NS-11821
| Clinical data | |
|---|---|
| Other names | NS11821 |
| Routes of administration | Oral[1][2] |
| Drug class | GABAA receptor positive allosteric modulator; Nonbenzodiazepine; Anxiolytic |
| ATC code |
|
| Pharmacokinetic data | |
| Onset of action | 0.5–4.0 hours (Tmax)[2] |
| Elimination half-life | 0.62–5.0 hours[2] |
NS-11821, or NS11821 is a GABAA receptor positive allosteric modulator and nonbenzodiazepine which was under development for the treatment of anxiety disorders and CNS disorders but was never marketed.[1][3][2] It is taken orally.[1][2]
The drug is a subunit-selective partial positive allosteric modulator of the GABAA receptor.[2] More specifically, it shows affinity (Ki) values of 1.6 nM at α1, 9.7 nM at α2, 3.8 nM at α3, and 2.5 nM at α5, whereas it shows EC50 (Emax) values of ND (4%) at α1, 59 nM (17%) at α2, 73 nM (40%) at α3, and 44 nM (41%) at α5.[2] Based on animal studies, this is expected to translate into a profile of anxiolytic effects with low propensity for sedation.[2] Clinical findings of NS-11821 in humans have been described.[2]
NS-11821 was under development by NeuroSearch.[1][3] It reached phase 1 clinical trials for both anxiety disorders and CNS disorders prior to the discontinuation of its development in 2017.[1][3] The chemical structure of NS-11821 does not yet appear to have been disclosed.[1]
See also
[edit]References
[edit]- 1 2 3 4 5 6 "NS 11821". AdisInsight. 10 March 2017. Retrieved 5 June 2026.
- 1 2 3 4 5 6 7 8 9 Zuiker RG, Chen X, Østerberg O, Mirza NR, Muglia P, de Kam M, et al. (March 2016). "NS11821, a partial subtype-selective GABAA agonist, elicits selective effects on the central nervous system in randomized controlled trial with healthy subjects". Journal of Psychopharmacology. 30 (3). Oxford, England: 253–262. doi:10.1177/0269881115620435. PMID 26655084.
- 1 2 3 "Delving into the Latest Updates on NS-11821 with Synapse". Synapse. 8 May 2025. Retrieved 5 June 2026.
