6533b834fe1ef96bd129d789
RESEARCH PRODUCT
Beta-carbolines as benzodiazepine receptor ligands II: Synthesis and benzodiazepine receptor affinity of beta-carboline-3-carboxylic acid amides.
Klaus P. LippkeWalter E. MüllerSchunack Walter GSchunack Walter Gsubject
MaleIndolesChemical PhenomenaStereochemistrymedicine.drug_classPharmaceutical ScienceIn Vitro TechniquesLigandsMiceCarboline-3-carboxylic acidmedicineAnimalsReceptorchemistry.chemical_classificationBrain ChemistryBenzodiazepineReceptors GABA-AAffinitiesAmino acidChemistryKineticsMembranechemistryAmine gas treatingBenzodiazepine receptor ligandsCarbolinesdescription
Numerous beta-carboline-3-carboxamides were synthesized by amidation of beta-carboline-3-carboxylic acid, with various amino acids and amino acid esters serving as amine components, and tested in respect to their affinity for the benzodiazepine receptor in mouse brain membranes. The title compounds have affinities in the low micromolar range. The results are discussed with respect to their relevance for a possible beta-carboline structure containing the endogenous ligand of the benzodiazepine receptor.
year | journal | country | edition | language |
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1985-06-01 | Journal of pharmaceutical sciences |