sigma-2

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

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).

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-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).

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.

KSK68 is a potent dual sigma-1 and histamine H3 receptor antagonist with potential analgesic activity and high affinity for H3 receptors, sigma-1, sigma-2 receptors.KSK68 can be used in the study of pain related diseases.

KSK94 is a specific H3 receptor antagonist that inhibits H3, sigma-1, and sigma-2 receptors , with Ki values of 7.9, 2958, and 75.2 nM, respectively, and can be used to study injurious pain and neuropathic pain.

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

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).

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

Ifenprodil (RC61-91) is an inhibitor of the NMDA receptor, specifically of GluN1 (glycine-binding NMDA receptor subunit 1) and GluN2B (glutamate-binding NMDA receptor subunit 2) subunits. Additionally, Ifenprodil inhibits GIRK channels and interacts with alpha1 adrenergic, serotonin, and sigma receptors.

BD 1008 dihydrobromide is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM). BD 1008 dihydrobromide have high affinity for sigma1 receptors, moderate affinity for sigma2 receptors.

3-(2-phenylethynyl)pyridine is a pyridine derivative that is a ligand for a variety of receptors in the human body, including dopamine D2 receptors, sigma-1 receptors, and 5-HT6 receptors. It has been studied for the treatment of various neurological disorders, including schizophrenia, depression and Alzheimer's disease.

KSK67 is a selective dual antagonist of sigma-2 and histamine H3 receptors with inhibitory effects on H3 receptors, sigma-1, and sigma-2 receptors, with Ki values of 3.2, 1531, and 101 nM, respectively.KSK67 can be used to study injury pain and neuropathic pain.

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.

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.

Glycerol phenylbutyrate-D15 is a deuterium-labeled Glycerol phenylbutyrate. Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand (pKi: 8.02).

Glycerol phenylbutyrate-D5 is a deuterium-labeled Glycerol phenylbutyrate. Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand (pKi: 8.02).

CB-184 is a selective ligand for sigma-2 (σ2) receptors, with Ki values of 7436 nM for sigma-1 (σ1) and 13.4 nM for sigma-2 (σ2), and it promotes apoptosis with antitumor activity.

4-Hydroxy-1-(2-phenylethyl)piperidine is a synthetic ligand for muscarinic acetylcholine receptors (mAChR) or non-opioid intracellular sigma-1 receptors (σ1 receptors). It serves as a metabolite of the opioid compounds furanylfentanyl and 4-fluoroisobutyryl fentanyl (FIBF).