Development of selective 5-HT2AR Agonists
Activation of the serotonin 2A receptor (5-HT2AR) is directly linked to the psychedelic effects of classic hallucinogens like psilocybin and LSD that interact with several receptors in the CNS – including the 5-HT2AR. The effects of selectively activating the 5-HT2AR are unknown, as appropriate agonist ligands remain elusive. In order to gain a better understanding of the effects of classic hallucinogens we are trying to develop a selective 5-HT2AR agonist. Our research is primarily based on the design and synthesis of new ligands followed by characterization in various assays within molecular, cellular and in vivo pharmacology – in the pursuit of a suitable candidate that could be advanced into clinical research.
Jesper L. Kristensen is Assoc. Professor at the Department of Drug Design and Pharmacology, University of Copenhagen in Denmark. His research deals with the development of selective ligands targeting various CNS targets. Within CIMBI (Center for Integrated Molecular Brain Imaging) he has been involved in the development of selective ligands and PET-tracers that can be used to study and image the 5-HT2A receptor – the site of action of classic hallucinogens like psilocybin.