Opioid Bioactivity

Medicinal Chemistry Group

The critical pharmacological and physiological assessment of the bioactivity of these novel opioid ligands containing Dmt provided evidence on their antinociceptive mode of action as potential drugs that act centrally and peripherally. Non-human animal studies are an obligatory step prior clinical trials and therapeutic applications.

The essential key to understand the inherent biological activity of an opioid substance required in all drug applications for eventual human therapeutic applications consist of demonstration of efficacy in vivo using several distinct species of animals and tested for toxicity. In the initial studies conducted during the past two years, we focused on two main objectives:

1. Antinociception elicited by µ- and δ-opioid receptor agonists, and inhibition of analgesia by antagonists
2. Determination of the biological accessibility of these compounds

Application at peripheral sites (subcutaneous, intravenous, intradermal, per oral) would imply transport through epithelial membranes, transit by the blood to and passage through the intractable blood-brain barrier resulting in analgesia.

For more information on the Medicinal Chemistry Group’s opioid bioactivity research, see the following links.

• Accomplishments
• Conclusions