In vitro evaluation of radioiodinated butyrophenones as radiotracer for dopamine receptor study

Journal Article · Mon Oct 26 04:00:00 EST 1987 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(87)90472-3· OSTI ID:6080839

Nakatsuka, I; Saji, H; Shiba, K; Shimizu, H; Okuno, M; Yoshitake, A; Yokoyama, A

Radioiodinated butyrophenone compounds are attracting the interest of those working on dopamine receptor studies; structure-activity relationship study has revealed the ortho position of the p-fluorobutyrophenone moiety as a very plausible iodination site. Various synthesized butyrophenones iodinated at the ortho position of p-fluorobutyrophenone moiety, 2'-iodohaloperidol (2'-IHP), 2'-iodotrifluperidol (2'-ITP) and 2'-iodospiperone (2'-ISP) were tested for their abilities to inhibit /sup 3/H-spiperone (SP) binding for the dopamine (D-2) receptor, together with reference compounds (SP, haloperidol(HP) and 4-iodospiperone (4-ISP)). The order of binding affinity of the tested compounds was SP > 2'-ISP > HP > 4-ISP > 2'-IHP > 2'-ITP. Whereas, the serotonin (S-2) receptor binding affinity of SP and its iodinated analogues were in the order of SP >> 4-ISP > 2'-ISP. These data indicated the 2'-ISP as holding high affinity for dopamine receptors and a low affinity for serotonin receptors. Thus, the /sup 125/I-2'-ISP was a very potent radioligand for in vitro dopamine (D-2) receptor studies, and /sup 123/I-2'-ISP holds very promising characteristics as for in vivo dopamine receptor studies, as well.

• Research Organization: Sumitomo Chemical Co., Ltd., Hyogo, Japan
• OSTI ID: 6080839
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 41:17; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
AMINES
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
CARDIOTONICS
CARDIOVASCULAR AGENTS
COMPARATIVE EVALUATIONS
DATA
DAYS LIVING RADIOISOTOPES
DOPAMINE
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EXPERIMENTAL DATA
HOURS LIVING RADIOISOTOPES
HYDROXY COMPOUNDS
IN VITRO
INFORMATION
INHIBITION
INTERMEDIATE MASS NUCLEI
IODINE 123
IODINE 125
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LABELLED COMPOUNDS
MEMBRANE PROTEINS
NEUROREGULATORS
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
PHENOLS
POLYPHENOLS
PROTEINS
RADIOISOTOPES
REACTION KINETICS
RECEPTORS
SPIPERONE
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS