Clonidine displacement from type 1 imidazoline receptor by p-aminobenzamidine, the prototype of trypsin-like serine protease inhibitors

Valentina Pallottini, Maria Marino, Paolo Ascenzi

Research output: Contribution to journalArticle

Abstract

p-Aminobenzamidine inhibits competitively the catalytic activity of enzymes that recognize preferentially the L-arginyl side chain and related structures. Notably, p-aminobenzamidine is considered as the prototype of trypsin-like serine protease inhibitors. Furthermore, p-aminobenzamidine inhibits the catalytic activity of nitric oxide synthase type I and type II as well as copper amine oxidase. Taking into account the structural similarity between p-aminobenzamidine, agmatine (the putative endogenous ligand of the membrane type 1 imidazoline receptor (I1-R)), and N-amidino-2-hydroxypyrrolidine (the product of agmatine oxidation by copper amine oxidase), the [3H]clonidine displacement from I1-R in rat heart membranes by p-aminobenzamidine was investigated. p-Aminobenzamidine is as effective as agmatine and N-amidino-2-hydroxypyrrolidine and more effective than the antihypertensive drug clonidine to displace [3H]clonidine from I1-R. Therefore, trypsin-like serine protease inhibitors structurally related to p-aminobenzamidine should be administrated under careful control.

Original languageEnglish
Pages (from-to)301-304
Number of pages4
JournalIUBMB Life
Volume54
Issue number5
DOIs
Publication statusPublished - Nov 1 2002

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Serine Proteinase Inhibitors
Clonidine
Agmatine
Amine Oxidase (Copper-Containing)
Catalyst activity
Membranes
Nitric Oxide Synthase Type I
Nitric Oxide Synthase Type II
imidazoline I1 receptors
trypsin-like serine protease
4-aminobenzamidine
Antihypertensive Agents
Rats
Ligands
Oxidation
Enzymes

Keywords

  • Agmatine
  • Clonidine
  • N-amidino-2-hydroxypyrrolidine
  • p-aminobenzamidine
  • Type 1 imidazoline receptor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology

Cite this

Clonidine displacement from type 1 imidazoline receptor by p-aminobenzamidine, the prototype of trypsin-like serine protease inhibitors. / Pallottini, Valentina; Marino, Maria; Ascenzi, Paolo.

In: IUBMB Life, Vol. 54, No. 5, 01.11.2002, p. 301-304.

Research output: Contribution to journalArticle

Pallottini, Valentina ; Marino, Maria ; Ascenzi, Paolo. / Clonidine displacement from type 1 imidazoline receptor by p-aminobenzamidine, the prototype of trypsin-like serine protease inhibitors. In: IUBMB Life. 2002 ; Vol. 54, No. 5. pp. 301-304.
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