Effect of the bradykinin B2 receptor antagonist Hoe140 in experimental pneumococcal meningitis in the rat

Eur J Pharmacol. 1996 Jul 25;308(3):335-41. doi: 10.1016/0014-2999(96)00375-5.

Abstract

To elucidate the role of bradykinin in the complex pathophysiology of bacterial meningitis we investigated the effect of the bradykinin B2 receptor antagonist Hoe140, icatibant (D-Arg[Hyp3-Thi5-D-Tic7-Oic8]-bradykinin), on pathophysiological alterations in experimental pneumococcal meningitis. Untreated rats injected intracisternally (i.c.) with heat-killed pneumococci developed an increase of regional cerebral blood flow (185.4 +/- 27.4%, baseline 100%, mean +/- S.D.), brain water content (79.16 +/- 0.23%), intracranial pressure (21.4 +/- 6.0 mm Hg), and white blood cell count in the cerebrospinal fluid (CSF) (4621 +/- 1894 cells/microliter) within 6 h after i.c. challenge. Treatment with Hoe140 (0.1 mg/kg i.v. at baseline and 0.05 mg/kg s.c. at 2 h after i.c. challenge) attenuated the increase of brain water content (78.53 +/- 0.28%; P < 0.05), intracranial pressure (7.5 +/- 2.2 mm Hg; P < 0.05), and regional cerebral blood flow (128.6 +/- 23.1%; P < 0.05), and reduced CSF pleocytosis (2690 +/- 1898 cells/microliter. N.S.). When treatment was started 4 h after i.c. challenge Hoe140 reduced intracranial pressure (P < 0.05), but was no more capable to significantly influence the other pathophysiological parameters. Treatment with lower (0.01 mg/kg i.v. at baseline, followed by 0.005 mg/kg s.c. at 2 h) and higher (2 mg/kg i.v., followed by 1 mg/kg s.c. at 2 h) concentrations of Hoe140 was ineffective. Likewise, i.c. injection of Hoe140, at different dosages (4 nmol, 40 nmol, 400 nmol) did not significantly alter the pathophysiological parameters in pneumococci-induced meningitis, but caused changes in mean arterial blood pressure at dosages greater than 4 nmol. We conclude that bradykinin is involved as an inflammatory mediator of microvascular changes, brain edema, and increased intracranial pressure during the early phase of experimental pneumococcal meningitis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Infective Agents / administration & dosage
  • Anti-Infective Agents / pharmacology
  • Anti-Infective Agents / therapeutic use*
  • Body Water
  • Bradykinin / administration & dosage
  • Bradykinin / analogs & derivatives*
  • Bradykinin / pharmacology
  • Bradykinin / therapeutic use
  • Bradykinin Receptor Antagonists*
  • Brain / blood supply
  • Brain / drug effects
  • Disease Models, Animal
  • Interleukin-6 / cerebrospinal fluid
  • Intracranial Pressure / drug effects
  • Leukocyte Count
  • Male
  • Meningitis, Pneumococcal / cerebrospinal fluid
  • Meningitis, Pneumococcal / drug therapy*
  • Meningitis, Pneumococcal / physiopathology
  • Nitrites / cerebrospinal fluid
  • Rats
  • Rats, Wistar
  • Receptor, Bradykinin B2

Substances

  • Anti-Infective Agents
  • Bradykinin Receptor Antagonists
  • Interleukin-6
  • Nitrites
  • Receptor, Bradykinin B2
  • icatibant
  • Bradykinin