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Flupenthixyl chloride (FPT-Cl), a derivative of the dopamine (DA) receptor antagonist and neuroleptic alpha-flupenthixol possessing a chloroethyl side chain, has been prepared and evaluated for use in vivo in affinity labeling of DA receptors. Binding of [3H]spiperone to rat striatal DA receptors was markedly altered up to 12 h after intraventricular injection of FPT-Cl as compared with controls, while Scatchard plots of [3H]spiperone binding obtained on rat striatal homogenates 24 and 48 h after injection of FPT-Cl had values of Bmax significantly lower than in controls. The results suggest that the administration of FPT-Cl leads to irreversible and possibly covalent blockade of a portion of the spiperone binding sites in rat striatum. A second population of receptors appears to be blocked reversibly and presumably noncovalently by FPT-Cl, and these spiperone binding sites are partially reactivated in vivo after 48 h.
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
January 1985,
The Journal of pharmacology and experimental therapeutics,
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
January 1983,
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D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
April 1982,
Neuropharmacology,
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
January 1985,
Naunyn-Schmiedeberg's archives of pharmacology,
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
December 1987,
Brain research,
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
April 2001,
Journal of clinical psychopharmacology,
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
November 1981,
Biochemical pharmacology,
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
July 1982,
Life sciences,
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
November 1990,
Neuropharmacology,
D I Schuster, and
W L Holden, and
A P Narula, and
R B Murphy
January 2011,
Naunyn-Schmiedeberg's archives of pharmacology,
