bitopertin

Ligand id: 7546

Name: bitopertin

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 0
Rotatable bonds 8
Topological polar surface area 88.19
Molecular weight 543.11
XLogP 4.7
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Bitopertin is being investigated as an anti-schzophrenia drug [1,3]. Treatment with bitopertin Improves negative symptoms of schizophrenia, especially social and emotional withdrawal, in patients with persistent, predominant negative symptoms, when used adjunctively with antipsychotic therapy. ClinicalTrials.gov hosts a list of registered trials assessing this potential drug.
Mechanism Of Action and Pharmacodynamic Effects
Bitopertin is a glycine transporter type 1 (GlyT1, SLC6A9) inhibitor [2]. Inhibition of this transporter increases levels of the excitatory neurotransmitter, glycine, by inhibiting its reuptake from the synaptic cleft. Glycine, alongside glutamate, is required as a co-agonist at N-methyl-D-aspartate (NMDA) receptors. Dysfunction of NMDA receptors is believed to play a role in the pathogenesis of schizophrenia. Bitopertin-induced activation of NMDA receptors improves the symptoms of schizophrenia.