreleaseofacetylcholineandnoradrenalin2,3.
Talipexolehasbeenestablishedinanumberofclinicaltrialsasananti-Parkinsonianagent.Thesetrialsshowedsignificantimprovementinmotoractivityandinotherparkinsoniansymptomsincludingakinesia,rigidity,tremorandgaitdisturbances.Thereareseveralsideeffectscausedbythisdrugsuchasdrowsiness,dizziness,hallucinations,gastrointestinaldiscomfort,nauseaandlossofappetite3.
Inaddition,talipexoleisalsoexpectedtobebeneficialforthetreatmentofperiodiclegmovementdisorderandrestlesslegsyndrome4.
Talipexoledihydrochloride(#B-140) isahighlypure,synthetic,andbiologicallyactivecompound.



