PHNO, a novel dopamine agonist, in animal models of parkinsonism.

PHNO, a naphthoxazine compound, was investigated in animal models of central dopaminergic activity. The drug in doses of 5-300 micrograms/kg when administered subcutaneously, or transdermally, induced stereotypic behavior in rats which was blocked by haloperidol but not by reserpine pretreatment. In rats with unilateral 6-hydroxydopamine lesions of the substantia nigra PHNO induced dose-dependent contralateral turnings. The drug caused emesis in dogs and hypothermia in mice. PHNO bound to D-2 dopamine receptors in the rat striatum. Chronic injection with PHNO did not induce behavioral supersensitivity or increase dopamine receptor density. These data indicate that PHNO is a direct acting dopamine agonist that is highly potent. PHNO differs from other dopaminergic drugs and may be useful in the treatment of Parkinson's disease.
AuthorsW Koller, G Herbster, J Gordon
JournalMovement disorders : official journal of the Movement Disorder Society (Mov Disord) Vol. 2 Issue 3 Pg. 193-9 ( 1987) ISSN: 0885-3185 [Print] UNITED STATES
PMID2904649 (Publication Type: Journal Article, Research Support, U.S. Gov't, Non-P.H.S.)
Chemical References
  • Dopamine Agents
  • Oxazines
  • Receptors, Dopamine
  • naxagolide
  • Animals
  • Corpus Striatum (drug effects)
  • Dopamine Agents (therapeutic use)
  • Dose-Response Relationship, Drug
  • Injections, Subcutaneous
  • Male
  • Oxazines (therapeutic use)
  • Parkinson Disease, Secondary (drug therapy)
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine (drug effects)
  • Stereotyped Behavior (drug effects)

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