AI Article Synopsis
- * These modified probes incorporate various functional groups (like isothiocyanato, azido, and cyano) that can be used individually or combined, targeting different sites within the CBR-binding domains.
- * One notable probe, AM11245, is highlighted for its extraordinary potency and binding affinity, earning it the title of "megagonist," and it functions both centrally and peripherally, unlike a previously researched "megagonist," AM841, which operates only in peripheral locations.
Article Abstract
We report the development of novel cannabinergic probes that can stabilize the cannabinoid receptors (CBRs) through tight binding interactions. Ligand design involves the introduction of select groups at a judiciously chosen position within the classical hexahydrocannabinol template (monofunctionalized probes). Such groups include the electrophilic isothiocyanato, the photoactivatable azido, and the polar cyano moieties. These groups can also be combined to produce bifunctionalized probes potentially capable of interacting at two distinct sites within the CBR-binding domains. These novel compounds display remarkably high binding affinities for CBRs and are exceptionally potent agonists. A key ligand (, AM11245) exhibits exceptionally high potency in both and assays and was designated as "megagonist," a property attributed to its tight binding profile. By acting both centrally and peripherally, distinguishes itself from our previously reported "megagonist" AM841, whose functions are restricted to the periphery.
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| http://dx.doi.org/10.1021/acs.jmedchem.0c02053 | DOI Listing |
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