Muscarinic cholinergic receptor binding: in vivo depiction using single photon emission computed tomography and radioiodinated quinuclidinyl benzilate
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), Vol. 6:3
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
BRAIN
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
IODINE 123
ISOTOPE APPLICATIONS
BIOCHEMISTRY
CALVES
CARBOXYLIC ACID ESTERS
LABELLED COMPOUNDS
RECEPTORS
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
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 ISOTOPES
ISOTOPES
MAMMALS
NERVOUS SYSTEM
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
RADIOISOTOPES
RUMINANTS
TOMOGRAPHY
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
550201 - Biochemistry- Tracer Techniques