sigma-2 receptor

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

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 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.

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).

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).

PB28 dihydrochloride is a selective and potent sigma 2 (σ2) receptor agonist and σ1 receptor antagonist with anti-SARS-CoV-2 activity and anti-tumor activity, which inhibits cell proliferation and invasion and suppresses SKF by modulating the PI3K-AKT-mTOR signaling pathway in renal cancer. It inhibits cell proliferation and invasion by regulating the PI3K-AKT-mTOR signaling pathway in renal cancer, inhibits calcium release from the endoplasmic reticulum of SK-N-SH neuroblastoma cells, and induces non-caspase-dependent apoptosis.

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

SW43 is a selective ligand of sigma-2 receptor.

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2 1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

PB28 is a cyclohexylpiperazine derivative that functions as a potent and highly selective agonist of the sigma 2 (σ2) receptor, exhibiting a Ki (binding affinity) of 0.68 nM. At the same time, PB28 acts as an antagonist of the sigma 1 (σ1) receptor, with a Ki of 0.38 nM. PB28 demonstrates a lower affinity for other receptors. It effectively inhibits electrically evoked twitch in both the guinea pig bladder (EC50 value of 2.62 μM) and ileum (EC50 value of 3.96 μM). Moreover, PB28 exhibits the ability to modulate protein-protein interaction between SARS-CoV-2 and human cells. Additionally, PB28 triggers caspase-independent apoptosis and possesses significant antitumor activity.

Blarcamesine hydrochloride (AVex-73 hydrochloride) is a Sigma-1 Receptor agonist (IC50: 860 nM).