Supervisors info:
ΑΝΔΡΕΑΣ ΤΣΟΤΙΝΗΣ, ΚΑΘΗΓΗΤΗΣ ΤΜΗΜ. ΦΑΡΜΑΚΕΥΤΙΚΗΣ ΕΚΠΑ (ΕΠΙΒΛΕΠΩΝ)
ΙΩΑΝΝΗΣ ΠΑΠΑΝΑΣΤΑΣΙΟΥ, ΕΠΙΚΟΥΡΟΣ ΚΑΘΗΓΗΤΗΣ ΤΜΗΜ. ΦΑΡΜΑΚΕΥΤΙΚΗΣ ΕΚΠΑ
ΔΗΜΗΤΡΙΟΣ ΠΑΠΑΧΑΤΖΗΣ, ΔΙΕΥΘΥΝΤΗΣ ΕΡΕΥΝΩΝ Ε.Ι.Ε
Summary:
The (-)-Δ9-tetrahydrocannabinol (Δ9THC) is the main psychotropic component of cannabis, which originates from the Cannabis Sativa L. plant. In 1964 the identification of Δ9-THC led to the creation of a unique class of compounds that was named cannabinoids. The pharmaceutical use of cannabis from ancient times gave the stimulus for the scientific community to study its effect on the human organism. This was followed by the discovery and cloning of the two known receptors of cannabinoids, CB1 and CB2, which act through G proteins and also, by the characterization of the endogenous cannabinoid system. Anandamide is the main representative of endocannabinoids, a series of compounds structurally different from phytocannabinoids which are produced by the human body and interact with the cannabinoid receptors.
Cannabinoid receptors' involvement to a plethora of the organism’s functions and responses, render the CB1 and CB2 receptors as pharmaceutical targets. Through the development of synthetic cannabinoid mimetic analogues, important information is provided regarding the stereochemical requirements for recognizing and activating the receptors. Concurrently, structure-activity studies of natural and synthetic cannabinoids have indicated the basic pharmacophores in their structure. Research in the field of cannabinoids focuses on the designing and synthesizing improved cannabinoid mimetic analogues, with higher affinity and selectivity for CB1 and CB2 receptors. Nowadays, there are many candidate drugs in advanced phases of clinical trials, but also approved medicines, like the anti-emetic drug Cesamet, which belongs to the cannabinoid class.
Cannabinoids are a very promising field of research for combating disease and battling symptoms that have, until now, no cure. The present project focuses on developing new cannabinoid mimetic analogs of Δ8-THC and 11-hydroxy-Δ8-THC. The design and synthesis of these new analogues are based on the 1',1'-heterocyclic substitution of the side chain, which constitutes the major pharmacophore group of classical cannabinoids.
Keywords:
Cannabinoids, Δ8 THC analogues, Cannabinomimetic analogues, CBD
