Studies of uptake of the bretylium analogue, iodobenzyltrimethylammonium iodide, by non-primate, monkey and human hearts

Br J Clin Pharmacol. 1979 Nov;8(5):425-32. doi: 10.1111/j.1365-2125.1979.tb01021.x.

Abstract

Uptake of (+/-)-[3H]-noradrenaline, [14C]-bretylium and [125I]-o-iodobenzyltrimethylammonium iodide (RIBA) by rat heart was studied by the Langendorff technique. All three compounds showed significant uptake. 2 Corticosterone and 17-beta-oestradiol inhibited the uptake of all three compounds by rat heart, a finding consistent with extraneuronal uptake (uptake2). 3 [131I]-RIBA was injected intravenously into pigs and monkeys (M. speciosus). Myocardial samples taken from pigs killed 1 and 2 h after injection showed significant uptake. No significant uptake was found in myocardial samples of monkeys killed 10 min, 2 h and 24 h, respectively, after injection. 4 Four normal human volunteers received [125I]-RIBA intravenously and the image of the precordial area was followed by means of scintillation camera for the first 4 h after injection. In two of the subjects, the scintigrams were repeated at 22 and 23 h after injection, respectively. No evidence of myocardial uptake was observed. 5 These results suggest the possibility that man and at least one other primate species may differ from lower species with regard to uptake.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Animals
  • Bretylium Compounds / metabolism*
  • Female
  • Haplorhini
  • Humans
  • In Vitro Techniques
  • Iodobenzenes / metabolism
  • Macaca
  • Male
  • Myocardium / metabolism*
  • Norepinephrine / metabolism
  • Rats
  • Species Specificity
  • Swine

Substances

  • Bretylium Compounds
  • Iodobenzenes
  • iodobenzyltrimethylammonium
  • Norepinephrine