DOPAMINE RECEPTOR STIMULATING ACTIVITY OF 5-HYDROXY-6-METHYL-2-AMINOTETRALIN DERIVATIVES

  • 1 January 1981
    • journal article
    • research article
    • Vol. 250  (2) , 221-241
Abstract
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 .mu.g/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 after i.v. administration. Reflex sympathetic activation produced by 30 s bilateral carotid occlusion was inhibited by DK-118 in the dog. Centrally, DK-118 caused contralateral circling behavior in rats that had unilateral lesions of the caudate nucleus. DK-118 did not effect dopa levels in the caudate nucleus or olfactory tubercle. 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. DK-121 and DK-118 possess stimulant properties on dopaminergic receptors in the central and peripheral nervous system. DK-121 does not appear to stimulate postsynaptic dopamine receptors in the CNS.