Novel approaches and current challenges with targeting the endocannabinoid system

P Morales, N Jagerovic - Expert opinion on drug discovery, 2020‏ - Taylor & Francis
Introduction The pathophysiological relevance of the endocannabinoid system has been
widely demonstrated in a variety of diseases including cancer, neurological disorders, and …

Δ9-cis-Tetrahydrocannabinol: Natural Occurrence, Chirality, and Pharmacology

MA Schafroth, G Mazzoccanti… - Journal of natural …, 2021‏ - ACS Publications
The cis-stereoisomers of Δ9-THC [(−)-3 and (+)-3] were identified and quantified in a series
of low-THC-containing varieties of Cannabis sativa registered in Europe as fiber hemp and …

Design, synthesis, and biological activity of new CB2 receptor ligands: From orthosteric and allosteric modulators to dualsteric/bitopic ligands

F Gado, R Ferrisi, B Polini, KA Mohamed… - Journal of Medicinal …, 2022‏ - ACS Publications
The design of dualsteric/bitopic agents as single chemical entities able to simultaneously
interact with both the orthosteric and an allosteric binding site represents a novel approach …

Development of N-(1-Adamantyl)benzamides as Novel Anti-Inflammatory Multitarget Agents Acting as Dual Modulators of the Cannabinoid CB2 Receptor and Fatty …

F Intranuovo, L Brunetti, P DelRe… - Journal of Medicinal …, 2022‏ - ACS Publications
Cannabinoid type 2 receptor (CB2R), belonging to the endocannabinoid system, is
overexpressed in pathologies characterized by inflammation, and its activation counteracts …

Advances in the discovery of fatty acid amide hydrolase inhibitors: what does the future hold?

D Fazio, E Criscuolo, A Piccoli, B Barboni… - Expert Opinion on …, 2020‏ - Taylor & Francis
Introduction Fatty acid amide hydrolase (FAAH) is a membrane-bound enzyme, that
inactivates endogenous signaling lipids of the fatty acid amide family, including the …

The cannabinoid CB2 receptor positive allosteric modulator EC21a exhibits complicated pharmacology in vitro

A Qi, X Han, M Quitalig, J Wu, PP Christov… - Journal of Receptors …, 2024‏ - Taylor & Francis
Schizophrenia is a complex disease involving the dysregulation of numerous brain circuits
and patients exhibit positive symptoms (hallucinations, delusions), negative symptoms …

Novel Orthosteric/Allosteric Ligands of Cannabinoid Receptors: An Unexpected Pharmacological Profile

R Ferrisi, B Polini, AM Smolyakova… - Journal of Medicinal …, 2025‏ - ACS Publications
The design of dualsteric/bitopic receptor ligands as compounds capable of simultaneously
interacting with both the orthosteric and an allosteric binding site has gained importance to …

The endocannabinoid system dual-target ligand N-cycloheptyl-1, 2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease …

C Arena, F Gado, LDC Mannelli, C Cervetto… - European journal of …, 2020‏ - Elsevier
Multiple sclerosis is a chronic inflammatory demyelinating disorder of the central nervous
system that eventually leads to progressive neurodegeneration and disability. Recent …

Design, synthesis, and evaluation of anticonvulsant activities of new triazolopyrimidine derivatives

M Song, W Zhao, Y Zhu, W Liu, X Deng… - Frontiers in …, 2022‏ - frontiersin.org
Epilepsy, a severe brain disease affecting a large population, is treated mainly by
antiepileptic drugs (AEDs). However, toxicity, intolerance, and low efficiency of the available …

Interplay Between Endocannabinoid System and Neurodegeneration: Focus on Polypharmacology

F Seghetti, S Gobbi, F Belluti… - Current Medicinal …, 2022‏ - ingentaconnect.com
Pharmacological treatment of complex pathologies, such as neurodegenerative diseases
still represents a major challenge, due to the networked pathways involved in their onset …