✦ LIBER ✦

Session 6: Neuroscience II Receptors - Chemistry and Pharmacology

Publisher: John Wiley and Sons
Year: 2003
Tongue: French
Weight: 657 KB
Volume: 46
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.755

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✦ Synopsis

Figure 1, 1a, hNK1 IC 50 = 67pM) is an NK1 receptor PET ligand that was developed in collaboration with the Turku, Uppsala and Hammersmith PET Centers. One drawback of this tracer is its faster rate of defluorination in nonhuman primates than in humans. It was our desire to improve [ 18 F]SPARQ for preclinical PET studies in non-human primates by slowing the rate of defluorination and increasing the plasma halflife of the tracer. Previously we introduced deuterium atoms in the fluoromethyl methylene group to produce [ 18 F]DSPARQ, 1b, and more recently we have synthesized the fluoroethyl analog ([ 18 F]FESPARQ, 2; hNK1 IC 50 = 17pM).

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