Autoradiography: (/sup 125/I)SCH 23982 binds with picomolar affinity to D1 sites on striatonigral neurons
SCH 23390 is selective D1 antagonist. The authors show for the first time, with iodinated SCH 23390, (/sup 125/I)SCH 23982, D1 binding sites on striatonigral neurons. Rat brain sections were covered for 1 hr by a pH 7.6 TRIS buffer containing 2-770 pM (/sup 125/I)SCH 23982, rinsed 2 min at 4 /sup 0/C, dried, and exposed to film for 18 hr. (/sup 125/I)SCH 23982 was displaced by D1 (SCH 23390; IC50= 200 pM; cis-flupenthixol, 10 nM; SKF 38393, 90 nM) but not D2 (sulpiride, LY171555) ligands. Intermediate D1 binding was found in the internal capsule and entopeduncular nucleus. Striatal quinolinate (100 nmol) decreased nigral and striatal D1 binding. Intranigral 6-hydroxydopamine (6 ..mu..g) that destroyed > 90% of nigrostriatal dopamine neurons did not alter nigral or striatal D1 binding. Thus, (/sup 125/I)SCH 23982 labels with pM affinity D1 sites that reside on striatonigral neurons.
- Research Organization:
- CIBA-GEIGY Corp., Summit, NJ
- OSTI ID:
- 5451194
- Report Number(s):
- CONF-8604222-
- Journal Information:
- Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States), Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Vol. 45:3; ISSN FEPRA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AUTORADIOGRAPHY
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
DAYS LIVING RADIOISOTOPES
DOPAMINE
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
KINETICS
LIGANDS
MAMMALS
NERVES
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PHENOLS
POLYPHENOLS
RADIOISOTOPES
RATS
REACTION KINETICS
RODENTS
SYMPATHOMIMETICS
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