Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...
Patent
1987-04-29
1989-10-03
Maples, John S.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
546 20, A61K 4902, C07D47110
Patent
active
048715271
ABSTRACT:
There is disclosed radioligands labeled with the position emitting radionuclide [.sup.18 F] suitable for dynamic study in living humans with position emission transaxial tomography. These new [.sup.18 F]-N-fluoroalkylspiroperidols, wherein the alkyl group contains from 2-6 carbon atoms, exhibit extremely high affinity for the dopamine receptors and provide enhanced uptake and retention in the brain concomitant with reduced radiation burden. These characteristics all combine to make these new radioligands useful for mapping dopamine receptors in normal and disease states in the living brain. Additionally, a new synthetic procedure for these radioligands as well as a new procedure for preparing the radiolabeled alkyl halide alkylating reagents are also disclosed.
REFERENCES:
patent: 4656280 (1987-04-01), Garlick
Welch, Michael J. et al., "Biodistribution of Derivatives of Spiroperidols", Nucl. Med. Biol., 2/2/1986, 13(5), 523-6, [Chem. Absts. 106:134386w].
Satyamurthy, Nagichettiar et al, "NCA 3-(2-Fluoroethyl)Spiperone", Nucl. Med. Biol., 2/6/1986, 13(6), 617, 620-21, 623-626-27, [Chem. Absts. 106:134389z].
Bai Lan-Qin
Shiue Chyng-Yann
Teng Ren-Tui
Wolf Alfred P.
Bogosian Margaret C.
Hightower Judson R.
Maples John S.
The United States of America as represented by the United States
Weinberger James W.
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