Dihydrexidine: a new potent peripheral dopamine D1 receptor agonist

Eur J Pharmacol. 1993 Apr 22;235(1):31-5. doi: 10.1016/0014-2999(93)90816-z.

Abstract

Dihydrexidine (trans-10,11-dihydroxyhexahydrobenzo-[a]phenanthridine) was found to be a full dopamine D1 receptor agonist with a potency five times that of dopamine. Dihydrexidine showed no agonist activity at peripheral dopamine D2 receptors, alpha- or beta-adrenoceptors at the doses which produced near maximal stimulation of dopamine D1 receptors. The chemical structure of dihydrexidine shows that addition of a phenyl ring to a benzo[f]quinoline moiety bestows potent D1 activity upon a structure which had no such activity previously. This observation introduces a new factor in structure-activity considerations for dopamine receptor ligands.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Blood Pressure / drug effects
  • Dogs
  • Dopamine / pharmacology
  • Dopamine Agents / pharmacology*
  • Heart Rate / drug effects
  • Kidney / blood supply
  • Kidney / drug effects
  • Phenanthridines / pharmacology*
  • Receptors, Adrenergic, alpha / drug effects
  • Receptors, Adrenergic, beta / drug effects
  • Receptors, Dopamine D1 / drug effects*
  • Receptors, Dopamine D1 / metabolism
  • Renal Circulation / drug effects
  • Structure-Activity Relationship
  • Vascular Resistance / drug effects

Substances

  • Dopamine Agents
  • Phenanthridines
  • Receptors, Adrenergic, alpha
  • Receptors, Adrenergic, beta
  • Receptors, Dopamine D1
  • dihydrexidine
  • Dopamine