- |||||||||| basmisanil (RG1662) / Roche, darigabat (CVL-865) / AbbVie
Journal: New Insights Into Pharmacology of GABAA Receptor Alpha Subunits-Selective Modulators. (Pubmed Central) - Jan 10, 2025 Future drug discovery efforts are encouraged to focus on positive allosteric modulators that selectively target the ?2, ?3 subunits and negative/positive allosteric modulators that target the ?5 subunit of the GABAA receptor. The pursuit of ligands possessing only anxiolytic effects or those enhancing cognition continues to be an important focus for future research, with promising advancements depicted in recent studies.
- |||||||||| basmisanil (RG1662) / Roche
Preclinical, Journal: Basmisanil, an ?5-GABAAR negative allosteric modulator, produces rapid and sustained antidepressant-like responses in male mice. (Pubmed Central) - Jun 2, 2024 Bioanalysis of plasma and brain samples confirms effective blood-brain barrier penetration by Basmisanil and extrapolation to previously published data suggest that effects were observed at doses (10 and 30?mg/kg i.p.) corresponding to relatively modest levels of ?5-GABAAR occupancy (40-65?%). These results suggest that Basmisanil exhibits a combination of rapid and sustained antidepressant-like effects highlighting the potential of ?5-NAMs as a novel therapeutic strategy for depression.
- |||||||||| basmisanil (RG1662) / Roche
The GABAA α5 Receptor as a Therapeutic Target for Dup15q Syndrome ([VIRTUAL]) - Nov 28, 2021 - Abstract #ACNP2021ACNP_1242; The converging evidence reported here strongly suggests that excess GABAA receptor function contributes to the pathophysiology of Dup15q syndrome and points to the GABAA α5 receptor subtype as a novel and tractable target for the treatment of Dup15q syndrome. Roche is planning a randomized-controlled phase 2 trial in children with Dup15q syndrome to evaluate the effects of a GABAA α5 NAM (basmisanil) on core symptoms of Dup15q syndrome.
- |||||||||| basmisanil (RG1662) / Roche
Clinical, Journal: A de novo variant of CHD8 in a patient with autism spectrum disorder. (Pubmed Central) - Apr 21, 2020 Whole exome sequencing for parent-child trio revealed a de novo heterozygous loss-of-function mutation (c.4984C>T, p.Arg1662Ter) in CHD8 gene. Our findings elaborate the genotype-phenotype correlation and confirm that the CHD8 disruptions represent a clinical ASD subtype and further highlight the significance of implementing genomic medicine in clinical practice for an early intervention and necessary support for the families.
- |||||||||| basmisanil (RG1662) / Roche
Journal: HIV gp120 upregulates tonic inhibition through α5-containing GABARs. (Pubmed Central) - Jan 29, 2020 The increased current resulted from upregulation of extrasynaptic α5-containing GABARs, as indicated by inhibition with the selective inverse agonist basmisanil...Increased tonic inhibition impairs neuroplasticity and inhibition of α5-containing GABARs improves cognitive function in disease models. Thus, gp120-induced upregulation of α5-containing GABARs presents a novel therapeutic target for HAND.
|