6533b830fe1ef96bd1296802

RESEARCH PRODUCT

Stereospecific interaction of bicuculline with specific [3H]strychnine binding to rat spinal cord synaptosomal membranes

Werner E.g. MüllerA. Goldinger

subject

GlycineSynaptic MembranesReceptors Cell SurfaceBicucullineBinding CompetitiveStructure-Activity Relationshipchemistry.chemical_compoundReceptors GlycineSpecies SpecificityGABA receptorPostsynaptic potentialmedicineAnimalsReceptorGlycine receptorChemistryGABAA receptorGeneral NeuroscienceStereoisomerismStrychnineStrychnineBicucullineRatsSpinal CordBiochemistryGlycineBiophysicsmedicine.drug

description

The gamma-aminobutyric acid (GABA) antagonist (+/-)-bicuculline inhibits specific [3H]strychnine binding to postsynaptic glycine receptor sites in rat spinal cord synaptosomal membranes with an inhibition constant of about 5 microM, which is fairly similar to its inhibition constant reported for the GABA receptor. This effect is highly stereospecific, since the affinity of (-)-bicuculline for the specific [3H]strychnine binding sites is more than ten times less than that of the pharmacologically active (+)-bicuculline. Besides an unspecific effect at the glycine receptor, the results could suggest that the glycine and the GABA receptors are located close together in spinal cord membranes, so that the antagonist states of both receptors may be able to interfere with each other in some mechanistic way.

yearjournalcountryeditionlanguage
1980-01-01Neuroscience Letters
https://doi.org/10.1016/0304-3940(80)90107-x