Search results for "Metergoline"

showing 2 items of 2 documents

Regulation of noradrenergic coerulean neuronal firing mediated by 5-HT2 receptors: involvement of the prepositus hypoglossal nucleus.

1991

Abstract Previous studies have indicated a 5-HT2-mediated inhibitory influence on unit activity in the locus coeruleus. In the present work, attempts were made to determine which area(s) of the brain is (are) involved in this effect: (1) Microiontophoretic application of serotoninergic compounds (quipazine, ketanserin, RU 24969 (Roussel Uclaf), 8-hydroxy-2(di-n-propylamino) tetralin (8-OH-DPAT), metergoline, serotonin) in the locus coeruleus, did not alter the coerulean discharge. Local microinjection of quipazine or ketanserin in the area of the locus coeruleus, as well as in one of its major afferents, the prepositus hypoglossi, had no effect on the unit activity in the locus coeruleus. 1…

Maleendocrine systemMetergolinemedicine.medical_specialtyHypoglossal NerveSerotoninKetanserinHypoglossal nucleusMicroinjectionsSerotonergicLigandsCellular and Molecular Neurosciencechemistry.chemical_compoundNorepinephrineNorepinephrineInternal medicinemedicineAnimalsheterocyclic compoundsNeurons Afferent5-HT receptorPharmacologyNeuronsChemistrymusculoskeletal neural and ocular physiologyQuipazineRats Inbred StrainsIontophoresisRatsEndocrinologynervous systemReceptors SerotoninLocus coeruleusRaphe NucleiLocus CoeruleusNeurosciencemedicine.drugNeuropharmacology
researchProduct

Evaluation of [11C]Metergoline as a PET Radiotracer for 5HTR in Nonhuman Primates

2010

Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [{sup 11}C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [{sup 11}C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.

PrimatesMetergolinemedicine.medical_specialtyBiodistributionClinical BiochemistryPharmaceutical ScienceBiochemistryArticlechemistry.chemical_compoundPharmacokineticsInternal medicineDrug DiscoverymedicineDistribution (pharmacology)Serotonin receptor antagonistAnimalsTissue DistributionCarbon RadioisotopesMolecular BiologyChemistryOrganic ChemistryAntagonistBrainEndocrinologyPositron-Emission TomographyReceptors SerotoninAltanserinMetergolineMolecular MedicineSerotoninRadiopharmaceuticalsProtein Binding
researchProduct