Publications by authors named "R G Pertwee"
Article Synopsis
- The Concise Guide to PHARMACOLOGY 2023/24 offers a summarized overview of approximately 1800 drug targets and around 6000 interactions with 3900 ligands, mostly in a tabular format.
- It focuses on selective pharmacology and includes links to an open access knowledgebase for more detailed drug information.
- The guide divides drug targets into six major categories, providing essential summaries and guidance based on the latest pharmacological data available as of mid-2023, while serving as an official resource by the International Union of Basic and Clinical Pharmacology.
3-3'-Diindolylmethane (DIM) is a biologically active dimer derived from the endogenous conversion of indole-3-carbinol (I3C), a naturally occurring glucosinolate found in many cruciferous vegetables (i.e., ).
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- - This study explores how M receptors interact with CB receptors in SH-SY5Y cells, finding that M receptor activation boosts CNR1 gene expression, which enhances the CB receptor's response to agonists.
- - Calcium homeostasis is crucial for this interaction, as M receptor activation increases calcium release, which in turn raises CB receptor levels through both gene expression and protein synthesis.
- - The presence of both M and CB receptors in certain brain regions suggests that their interaction may influence how the brain adapts to cannabinoids, presenting potential for new drug development targeting addiction and tolerance.
Article Synopsis
- Positive allosteric modulation of the type 1 cannabinoid receptor (CB1R) shows promise for treating neurological and immune disorders.
- The study focused on separating enantiomers of two potent CB1R ago-PAMs, GAT591 and GAT593, to assess their biochemical activity at CB1R.
- Distinct binding behaviors and activities were observed between the enantiomers, indicating that they may operate through different mechanisms, which highlights their potential in treating conditions like pain, epilepsy, glaucoma, and Huntington's disease.
It is well known that G protein-coupled receptors (GPCRs) assume multiple active states. Orthosteric ligands and/or allosteric modulators can preferentially stabilize specific conformations, giving rise to pathway-biased signaling. One of the most promising strategies to expand the repertoire of signaling-selective GPCR activators consists of dualsteric agents, which are hybrid compounds consisting of orthosteric and allosteric pharmacophoric units.
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