Ligand id: 9309

Name: basimglurant

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 3
Hydrogen bond donors 0
Rotatable bonds 1
Topological polar surface area 30.71
Molecular weight 325.08
XLogP 5.55
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Basimglurant (RO4917523) has completed Phase 2 clinical trials for major depressive disorder and fragile X syndrome (see NCT01437657 and NCT01015430 as examples)
Mechanism Of Action and Pharmacodynamic Effects
Fragile X syndrome (FXS): Increased mGlu5 receptor activity is believed to underlie disease-related phenotypes in FXS, with symptoms improved by pharmacological or genetic inhibition of mGlu5 receptor activity. mGlu5 NAMs such as basimglurant are being evaluated for their clinical efficacy in improving FXS pathophysiology.
Depression:Evidence suggests that the pathophysiology of depression can be the result of glutamatergic system dysfunction, with predictions that pharmacological modulation of glutamatergic neurotransmission may deliver antidepressant effects. Initial preclinical studies focussed on mGlu5 antagonists (e.g. MPEP and MTEP), and has more recently shifted towards investigating mGlu5 NAMs.