Dec 5, 2019

Novel Analgesic Agents Obtained by Molecular Hybridization of Orthosteric and Allosteric Ligands

BioRxiv : the Preprint Server for Biology
Carlo MateraSimona Bertoni


Despite the high incidence of acute and chronic pain in the general population, the efficacy of currently available medications is unsatisfactory. Insufficient management of pain has a profound impact on the quality of life and can have serious physical, psychological, social, and economic consequences. This unmet need reflects a failure to develop novel classes of analgesic drugs with superior clinical properties and lower risk of abuse. Nevertheless, recent advances in our understanding of the neurobiology of pain are offering new opportunities for developing different therapeutic approaches. Among those, the activation of M2 muscarinic acetylcholine receptors, which play a key role in the cholinergic regulation of the nociceptive transmission, constitutes one of the most promising strategies. We have recently developed a small library of novel pharmacological agents by merging the structures of known orthosteric and allosteric muscarinic ligands through their molecular hybridization, an emerging approach in medicinal chemistry based on the combination of pharmacophoric moieties of different bioactive substances to produce a new compound with improved pharmacological properties. Herein we report the functional characterizatio...Continue Reading

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Mentioned in this Paper

Cholinergic Effect
Nucleic Acid Hybridization Procedure
Pharmacologic Substance
Pharmaceutical Preparations
Disease Management

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