Tritium-3-N-methylspiperone labels D2 dopamine receptors in basal ganglia and S2 serotonin receptors in cerebral cortex

Journal Article · Wed Oct 01 00:00:00 EDT 1986 · J. Neurosci.; (United States)

OSTI ID:6992696

Lyon, R A; Titeler, M; Frost, J J; Whitehouse, P J; Wong, D F; Wagner, Jr, H N; Dannals, R F; Links, J M; Kuhar, M J

Detailed studies of the properties of /sup 3/H-3-N-methylspiperone (NMSP) binding in rat and human brain homogenates were performed at 37/sup 0/C. In homogenates of rat striatum and frontal cortex and human caudate and frontal cortex tissues, the specific binding was found to be saturable. Rat caudate contained 33.2 pmol/gm wet-weight tissue and displayed an equilibrium dissociation constant (Kd) of 8.7 X 10(-11) M; rat frontal cortex contained 18.5 pmol/gm wet-weight tissue and displayed a Kd of 1.5 X 10(-10) M. Human caudate contained 8.96 pmol/gm wet-weight tissue and displayed a Kd of 1.1 X 10(-10) M; human frontal cortex possessed 9.8 pmol/gm wet-weight tissue and a Kd of 4.4 X 10(-10) M. Kinetic studies revealed a very rapid rate of association in all the tissues studied. The rate of dissociation was relatively slow in all 4 tissue preparations; the dissociation rate was somewhat slower in rat striatum and human caudate relative to rat and human frontal cortex. This was consistent with the somewhat higher affinity, relative to frontal cortex, displayed by /sup 3/H-NMSP in rat striatal and human caudate tissue. The pharmacological properties of the specific binding in rat striatal and human caudate tissues were very similar and indicated the presence of brain D2 dopamine receptors. In rat and human frontal cortex tissue homogenates, the pharmacological characteristics of the specific binding indicated the presence of 5-HT2 receptors.

• Research Organization: Albany Medical College, NY
• OSTI ID: 6992696
• Journal Information: J. Neurosci.; (United States), Vol. 10
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
DOPAMINE
RADIORECEPTOR ASSAY
SEROTONIN
CEREBRAL CORTEX
RATS
RECEPTORS
TRITIUM COMPOUNDS
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZOLES
BODY
BRAIN
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
CEREBRUM
DRUGS
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
INDOLES
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PHENOLS
POLYPHENOLS
PROTEINS
PYRROLES
RADIOPROTECTIVE SUBSTANCES
RODENTS
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRYPTAMINES
VERTEBRATES
550201* - Biochemistry- Tracer Techniques