Muscarinic cholinergic receptor binding: in vivo depiction using single photon emission computed tomography and radioiodinated quinuclidinyl benzilate

Journal Article · Tue Jun 01 00:00:00 EDT 1982 · J. Comput. Assist. Tomogr.; (United States)

DOI:https://doi.org/10.1097/00004728-198206000-00019· OSTI ID:6943153

Drayer, B; Jaszczak, R; Coleman, E; Storni, A; Greer, K; Petry, N; Lischko, M; Flanagan, S

An attempt was made to characterize, in vivo, specific binding to the muscarinic cholinergic receptor in the calf using the radioiodinated ligand quinuclidinyl benzilate (/sup 123/I-OH-QNB) and single photon detection emission computed tomography (SPECT). The supratentorial brain activity was significantly increased after the intravenous infusion of /sup 123/I-OH-QNB as compared to free /sup 123/I. Scopolamine, a muscarinic cholinergic receptor antagonist, decreased the measured brain activity when infused prior to /sup 123/I-OH-QNB consistent with pharmacologic blockade of specific receptor binding. Quantitative in vitro tissue distribution studies obtained following SPECT imaging were consistent with regionally distinct specific receptor binding in the striatum and cortical gray matter, nonspecific binding in the cerebellum, and pharmacologic blockade of specific binding sites with scopolamine. Although /sup 123/I-OH-QNB is not the ideal radioligand, our limited success will hopefully encourage the development of improved binding probes for SPECT imaging and quantitation.

• Research Organization: Department of Radiology, Duke University Medical Center, Durham, NC
• OSTI ID: 6943153
• Journal Information: J. Comput. Assist. Tomogr.; (United States), Journal Name: J. Comput. Assist. Tomogr.; (United States) Vol. 6:3; ISSN JCATD
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BIOCHEMISTRY
BODY
BRAIN
CALVES
CARBOXYLIC ACID ESTERS
CATTLE
CENTRAL NERVOUS SYSTEM
CHEMISTRY
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DOMESTIC ANIMALS
ELECTRON CAPTURE RADIOISOTOPES
EMISSION COMPUTED TOMOGRAPHY
ESTERS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
IODINE 123
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
RADIOISOTOPES
RECEPTORS
RUMINANTS
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
TOMOGRAPHY
VERTEBRATES