Synthesis and anticonvulsant activity of 1,2-aminoalkanol derivatives

Acta Pol Pharm. 1998 Nov-Dec;55(6):487-98.

Abstract

A series of 1,2-aminoalkanol derivatives were prepared and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scMet) assays and for neurotoxicity (TOX). Most interesting were the anticonvulsant results of S-(+)-2-amino-1-butanol derivative VIII, which displayed anti-MES activity with a protective index (TD50/ED50) of 4.55 corresponding with that for phenytoin, carbamazepine and valproate.

MeSH terms

  • Amino Alcohols / chemical synthesis*
  • Amino Alcohols / metabolism
  • Amino Alcohols / pharmacology
  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / metabolism
  • Anticonvulsants / pharmacology
  • Binding, Competitive / drug effects
  • Convulsants
  • In Vitro Techniques
  • Injections, Intraperitoneal
  • Magnetic Resonance Spectroscopy
  • Male
  • Mice
  • Pentylenetetrazole
  • Rats
  • Rats, Sprague-Dawley
  • Seizures / chemically induced
  • Seizures / prevention & control
  • Synaptosomes / drug effects
  • Synaptosomes / metabolism

Substances

  • Amino Alcohols
  • Anticonvulsants
  • Convulsants
  • Pentylenetetrazole