Effect of tuamine, heptaminol and two analogues on uptake and release of catecholamines in cultured chromaffin cells

Biochem Pharmacol. 1990 Aug 15;40(4):821-5. doi: 10.1016/0006-2952(90)90322-c.


The effects of tuamine (1-methylhexylamine), a sympathomimetic compound with hypertensive properties, heptaminol (6-amino-2-methyl-2-heptanol), an aliphatic amine with pressor properties, and two structural analogues of tuamine on high-affinity Na(+)-dependent noradrenaline uptake and on nicotine-evoked release were examined in bovine chromaffin cells maintained in primary culture for 3 to 6 days. Tuamine was found to be a potent competitive inhibitor of noradrenaline uptake with an effect similar to that of cocaine. Its inhibition constant (Ki) was 1.1 +/- 0.1 microM while Ki values of heptaminol, of 1-methylamino-5-pentanol oxalate and of 5-amino-2-methylhexanol oxalate, which were also found to be competitive inhibitors of noradrenaline uptake, were 60 +/- 2 microM, 260 +/- 28 microM and 48 +/- 76 microM, respectively. Tuamine, hepataminol and 5-amino-2-methyl-2-hexanol were also shown to be inhibitors of nicotine-induced release of catecholamines, with IC50 values of 26 +/- 2 microM, 650 +/- 11 microM and 500 +/- 10 microM, respectively. Tuamine and hepataminol did not inhibit noradrenaline release evoked by 59 mM K+, suggesting that it acts at a step prior to calcium entry. The pharmacological properties of heptaminol as an anti-hypotension agent may partially account for its inhibitory effect on catecholamine uptake and release.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / pharmacology*
  • Amino Alcohols / pharmacology*
  • Animals
  • Cattle
  • Cells, Cultured
  • Chromaffin Granules / drug effects
  • Chromaffin Granules / metabolism*
  • Chromaffin System / metabolism*
  • Heptaminol / pharmacology*
  • Nicotine / pharmacology
  • Norepinephrine / metabolism*
  • Structure-Activity Relationship
  • Sympathomimetics / pharmacology*


  • Amines
  • Amino Alcohols
  • Sympathomimetics
  • Heptaminol
  • Nicotine
  • Norepinephrine
  • tuaminoheptane