Description
BaclofenisaGABAderivativethatactsasanagoNISTatGABA-Breceptors;itiscommonlyusedinanimalmodelstoexaminetheeffectsofGABAergicneurotransmissioninavarietyoffields,includingsubstancedependence,spasticity,pain,andfeedingbehavior.Baclofenexhibitsanalgesic,antinociceptive,andantiepileptic/anticonvulsantactivities.TheanalgesiceffectofbaclofenismediatedbyitsGABA-Breceptoractivation,inducingapresynapticblockofactionpotentialsinducedbymechanicalorthermalstimulithatdecreasesfrequencyandamplitudeofexcitatorypost-synapticcurrents.Baclofenisusedclinicallytopromoteabstinenceinalcoholdependentsubjects,potentiallymediatingalcoholcravingduringwithdrawal.Thiscompoundisalsodeliveredintrathecallytotreatspasticityanddystonia.
References
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