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  • Title: Resolution of multiple affinity states of 5-hydroxytryptamine-1A receptors labelled by [3H]-8-hydroxy-2-(di-n-propilamino) tetralin in rat hippocampal membranes.
    Author: Pesce G, Hery F.
    Journal: Gen Pharmacol; 1996 Jun; 27(4):723-9. PubMed ID: 8853311.
    Abstract:
    1. We examined the binding of [3H]-8-hydroxy-2-(DI-n-propilamino)tetralin ([3H]-8OH-DPAT) to 5-hydroxytriptamine-1A (5-HT1A) receptors in rat hippocampal membranes. 2. Computer analysis of [3H]-8OH-DPAT displacement curves in the absence and in the presence of 100 microM guanosine-5'-O-(3-thiotriphosphate) (GTP gamma S) were best fitted with a three-site model with apparent dissociation constants (Kd) of 0.45, 2.8 and 30 nM; the corresponding binding capacity (Bmax) existing in the three affinity states were 4, 2 and 12 pmol/g of tissue (wet weight), respectively. 3. These results suggest that [3H]-8OH-DPAT binding can be resolved as complex isotherms and we provided evidence that [3H]-8OH-DPAT labels 2 high-affinity GTP gamma S-sensitive and one low-affinity GTP gamma S-sensitive state of 5-HT1A receptors.
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