Search results for "DMCM"

showing 3 items of 3 documents

Pharmacological heterogeneity of γ-aminobutyric acid receptors during development suggests distinct classes of rat cerebellar granule cells in situ

2001

The gamma-aminobutyric acid receptor (GABA(A)R) represents a ligand-gated Cl(-)-channel assembling as heteropentamere from 19 known subunits. Cerebellar granule cells contain a unique subset, namely the alpha1-, alpha6-, beta2-, gamma2- and delta-subunits. We studied their GABAergic pharmacology in situ using whole-cell patch-clamp recordings in brain slices and a modified Y-tube application system. The distribution of the EC50s for GABA in young (P8-P14) and medium aged animals (P15-P28) could be fitted with the sum of two Gaussian distributions with means of 60 and 185 microM and 27 and 214 microM, respectively. In older animals (P29-P48) the observed homogeneous range of sensitivities fi…

Agingmedicine.medical_specialtyCerebellumPatch-Clamp TechniquesLoreclezoleConvulsantsIn Vitro TechniquesBiologyBicucullineInhibitory postsynaptic potentialAminobutyric acidMembrane PotentialsGABA AntagonistsRats Sprague-DawleyCellular and Molecular Neurosciencechemistry.chemical_compoundFurosemideCerebellumInternal medicineDMCMmedicineAnimalsDiureticsGABA ModulatorsReceptorPharmacologyDiazepamLong-term potentiationReceptors GABA-ARatsElectrophysiologymedicine.anatomical_structureEndocrinologychemistryGABAergicAlgorithmsCarbolinesmedicine.drugNeuropharmacology
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Actions of two GABAA receptor benzodiazepine-site ligands that are mediated via non-γ2-dependent modulation.

2011

The potent sedative-hypnotic zolpidem and the convulsant methyl-6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate (DMCM) act primarily by binding to the benzodiazepine site of the main inhibitory neurotransmitter receptor, the pentameric γ-aminobutyric acid type A receptor (GABA(A)). This binding depends critically on the wild-type F77 residue of the GABA(A) receptor γ2 subunit. Mice with γ2 subunit F77I point mutation (γ2I77 mouse line) lose the high-affinity nanomolar binding of these ligands as well as their most robust behavioral actions at low doses. Interestingly, the γ2I77 mice offer a tool to study the actions of these substances mediated via other possible binding sites of the GABA(A…

AgonistMaleZolpidemAzidesmedicine.drug_classPyridinesConvulsantsPharmacologyLigandsGABAA-rho receptor03 medical and health scienceschemistry.chemical_compoundBenzodiazepinesMice0302 clinical medicineDMCMmedicineAnimalsHumansHypnotics and SedativesBinding site030304 developmental biologyPharmacology0303 health sciencesBenzodiazepineBinding SitesBehavior AnimalGABAA receptorBrainLigand (biochemistry)Receptors GABA-AMice Inbred C57BLZolpidemProtein SubunitsHEK293 CellschemistryAutoradiographyFemale030217 neurology & neurosurgerymedicine.drugCarbolinesProtein BindingEuropean journal of pharmacology
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Furosemide action on cerebellar GABA(A) receptors in alcohol-sensitive ANT rats.

1999

Furosemide increases the basal tert-[35S]butylbicyclophosphorothionate ([35S]TBPS) binding and reverses the inhibition of the binding by gamma-aminobutyric acid (GABA) in the cerebellar GABA(A) receptors containing the alpha6 and beta2/beta3 subunits. These effects are less pronounced in the alcohol-sensitive (ANT) than in the alcohol-insensitive (AT) rat line. The difference between the rat lines in the increase of basal [35S]TBPS binding was removed after a longer preincubation with ethylendiaminetetraacetic acid (EDTA) containing buffer, but long preincubation did not reduce the GABA content of the incubation fluid or remove the difference in GABA antagonism by furosemide. The GABA sensi…

Malemedicine.medical_specialtyCerebellumAzidesHealth (social science)BiologySodium ChlorideToxicologyBicucullineLigandsBiochemistryGABA AntagonistsBehavioral Neurosciencechemistry.chemical_compoundBenzodiazepinesFurosemideDMCMInternal medicineCerebellummedicineAnimalsReceptorGABA AgonistsEthanolGABAA receptorFurosemideGeneral MedicineBridged Bicyclo Compounds HeterocyclicReceptors GABA-AANTRatsPyridazinesAlcoholismDrug Combinationsmedicine.anatomical_structureEndocrinologyNeurologyMechanism of actionchemistryFemalemedicine.symptommedicine.drugCarbolinesAlcohol (Fayetteville, N.Y.)
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