Search results for "Iodobenzamide"

showing 4 items of 4 documents

[123I]IBZM SPECT in patients treated with typical and atypical neuroleptics: relationship to drug plasma levels and extrapyramidal side effects

1997

[123I]Iodobenzamide (IBZM) is an iodine-labeled dopamine receptor ligand and can be used to visualize brain D2 receptors in humans with single photon emission computerized tomography (SPECT). The ratio of striatal IBZM uptake to uptake in frontal cortex (ST/FC ratio) represents a semiquantitative measure of D2 receptor binding in the striatum. Our study sample included six patients treated with haloperidol (3.0-8.0 mg/day orally; one patient with an average of 0.9 mg/day intramuscularly), five patients with benperidol (9.0-15.0 mg/day orally) and nine patients treated with clozapine (200.0-600.0 mg/day orally). Typical neuroleptics (TNs) and atypical neuroleptics (ANs) were significantly di…

AdultMalemedicine.medical_specialtyBipolar DisorderPyrrolidinesNeuroscience (miscellaneous)Benperidolchemistry.chemical_compoundIodobenzamideBasal Ganglia DiseasesDopamineInternal medicineDopamine receptor D2medicineHaloperidolHumansRadiology Nuclear Medicine and imagingChlorpromazineClozapineClozapineAgedNeurologic ExaminationPsychiatric Status Rating ScalesTomography Emission-Computed Single-PhotonDepressive Disorder MajorSchizophrenia ParanoidDose-Response Relationship DrugReceptors Dopamine D2business.industryBenperidolBrainMiddle AgedCorpus StriatumFrontal LobePsychiatry and Mental healthEndocrinologychemistryDopamine receptorBenzamidesDopamine AntagonistsHaloperidolFemalebusinessAntipsychotic Agentsmedicine.drugPsychiatry Research: Neuroimaging
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Occupancy of striatal D 2 -like dopamine receptors after treatment with the sigma ligand EMD 57445, a putative atypical antipsychotic

1999

Rationale: EMD 57445 (panamesine) is a high affinity sigma ligand with the profile of an atypical antipsychotic in animal studies. It has been reported recently to have antipsychotic activity in schizophrenia. However, its metabolite, EMD 59983, binds also to D2 and D3 dopamine (DA) receptors. Objectives: The aim of this study was to test, using single photon emission computed tomography (SPECT) and [123I]iodobenzamide (IBZM) as the radiotracer, whether EMD 59983 would pass the blood-brain barrier and to what extent it would contribute to the effects of EMD 57445 in schizophrenia. Methods: Two IBZM SPECT-scans were performed in five neuroleptic-free schizophrenic patients (DSM IV), one befo…

AdultMalemedicine.medical_specialtyPyrrolidinesmedicine.drug_classmedicine.medical_treatmentSigma receptorAtypical antipsychoticPanamesinePharmacologychemistry.chemical_compoundIodobenzamidePiperidinesDopamine receptor D3DopamineInternal medicinemedicineHumansReceptors sigmaAntipsychoticOxazolesTomography Emission-Computed Single-PhotonPharmacologyReceptors Dopamine D2Middle AgedCorpus StriatumPyrimidinesEndocrinologychemistryBlood-Brain BarrierDopamine receptorBenzamidesSchizophreniaFemaleAntipsychotic Agentsmedicine.drugPsychopharmacology
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Synthesis and antifungal activity of new N-(1-phenyl-4-carbetoxypyrazol-5-yl)-, N-(indazol-3-yl)- and N-(indazol-5-yl)-2-iodobenzamides

2002

N-(1-Phenyl-4-carbetoxypyrazol-5-yl)-, N-(indazol-3-yl)- and N-(indazol-5-yl)-2-iodobenzamides 6, with a Benodanil-like structure, were synthesized by refluxing in acetic acid the corresponding benzotriazinones 5 with potassium iodide for 1 h in order to study the role on the antifungal activity of the N-substitution with an aromatic heterocyclic system on benzamide moiety. Among the tested iododerivatives, compounds 6d,f,g,h possess interesting activities toward some phytopathogenic fungal strains.

AntifungalAntifungal AgentsIndazolesMagnetic Resonance SpectroscopySpectrophotometry Infraredmedicine.drug_classStereochemistryColony Count MicrobialPharmaceutical Sciencechemistry.chemical_elementCarboxamideMicrobial Sensitivity TestsIodineChemical synthesisAcetic acidchemistry.chemical_compoundN-(1-phenyl-4-carbetoxypyrazol-5-yl)-2-iodobenzamides N-(indazol-3-yl)-2-iodobenzamides N-(indazol-3-yl)-2-iodobenzamides antifungal activityDrug DiscoverymedicineMoietyBenzamideChemistryFungiSettore CHIM/08 - Chimica FarmaceuticaBenzamidesPyrazolesIl Farmaco
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Synthesis and antifungal activity of new N-isoxazolyl-2-iodobenzamides

1999

N-Isoxazolyl-2-iodobenzamides 3 and 9, with a benodanil-like structure, were synthesized by refluxing in acetic acid the corresponding benzotriazinones 2 and 8 with potassium iodide for 1 h with the aim to ascertain if they were active as fungicides against Phytophthora citricola Saw., Botrytis cinerea Pers., Rhizoctonia sp. and Alternaria sp. Among the tested iodo derivatives, compounds 3b and 9a possess interesting activities against the aforesaid fungal strains in several cases similar to that of benodanil I taken as reference drug.

Phytophthora citricolaMagnetic Resonance SpectroscopyChemical PhenomenaSpectrophotometry Infraredmedicine.drug_classStereochemistryColony Count MicrobialPharmaceutical ScienceCarboxamideRhizoctoniaChemical synthesisAcetic acidchemistry.chemical_compoundN-Isoxazolyl-2-iodobenzamideDrug DiscoverymedicineAntifungal activityBotrytis cinereabiologyChemistry PhysicalfungiFungifood and beveragesIsoxazolesbiology.organism_classificationAlternariaSettore CHIM/08 - Chimica FarmaceuticaFungicides IndustrialFungicidechemistryBenzamides
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