sigma-2

Sigma-2 receptor antagonist 1 is an antagonist of the sigma-2 (σ-2) receptor.

Sigma-2 Receptor ligand 1 (Compound 7i) is a highly selective ligand for the Sigma-2 receptor, with a Ki of 40 nM. It shows potential for Alzheimer's disease research.

Sigma-2 Radioligand 1 (compound 1) serves as a selective Sigma-2 ligand, demonstrating favorable biodistribution in mice and robust in vivo activity in rats. The [18F] modified version of Sigma-2 Radioligand 1 enhances the visualization of tumors in micro-PET/CT imaging by providing high tumor uptake and an impressive tumor-to-background ratio. Additionally, experiments confirm that this compound binds with high specificity to U87MG glioma xenografts [1].

Sigma-2 Radioligand 2 (compound 4) exhibits low nanomolar affinity for the σ2 receptor (Ki=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500).

Roluperidone (CYR-101), a novel cyclic amide derivative, exhibits high equipotent affinities for 5-HT2A and σ2 receptors with Ki values of 7.53 nM and 8.19 nM, respectively.

AB21 HCl is a selective antagonist of the σ1 receptor, with Kis of 13 nM for σ1 receptor and 102 nM for σ2 receptor. AB21 HCl is known for its ability to reduce mechanical hypersensitivity.

Sigma-1 receptor antagonist 2 is a more potent and selective antagonist of the sigma-1 receptor (σ1 R, Ki = 3.88 nM) compared to the sigma-2 receptor (Ki = 1288 nM).

Ditolylguanidine (Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).

Glycerol phenylbutyrate (HPN-100) (GPB) is a new generation ammonia scavenger drug and it also is a sigma-2 (σ2) receptor ligand (pKi: 8.02).

Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of Y cells and to exhibit a potent anticancer activity in vivo.

Siramesine (Lu 28-179)(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.lysosome-destabilizing agent siramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost

PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.

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).

4-IBP is a selective σ1 agonist with high affinity for the σ1 receptor (Ki = 1.7 nM) and moderate affinity for the σ2 receptor (Ki = 25.2 nM).

KSK94 FA is a potent histamine H3 receptor antagonist that inhibits H3 receptors and is used in the study of neuropathic pain and obesity.

AB10 is a selective Sigma-1 receptor (S1R) antagonist. It exhibits a Ki of 10 nM for S1R and 165 nM for S2R. AB10 has the ability to reverse the pain effects induced by Capsaicin in models.

KSCM-1 is a selective sigma-1 receptor ligand.

CB-64D is a sigma2R selective agonist which releases calcium in human neuroblastoma cells and produces cell death in tumor cell lines.

CM764 is a potent and selective antagonist of sigma-2 receptors, a novel derivative of SN79.

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].

KB-5492 free base is an orally available and selective antiulcer agent that inhibits sigma receptors, inhibits [3H]1,3-di(2-tolyl)guanidine (DTG) binding to sigma receptors, and may be useful in the study of gastric lesions and gastric secretion.

KB-5492 FA is a selective sigma receptor inhibitor with antiulcerogenic effects.128-52-56-8

OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist with antidepressant-like activity, showing high affinity for the sigma receptor σ1/2 (IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM).

Pridopidine (FR310826), a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist, improves motor performance and shows neuroprotective effects in Huntington disease R6/2 mouse model.