Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro,Bioorganic & Medicinal Chemistry Letters

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Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2022-08-06 , DOI: 10.1016/j.bmcl.2022.128923
Carson W Reed ₁ , Alice L Rodriguez ₁ , Jacob J Kalbfleisch ₁ , Mabel Seto ₁ , Matthew T Jenkins ₁ , Anna L Blobaum ₁ , Sichen Chang ₁ , Craig W Lindsley ₂ , Colleen M Niswender ₃

Affiliation

We describe here a series of metabotropic glutamate receptor 7 (mGlu₇) negative allosteric modulators (NAMs) with a saturable range of activity in inhibiting responses to an orthosteric agonist in two distinct in vitro pharmacological assays. The range of inhibition among compounds in this scaffold provides highly structurally related ligands with differential degrees of receptor blockade that can be used to understand inhibitory efficacy profiles in native tissue or in vivo.

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