1-[(IMIDAZOLIN-2-YL)AMINO]INDOLINE AND 1-[(IMIDAZOLIN-2 YL)AMINO] 1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES: NEW INSIGHTS INTO THEIR CIRCULATORY ACTIVITIES

Acta Pol Pharm. 2015 Mar-Apr;72(2):277-87.

Abstract

N-[(Imidazolin-2-yl)amino]indolines and N-[(imidazolin-2-yl)amino]-1,2,3,4-tetrahydroquinolines, previously described in patent literature as hypertensive agents, were synthesized and tested in viny for their affinities to α1- and α2-adrenoceptors as well as imidazoline I, and I2 receptors. The compounds most potent at either α1- or α2-adrenoceptors were administered intravenously to normotensive Wistar rats to determine their effects on mean arterial blood pressure and heart rate. Upon intravenous administration at dose of 0.1 mg/kg to normotensive male Wistar rats, the initial transient pressor effect was followed by long-lasting hypotension and bradycardia. In view of the above results the 1-[(imidazolin-2-yl)amino]indolines and [(imidazolin-2-yl)amino]-1,2,3,4-tetrahydroquinolines are now found to possess circulatory profile characteristic of the centrally acting clonidine-like hypotensive imidazolines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Pressure / drug effects*
  • Heart Rate / drug effects*
  • Imidazoline Receptors / metabolism
  • Imidazolines / pharmacology*
  • Indoles / pharmacology
  • Male
  • Quinolines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Adrenergic, alpha / metabolism

Substances

  • Imidazoline Receptors
  • Imidazolines
  • Indoles
  • Quinolines
  • Receptors, Adrenergic, alpha
  • indoline