s-1ra

S1RA (E-52862)(E-52862) is a potent, selective antagonist of the sigma-1 receptor (σ1R, Ki=17 nM), demonstrating significant selectivity over the sigma-2 receptor (σ2R, Ki > 1000 nM).

S1RA hydrochloride (E-52862 hydrochloride) is an effective and specific sigma-1 receptor(σ1R, Ki: 17 nM) antagonist, and has good selectivity against σ2R (Ki > 1000 nM).

S1R agonist 2 is a selective S1R agonist with a Ki of 88 nM for S2R and 1.1 nM for S1R and is protective against ROS and NMDA-induced neurotoxicity.

Compound 6b, also known as S1R agonist 1, is a selective agonist for S1R with dissociation constants (Ki) of 0.93 nM for S1R and 72 nM for S2R. This compound demonstrates neuroprotective effects against reactive oxygen species (ROS) and NMDA-induced neurotoxicity [1].

S1R Agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist, displaying K i values of 0.93 nM for S1R and 72 nM for S2R, and has demonstrated neuroprotective effects against ROS and NMDA-induced neurotoxicity [1].

Compound 8b hydrochloride, a selective S1R agonist, exhibits affinity with K i s of 1.1 nM for S1R and 88 nM for S2R. It demonstrates neuroprotective effects against ROS and NMDA-induced neurotoxicity [1].

Compound 10, an hNTS1R agonist-1, acts as a full agonist with a strong affinity for hNTS1R (K i: 6.9 nM), showing the ability to cross the blood-brain barrier (BBB). It not only enhances motor function but also improves memory in a mouse model of Parkinson's disease (PD). Additionally, this compound is an analog of Neurotensin(8-13) and demonstrates neuroprotective properties [1].