Positron-emitting radioligands for imaging neuroleptic receptors Page: 2 of 2
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specific distribution to nsurolsptlc receptors, Insignificant aetsbollsa In
the central nervous spates, end slow dlasodstlon rate, Is an Ideal choice
for PIT studies of neuroleptic receptors In humans. V* have recently
confined this positive evaluation by performing human studies with this
compound. PR studies for as long as 12 hours after Injection suggest that
this compound binds Irreversibly l£ vivo to sites In the human
caudate-putaaen.
A model was developed which allows the detenlnatlon of association and
dissociation rate constants for specific binding. The In vivo kinetics of
this binding differed significantly from the kinetics of specific binding of
the saae compounds studied In vitro. By using this model and varying the
specific activity of the radioligand administered, the concentration of
neuroleptic receptors In various brain regions may be determined In vivo.
This research was carried out at Brookhaven National Laboratory under
contract DE-ACC?.-?6CH00016 with the 0. S. Department of Energy and supported
by Its Office of Health and Environmental Kesearch and also supported by
National Institutes of Health Grant HS-15380.
1. Arnett, CD, Shlue C-T, Volf AP, Ptowler JS, Logan J, and Vatanabe N
(1985) Comparison of three *®P-labaled butyrophsnons neuroleptic drugs
In the baboon ”i%ias positron emission tomography. J. Neurochem. 44,
835-844.
2. Shlue C-T, Fowler JS, Volf AP, Vatanabe M, and Arnett CD (1985)
Syntheses and specific activity determinations of no-carrier-added
(NCA) 1BP-labeled butyrophenone neuroleptics - benperldol, haloperldol,
spiroperidol and plpamperone. J. Hud. Med. 26, 181-186.
3. Shlue C-T, Fowler JS, Volf AP, McPherson DV, Arnett CD, and Zecca L
(1985) Mo-carrler-added (NCA) l°F-labeled ll-methylsplroperldol -
Synthesis and blodlstrlbutlon In mice. (Submitted).
4. Arnett CD, Fowler JS, Volf AP, Shlue C-T, and McPherson DV (1985)
[18F]-IHlfathylsplroperldol: the radioligand of choice for PETT studies
of the dopamine receptor in human brain. Life Scl. 36, 1359-1366.
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Arnett, C. D.; Fowler, J. S.; Wolf, A. P.; Shiue, C. Y. & Logan, J. Positron-emitting radioligands for imaging neuroleptic receptors, article, January 1, 1985; Upton, New York. (https://digital.library.unt.edu/ark:/67531/metadc1069861/m1/2/: accessed July 16, 2024), University of North Texas Libraries, UNT Digital Library, https://digital.library.unt.edu; crediting UNT Libraries Government Documents Department.