AI Article Synopsis
- Metabotropic glutamate receptor 5 (mGlu5) negative allosteric modulators (NAMs) are linked to various conditions like migraines, Parkinson's disease, and anxiety, showing promise in preclinical and some clinical studies.
- Recordati Ireland Ltd has developed novel mGlu5 NAM derivatives for treating lower urinary tract disorders, which had previously been explored for their therapeutic potential.
- In animal tests, these new compounds demonstrated effectiveness in improving bladder function, indicating their potential use in treating lower urinary tract disorders.
Article Abstract
Metabotropic glutamate receptor 5 (mGlu5) negative allosteric modulators (NAMs) have previously been implicated in a number of pathophysiological conditions, based on preclinical, and to some extent clinical, proof of concept for migraine, gastroesophageal reflux disease, Parkinson's disease and anxiety. In the past, the potential use of known mGlu5 antagonists for the treatment of lower urinary tract disorders was disclosed. In the patent evaluated herein, novel derivatives of 4-(prop-2-ynylidene)piperidine are described and claimed by Recordati Ireland Ltd, Ireland, as NAMs at mGlu5 for the treatment of lower urinary tract disorders. Selected compounds reported in this application were efficacious in the cystometry model of bladder dysfunction in conscious rats, and mGlu5 NAMs are, therefore, suggested to have potential for the treatment of lower urinary tract disorders.
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| http://dx.doi.org/10.1517/13543770903547848 | DOI Listing |
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