-transparent.png){kind=logo}
A method is described for the rapid production and purification of new potential dopamine agonists. Via thermal heating (refluxing in an oil bath) and microwave exposure 2-[N-n-3-fluoropropyl-N-(4-methylphenyl)ethylamino]-5-hydroxyte tralin (12), 2-[N-n-3-fluoropropyl-N-(4-fluorophenyl)ethylamino]-5-hydroxyte tralin (13), and their isotopic fluorine-18 derivatives were synthesized, respectively. The fluorine-18 label was introduced via N-fluoroalkylation with no-carrier-added (n.c.a.) 18FCH2CH2CH2I. In 115 min, radiochemical yields of 11% (corrected for decay) were achieved for both compounds. The specific activity ranged from 15-75 GBq/mumol. After i.v. injection in rats, the fluorine-18 labeled compounds were evaluated for their in vivo binding to the D2-receptors. The radioactivity levels in the striatum, nucleus accumbens and tuberculum olfactorius were not significantly higher than in the cerebellum and frontal cortex at 15, 30 and 60 min after administration of the tetralin derivatives. Dopamine depletion with reserpine did not affect the uptake in the dopamine D2-receptor rich area. Remarkable high uptakes were found in the adrenal for both compounds.
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
April 1993,
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine,
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
July 1980,
Journal of medicinal chemistry,
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
April 2023,
Molecules (Basel, Switzerland),
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
October 1994,
Journal of nuclear medicine : official publication, Society of Nuclear Medicine,
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
April 1981,
Archives internationales de pharmacodynamie et de therapie,
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
March 2021,
Molecular pharmaceutics,
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
October 1977,
Steroids,
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
November 1994,
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine,
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
January 1994,
Nuclear medicine and biology,
S Zijlstra, and
P H Elsinga, and
E Z Oosterhuis, and
G M Visser, and
J Korf, and
W Vaalburg
November 2007,
Seminars in nuclear medicine,
