(/sup 3/H)Spiroxatrine labels a serotonin/sub 1A/-like site in the rat hippocampus
(/sup 3/H)Spiroxatrine was examined as a potential ligand for the labeling of 5-HT/sub 1A/ sites in the rat hippocampus. Analysis o the binding of (/sup 3/H)spiroxatrine in the absence and presence of varying concentrations of three monoamine neurotransmitters revealed that serotonin (5-HT) had high affinity for the (/sup 3/H)spiroxatrine binding sites, consistent with the labeling of 5-HT/sub 1/ sites, while dopamine and norepinephrine had very low affinity. Saturation studies of the binding of (/sup 3/H)spiroxatrine revealed a single population of sites with a K/sub d/ = 2.21 nM. Further pharmacologic characterization with the 5-HT/sub 1A/ ligands 8-hydroxy-2-(di-ni-propylamino)tetralin, ipsapirone, and WB4101 and the butyrophenone compounds spiperone and haloperidol gave results that were consistent with (/sup 3/H)spiroxatrine labeling 5-HT/sub 1A/ sites. This ligand produced stable, reproducible binding with a good ratio of specific to nonspecific binding. The binding of (/sup 3/H)spiroxatrine was sensitive to GTP, suggesting that this ligand may act as an agonist. 21 references, 5 figures, 2 tables.
- Research Organization:
- Univ. of Arizona, Tucson
- OSTI ID:
- 6030909
- Journal Information:
- Life Sci.; (United States), Vol. 41:13
- Country of Publication:
- United States
- Language:
- English
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RECEPTORS
LABELLING
SEROTONIN
SYMPATHOMIMETICS
BIOCHEMICAL REACTION KINETICS
AFFINITY
EXPERIMENTAL DATA
HIPPOCAMPUS
LIGANDS
RATS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZOLES
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
DATA
DRUGS
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
INDOLES
INFORMATION
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
NERVOUS SYSTEM
NEUROREGULATORS
NUMERICAL DATA
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
PYRROLES
RADIOPROTECTIVE SUBSTANCES
REACTION KINETICS
RODENTS
TRYPTAMINES
VERTEBRATES
550201* - Biochemistry- Tracer Techniques