Name: Héctor Manuel Torres Gómez
Diploma / M.Sc degree: Autonomous University of Morelos State, Mexico
(November 2009)

PhD Project: Design and synthesis of conformationally restricted selective σ₂ receptor ligands with the propellane scaffold

Abstract of Research Project

The sigma (σ) receptor was first described as a subtype of opioid receptors. Subsequent studies revealed that sigma binding sites are a distinct class of receptors and are classified in σ₁ and σ₂ subtypes. These receptors are localized in different tissues, including central nervous system and various organs and tissues in the periphery. Whereas the σ₁ receptor has been cloned, the σ₂ subtype isolation and characterization have not been carried out yet, although a number of studies reported evidences linking σ₂ receptors with several biological processes. Thus, selective σ₂ agonists and antagonists may be potentially useful drugs for the treatment of several pathological conditions such as psychiatric disorders, cocaine abuse, memory and learning disorders, dyskinesia and dystonic reactions induced by classical antipsychotic drugs, neurophatic pain and cancer. The aim of this work is the development of a new class of highly selective σ₂ receptor ligands, using the rigid propellane scaffold to fix the three-dimensional orientation of the pharmacophoric elements to each other. The new compounds should show high σ₂ affinity and high selectivity over the σ₁ subtype and related receptors.



Publications

H. Torres-Gómez, K. Lehmkuhl, D. Schepmann, B. Wünsch
Design, synthesis and receptor affinity of novel conformationally restricted σ ligands based on the [4.3.3]propellane scaffold
European Journal of Medicinal Chemistry 70 (2013), 78-87.


Héctor Manuel Torres Gómez
eMail: Héctor Manuel Torres Gómez