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Full-Text Articles in Medicine and Health Sciences
Identification Of An Orally Bioavailable, Brain-Penetrant Compound With Selectivity For The Cannabinoid Type 2 Receptor, Meirambek Ospanov, Suresh P. Sulochana, Jason J. Paris, John M. Rimoldi
Identification Of An Orally Bioavailable, Brain-Penetrant Compound With Selectivity For The Cannabinoid Type 2 Receptor, Meirambek Ospanov, Suresh P. Sulochana, Jason J. Paris, John M. Rimoldi
Faculty and Student Publications
Modulation of the endocannabinoid system (ECS) is of great interest for its therapeutic relevance in several pathophysiological processes. The CB2 subtype is largely localized to immune effectors, including microglia within the central nervous system, where it promotes anti-inflammation. Recently, a rational drug design toward precise modulation of the CB2 active site revealed the novelty of Pyrrolo[2,1-c][1,4]benzodiazepines tricyclic chemotype with a high conformational similarity in comparison to the existing leads. These compounds are structurally unique, confirming their chemo-type novelty. In our continuing search for new chemotypes as selective CB2 regulatory molecules, following SAR approaches, a total of 17 selected (S,E)-11-[2-(arylmethylene)hydrazono]-PBD analogs …
1,2,3-Triazole Derivatives As Highly Selective Cannabinoid Receptor Type 2 (Cb2) Agonists, Amer H. Tarawneh, Pankaj Pandey, Lo'ay A. Al-Momani, Anastassiya V. Gadetskaya
1,2,3-Triazole Derivatives As Highly Selective Cannabinoid Receptor Type 2 (Cb2) Agonists, Amer H. Tarawneh, Pankaj Pandey, Lo'ay A. Al-Momani, Anastassiya V. Gadetskaya
Faculty and Student Publications
The cannabinoid receptor 2 (CB2 receptor) has attracted considerable interest, mainly due to its potential as a target for therapeutics for treating various diseases that have a neuroinflammatory or neurodegenerative component while avoiding the adverse psychotropic effects that accompany CB1 receptor-based therapies. With the appreciation that CB2-selective ligands show marked functional selectivity, there is a renewed opportunity to explore this promising area of research from both a mechanistic as well as a therapeutic perspective. In this research, we are interested in the discovery of new chemotypes as highly selective CB2 modulators, which may serve as good starting points for further …