Pharmacological characterization and therapeutic potential for the treatment of opioid abuse with ATPM-ET, an N-ethyl substituted aminothiazolomorphinan with κ agonist and μ agonist/antagonist activity

Eur J Pharmacol. 2014 Oct 5:740:455-63. doi: 10.1016/j.ejphar.2014.06.045. Epub 2014 Jul 3.

Abstract

We previously reported that the κ agonists with mixed μ activity could attenuate heroin self-administration with less potential to develop tolerance. The present study further investigated the effects of (-)-3-N-Ethylamino-thiazolo[5,4-b]-N-cyclopropylmethylmorphinan hydrochloride (ATPM-ET), a κ agonist and μ agonist/antagonist, on the acquisition and reinstatement of morphine-induced conditioned place preference (CPP), heroin self-administration and heroin-primed reinstatement of drug-seeking behavior. We found that ATPM-ET produced a longer duration of potent antinociceptive effects with less side effect of sedation. More importantly, ATPM-ET attenuated the acquisition of morphine-induced CPP, without affecting the reinstatement of morphine CPP. Furthermore, ATPM-ET significantly inhibited heroin self-administration and the reinstatement of heroin primed drug-seeking behavior. Taken together, ATPM-ET, a novel κ agonist and μ agonist/antagonist may have utility for the treatment of drug dependence.

Keywords: Antinociception; CPP; Heroin self-administration; Reinstatement of drug-seeking behavior; Sedation; κ agonist and μ agonist/antagonist.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics, Opioid / administration & dosage
  • Animals
  • Conditioning, Psychological
  • Drug-Seeking Behavior / drug effects
  • Heroin Dependence / drug therapy*
  • Male
  • Mice
  • Morphinans / therapeutic use*
  • Morphine / administration & dosage
  • Narcotic Antagonists / therapeutic use*
  • Pain / drug therapy
  • Rats, Sprague-Dawley
  • Receptors, Opioid, kappa / agonists*
  • Receptors, Opioid, mu / agonists*
  • Receptors, Opioid, mu / antagonists & inhibitors*
  • Self Administration

Substances

  • 3-N-ethylaminothiazolo(5,4-b)-N-cyclopropylmethylmorphinan hydrochloride
  • Analgesics, Opioid
  • Morphinans
  • Narcotic Antagonists
  • Receptors, Opioid, kappa
  • Receptors, Opioid, mu
  • Morphine