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The effects of 5-hydroxy-6-methyl-2-aminotetralins were evaluated for central and presynaptic peripheral dopaminergic activity. Di-ethyl (DK-121) and di-propyl (DK-118) derivatives inhibited the tachycardia produced by postganglionic cardioaccelerator nerve stimulation in the cat. This effect was blocked by haloperidol (100 micrograms/kg). DK-118 inhibited stimulation-induced contraction of the cat nictitating membrane. The pressor response produced by lumbar sympathetic chain stimulation in the isolated hindlimb of the cat was inhibited by DK-118 following intravenous administration. Reflex sympathetic activation produced by 30 sec bilateral carotid occlusion was also inhibited by DK-118 in the dog. Centrally, DK-118 caused contralateral circling behavior in rats who had unilateral lesions of the caudate nucleus. DK-118 did not effect DOPA levels in either the caudate nucleus or olfactory tubercle. In contrast, DK-121 decreased DOPA levels in the caudate nucleus but did not produce circling behavior in rats. Both compounds have weak emetic activity in dogs. These results suggest that DK-121 and DK-118 possess stimulant properties on dopaminergic receptors in the central and peripheral nervous system. However, DK-121 does not appear to stimulate postsynaptic dopamine receptors in the central nervous system.
T Verimer, and
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R K Bhatnagar, and
D L Koble, and
J G Cannon, and
J R Flynn, and
D B Goodale, and
S P Arnerić
August 1984,
Journal of medicinal chemistry,
T Verimer, and
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D L Koble, and
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J R Flynn, and
D B Goodale, and
S P Arnerić
June 1986,
Journal of medicinal chemistry,
T Verimer, and
J P Long, and
R K Bhatnagar, and
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J R Flynn, and
D B Goodale, and
S P Arnerić
December 1975,
Journal of medicinal chemistry,
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S P Arnerić
December 1985,
Journal of medicinal chemistry,
T Verimer, and
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D L Koble, and
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J R Flynn, and
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S P Arnerić
January 1967,
Journal of the Chemical Society. Perkin transactions 1,
T Verimer, and
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S P Arnerić
October 1951,
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February 1987,
The Journal of pharmacy and pharmacology,
T Verimer, and
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March 1993,
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine,
T Verimer, and
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S P Arnerić
March 1956,
Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft,
T Verimer, and
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D B Goodale, and
S P Arnerić
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Journal of medicinal chemistry,
