The characterization of IBF as a new selective dopamine D-2 receptor imaging agent

Journal Article · Tue May 01 00:00:00 EDT 1990 · Journal of Nuclear Medicine; (USA)

OSTI ID:7044803

Kung, M P; Kung, H F; Billings, J; Yang, Y; Murphy, R A; Alavi, A ^[1]

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1. Univ. of Pennsylvania, Philadelphia (USA)

The in vivo and in vitro studies of a new iodinated benzamide analog, (125I)IBF,5-iodo-7-N-((1-ethyl-2-pyrrolidinyl)methyl)carboxamido-2,3- dihydrobenzofuran as a potential central nervous system (CNS) D-2 dopamine receptor imaging agent were investigated. In vivo biodistribution of IBF in rat indicated that this agent concentrated in the striatum region and displayed a remarkably high target-to-nontarget ratio (striatum/cerebellum = 48 at 120 min post-injection). The in vitro binding studies suggested that IBF binds selectively to D-2 dopamine receptors with high affinity and low nonspecific binding (Kd = 0.106 +/- 0.015 nM, Bmax = 448 +/- 18.2 fmole/mg protein). Ex vivo autoradiography results in rats further confirmed the high uptake and retention of this agent in the basal ganglia region. The planar images of monkey brains (lateral view of the head) after i.v. injection of ({sup 123}I)IBF clearly demonstrated that D-2 dopamine receptors can be visualized. With the excellent in vivo stability to deiodination and high target-to-nontarget ratio, ({sup 123}I)IBF may be useful as a CNS D-2 dopamine receptor imaging agent for single photon emission computed tomography (SPECT) in humans.

• OSTI ID: 7044803
• Journal Information: Journal of Nuclear Medicine; (USA), Vol. 31:5; ISSN 0161-5505
• Country of Publication: United States
• Language: English

Related Subjects

62 RADIOLOGY AND NUCLEAR MEDICINE
DOPAMINE
RECEPTORS
RADIOPHARMACEUTICALS
TISSUE DISTRIBUTION
AUTORADIOGRAPHY
BIOCHEMICAL REACTION KINETICS
BRAIN
IN VITRO
IN VIVO
IODINE 123
RATS
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BODY
CARDIOTONICS
CARDIOVASCULAR AGENTS
CENTRAL NERVOUS SYSTEM
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EMISSION COMPUTED TOMOGRAPHY
HOURS LIVING RADIOISOTOPES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
IODINE ISOTOPES
ISOTOPES
KINETICS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PHENOLS
POLYPHENOLS
PROTEINS
RADIOISOTOPES
REACTION KINETICS
RODENTS
SYMPATHOMIMETICS
TOMOGRAPHY
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics