Title:Impact of Cannabinoid Receptors in the Design of Therapeutic Agents
against Human Ailments
Volume: 23
Issue: 19
Author(s): Ankush Kumar, Ojasvi Gupta, Rohit Bhatia*VikramDeep Monga*
Affiliation:
- Department of Pharmaceutical Chemistry, ISF College of Pharmacy, GT Road, Ghal Kalan, Moga, 142001, Punjab, India
- Department of Pharmaceutical Chemistry, ISF College of Pharmacy, GT Road, Ghal Kalan, Moga, 142001, Punjab, India
- Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, 151001, India
Keywords:
Cannabinoid, Cancer, Obesity, Antagonists, Heterocycles, Docking.
Abstract: The Cannabinoid (CB) signalling cascade is widely located in the human body and is associated
with several pathophysiological processes. The endocannabinoid system comprises cannabinoid
receptors CB1 and CB2, which belong to G-protein Coupled Receptors (GPCRs). CB1 receptors
are primarily located on nerve terminals, prohibiting neurotransmitter release, whereas CB2
are present predominantly on immune cells, causing cytokine release. The activation of CB system
contributes to the development of several diseases which might have lethal consequences, such as
CNS disorders, cancer, obesity, and psychotic disorders on human health. Clinical evidence revealed
that CB1 receptors are associated with CNS ailments such as Alzheimer’s disease, Huntington’s
disease, and multiple sclerosis, whereas CB2 receptors are primarily connected with immune
disorders, pain, inflammation, etc. Therefore, cannabinoid receptors have been proved to be promising
targets in therapeutics and drug discovery. Experimental and clinical outcomes have disclosed
the success story of CB antagonists, and several research groups have framed newer compounds
with the binding potential to these receptors. In the presented review, we have summarized variously
reported heterocycles with CB receptor agonistic/antagonistic properties against CNS disorders, cancer,
obesity, and other complications. The structural activity relationship aspects have been keenly
described along with enzymatic assay data. The specific outcomes of molecular docking studies
have also been highlighted to get insights into the binding patterns of the molecules to CB receptors.