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• W2116414558 abstract "Abstract: [3H]Zacopride displayed regional saturable specific binding to homogenates of human brain tissues, as defined by the inclusion of BRL43694 [endo-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-l-methylindazole-3-carboxamide] in the incubation media. Scatchard analysis of the saturation data obtained from amygdaloid and hippocampal tissues identified the binding as being of high affinity and to a homogeneous population of binding sites (KD= 2.64 ± 0.75 and 2.93 ± 0.41 nmol/L and Bmax= 55 ± 7 and 44 ± 9 fmol/ mg of protein in the amygdala and hippocampus, respectively). 5-Hydroxytryptamine3 (5-HT3) receptor agonists and antagonists competed for the [3H]zacopride binding site, competing with up to 40% of total binding with a similar rank order of affinity in both tissues; agents acting on various other neurotransmitter receptors failed to inhibit binding. Kinetic data revealed a fast association that was fully reversible (k+1= 6.61 × 105 and 7.65 × 105/mol/L/s and k-1= 3.68 × 10−3 and 3.45 × 10−3/s in the amygdala and hippocampus, respectively). It is concluded that [3H]zacopride selectively labels with high affinity 5-HT3 recognition sites in human amygdala and hippocampus and, if these binding domains represent 5-HT3 receptors, may provide the opportunity for 5-HT3 receptor antagonists to modify 5-HT function in the human brain" @default.
• W2116414558 created "2016-06-24" @default.
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• W2116414558 date "1989-12-01" @default.
• W2116414558 modified "2023-09-24" @default.
• W2116414558 title "Identification and Characterisation of 5-Hydroxytryptamine₃Recognition Sites in Human Brain Tissue" @default.
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• W2116414558 doi "https://doi.org/10.1111/j.1471-4159.1989.tb09244.x" @default.
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