PMID: 1530770Jan 1, 1992Paper

Characterization of radioiodinated TISCH: a high-affinity and selective ligand for mapping CNS D1 dopamine receptor

Journal of Neurochemistry
J J BillingsH F Kung

Abstract

In developing CNS D1 dopamine receptor-imaging agents with improved specificity and longer brain retention, an iodinated D1 ligand was synthesized. In vitro and in vivo radiolabeling studies of a new iodinated benzazepine, TISCH [7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro-1H-3- benzazepine], an analog of SCH 23390 (7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepin e), were investigated. After an intravenous injection, the R(+) isomer of TISCH showed high brain uptake in rats (2.20 and 0.57% dose per whole brain at 2 and 60 min, respectively). The striatum/cerebellum ratio increased progressively with time (12 at 60 min). Ex vivo autoradiography of rat brain sections, after intravenous injection of R(+)-[125I]TISCH, displayed the highest uptake in striatum and substantia nigra, regions known to have a high concentration of D1 receptors, whereas the S(-) isomer displayed no specific uptake. Furthermore, the specific uptake can be blocked by pretreatment with SCH 23390. In vitro binding studies using the rat striatum tissue preparation showed high specific and low nonspecific bindings (KD = 0.21 +/- 0.03 nM). The rank order of potency exhibiting high specificity to the D1 receptor was SC...Continue Reading

References

Jan 1, 1990·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·S M MoerleinM J Welch
Sep 1, 1989·The British Journal of Psychiatry : the Journal of Mental Science·G P Reynolds
Jan 1, 1989·Life Sciences·J BillingsH F Kung
Sep 9, 1986·European Journal of Pharmacology·A SidhuJ W Kebabian
Mar 1, 1988·Trends in Pharmacological Sciences·D Hoyer
Sep 1, 1988·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·A Carlsson
Aug 1, 1988·Journal of Neurochemistry·C P ManikP McGonigle
Oct 1, 1986·Physiology & Behavior·J P Kroon, A L Riley
Oct 1, 1986·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·J L LearR Muth
Feb 5, 1985·European Journal of Pharmacology·A M FriedmanR J Dinerstein
Jan 1, 1984·Journal of Receptor Research·E Bürgisser
Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Feb 1, 1962·The Journal of Comparative Neurology·A J BLOMQUISTR EMMERS

❮ Previous
Next ❯

Citations

Jan 1, 1996·Nuclear Medicine and Biology·C PellevoisinD Guilloteau
Aug 1, 1993·Journal of Neuroscience Research·N T PanagopoulosT Valcana
Oct 1, 1994·Seminars in Nuclear Medicine·G B SahaR T Go

❮ Previous
Next ❯

Related Concepts

Related Feeds

Basal Ganglia

Basal Ganglia are a group of subcortical nuclei in the brain associated with control of voluntary motor movements, procedural and habit learning, emotion, and cognition. Here is the latest research.