Histamine receptors in an experimental mammary carcinoma

Biomed Pharmacother. 1994;48(8-9):399-406. doi: 10.1016/0753-3322(94)90058-2.

Abstract

An experimental mammary carcinoma was induced in Sprague-Dawley rats by the ip administration of N-nitroso-N-methylurea (NMU) in three doses of 50 mg/kg. In order to study the expression of histamine receptors in these experimental tumors, the presence of specific binding sites for histamine was studied. Using [3H]-histamine as a radioligand, two specific binding sites were characterized on the cell membrane. The first site, of high affinity, Kd = 4 +/- 2 nM, was further characterized as an H2 type using [3H]-cimetidine and [3H]-tiotidine as radioligands and by displacement experiments with different histamine agonists and antagonists. The second one of low affinity, Kd = 35 +/- 14 nM, needs further characterization. The determination of cAMP levels showed that histamine and the H2 agonist dimaprit, produced a significant decrease in the nucleotide concentration 6 minutes after stimulation, in a response that was specifically abolished by H2 antagonists. Based on these results, we conclude that neoplastic cells from NMU induced tumors express H2 histamine membrane receptors which are coupled to a transductional pathway different from cAMP production, which may be involved in the regulation of tumor growth.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carcinoma / chemically induced
  • Carcinoma / metabolism*
  • Cyclic AMP / analysis
  • Histamine Antagonists / pharmacology
  • Mammary Neoplasms, Experimental / chemically induced
  • Mammary Neoplasms, Experimental / metabolism*
  • Methylnitrosourea / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Histamine / metabolism*

Substances

  • Histamine Antagonists
  • Receptors, Histamine
  • Methylnitrosourea
  • Cyclic AMP