ReviewBiochemical pharmacology2017
Functional selectivity at G-protein coupled receptors: Advancing cannabinoid receptors as drug targets.
Review in Biochemical pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
34 citing papers in PubMed, 1 synthesis or guideline pooled it, 83 citations in OpenAlex.
- Cannabinoid Receptors: An Update on Cell Signaling, Pathophysiological Roles and Therapeutic Opportunities in Neurological, Cardiovascular, and Inflammatory Diseases.International journal of molecular sciences · 2020Pooled it
- Mechanistic insights into ligand selectivity inActa pharmaceutica Sinica. B · 2026Article
- Biased Allosteric Modulation in GPCR Drug Discovery.Handbook of experimental pharmacology · 2026Review
- Advances in cannabinoid receptors pharmacology: from receptor structural insights to ligand discovery.Acta pharmacologica Sinica · 2025Review
- Circular RNAs: novel noncoding players in male infertility.Hereditas · 2024Review
- Activation of cannabinoid receptor 2 by turmeric oleoresin reduces inflammation and oxidative stress in an osteoarthritisFrontiers in pharmacology · 2024Article
- The Interplay between Cannabinoid Receptors and Microglia in the Pathophysiology of Alzheimer's Disease.Journal of clinical medicine · 2023Review
- Opposite physiological and pathological mTORC1-mediated roles of the CB1 receptor in regulating renal tubular function.Nature communications · 2022Article
- New paradigms for the treatment of lysosomal storage diseases: targeting the endocannabinoid system as a therapeutic strategy.Orphanet journal of rare diseases · 2021Review
- THC Reduces Ki67-Immunoreactive Cells Derived from Human Primary Glioblastoma in a GPR55-Dependent Manner.Cancers · 2021Article
- Quality of Life and a Surveillant Endocannabinoid System.Frontiers in neuroscience · 2021Review
- Pharmacological Insights Into Safety and Efficacy Determinants for the Development of Adenosine Receptor Biased Agonists in the Treatment of Heart Failure.Frontiers in pharmacology · 2021Article
- Neural Stem Cells and Cannabinoids in the Spotlight as Potential Therapy for Epilepsy.International journal of molecular sciences · 2020Review
- Functionalized Cannabinoid Subtype 2 Receptor Ligands: Fluorescent, PET, Photochromic and Covalent Molecular Probes.ChemMedChem · 2020Review
- Assessment of Biased Agonism among Distinct Synthetic Cannabinoid Receptor Agonist Scaffolds.ACS pharmacology & translational science · 2020Article
- Differential activation of G protein-mediated signaling by synthetic cannabinoid receptor agonists.Pharmacology research & perspectives · 2020Article
- Endocannabinoid Modulation of Microglial Phenotypes in Neuropathology.Frontiers in neurology · 2020Review
- Cannabichromene is a cannabinoid CBBritish journal of pharmacology · 2019Article
- Allosteric Modulation of Cannabinoid Receptor 1-Current Challenges and Future Opportunities.International journal of molecular sciences · 2019Review
- Cannabinoid Signaling in the Skin: Therapeutic Potential of the "C(ut)annabinoid" System.Molecules (Basel, Switzerland) · 2019Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The phenomenon of functional selectivity, whereby a ligand preferentially directs the information output of a G-protein coupled receptor (GPCR) along (a) particular effector pathway(s) and away from others, has redefined traditional GPCR signaling paradigms to provide a new approach to structure-based drug design. The two principal cannabinoid receptors (CBRs) 1 and 2 belong to the class-A GPCR subfamily and are considered tenable therapeutic targets for several indications. Yet conventional orthosteric ligands (agonists, antagonists/inverse agonists) for these receptors have had very limited clinical utility due to their propensity to incite on-target adverse events. Chemically distinct classes of cannabinergic ligands exhibit signaling bias at CBRs towards individual subsets of signal transduction pathways. In this review, we discuss the known signaling pathways regulated by CBRs and examine the current evidence for functional selectivity at CBRs in response to endogenous and exogenous cannabinergic ligands as biased agonists. We further discuss the receptor and ligand structural features allowing for selective activation of CBR-dependent functional responses. The design and development of biased ligands may offer a pathway to therapeutic success for novel CBR-targeted drugs.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.