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Is domperidone a selective peripheral dopamine-receptor antagonist in vivo?

Abstract
The ability of domperidone (DOM) to antagonize dopamine (DA) receptor agonist-induced hypothermia or hyperactivity was investigated in rats. Apomorphine (APO) or RDS-127 (2-di-n-propylamino-4,7-dimethoxyindane), two DA receptor agonists, produced dose-dependent hypothermia following subcutaneous (s.c.) administration. Also, RDS-127 produced hypothermia following lateral ventricular (i.c.v.) administration. The hypothermia produced by apomorphine or RDS-127 (given s.c. or i.c.v.) was antagonized by pretreatment with pimozide (0.25 mg/kg, i.p.) or domperidone (0.2, 1.0 and 5.0 mg/kg, i.p.). The hyperactivity produced by apomorphine was unaffected by pretreatment with domperidone. These data suggested that central DA receptors mediating temperature regulation, but not those mediating locomotor activity are accessible to peripherally administered domperidone. Therefore, domperidone may not be useful to differentiate hypothalamic (central) vs peripheral sites of action for DA receptor agonists in the rat.
AuthorsS P Arnerić, E D Collins, R K Bhatnagar, J P Long
JournalNeuropharmacology (Neuropharmacology) Vol. 21 Issue 12 Pg. 1317-21 (Dec 1982) ISSN: 0028-3908 [Print] England
PMID7155311 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Receptors, Dopamine
  • Pimozide
  • Domperidone
Topics
  • Animals
  • Body Temperature (drug effects)
  • Domperidone (pharmacology)
  • Male
  • Motor Activity (drug effects)
  • Pimozide (pharmacology)
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine (drug effects)
  • Time Factors

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