D2 and D1 dopaminergic activity of 7-OH-DPAT

Brain Res. 1996 Sep 9;733(1):41-5. doi: 10.1016/0006-8993(96)00531-8.

Abstract

The D1 and D2 dopamine receptor agonist properties of 7-hydroxy-2-(N,N-di-n-propylamino) tetraline (7-OH-DPAT) was determined by investigating the effect of this compound on rat striatal acetylcholine (ACh) concentration and increase in cAMP formation in primary cerebellar granule cell cultures. 7-OH-DPAT at low doses (0.01 to 0.1 mumol/ kg) had no significant effect, and at high doses (0.3 to 30 mumol/kg) significantly (P < 0.01) increased striatal ACh levels. Likewise, quinpirole was found to significantly elevate ACh content. Pretreatment with haloperidol, a non-selective antagonist of the D2 family of receptors, significantly (P < 0.01) blocked 7-OH-DPAT- and quinpirole-induced increases in ACh. U-99194A, a D3 selective dopamine antagonist, had no significant effect on 7-OH-DPAT-induced increases in striatal ACh. However, raclopride, a D2 selective dopamine antagonist, completely blocked 7-OH-DPAT-induced elevations in ACh. 7-OH-DPAT in the mumolar range increased cAMP formation in granule cell cultures, and this effect was antagonized by SCH 23390, a D1 selective dopamine antagonist. The neurochemical study indicates that, at high doses, 7-OH-DPAT has both D1 and D2 agonist activities.

MeSH terms

  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine / pharmacology
  • Acetylcholine / metabolism
  • Animals
  • Benzazepines / pharmacology
  • Cells, Cultured / drug effects
  • Cells, Cultured / metabolism
  • Cerebellum / cytology
  • Cyclic AMP / metabolism
  • Dopamine Agonists / pharmacology*
  • Dopamine Antagonists / pharmacology
  • Haloperidol / pharmacology
  • Indans / pharmacology
  • Male
  • Neostriatum / drug effects
  • Neostriatum / metabolism
  • Quinpirole / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine D1 / agonists*
  • Receptors, Dopamine D2 / agonists*
  • Tetrahydronaphthalenes / pharmacology*

Substances

  • Benzazepines
  • Dopamine Agonists
  • Dopamine Antagonists
  • Indans
  • Receptors, Dopamine D1
  • Receptors, Dopamine D2
  • Tetrahydronaphthalenes
  • (5,6-dimethoxyindan-2-yl)dipropylamine
  • Quinpirole
  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine
  • Cyclic AMP
  • Haloperidol
  • Acetylcholine
  • 7-hydroxy-2-N,N-dipropylaminotetralin