sigma ligand 1

Sigma-LIGAND-1 is a selective Sigma Receptor ligand with IC50 values of 16 nM and 19 nM at the DTG site and the PPP site, respectively, and a Ki of 4000 nM at the dopamine D2 receptor.

Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with activity at DTG (IC50: 16 nM) and PPP (IC50: 19 nM) sites, and can also act on the dopamine D2 receptor (Ki: 4000 nM).

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.

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.

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.

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).

AD353 is a selective sigma-1 receptor ligand. It demonstrates high efficacy in models of capsaicin-induced allodynia and PGE2-induced mechanical hyperalgesia. Additionally, AD353 exhibits favorable pharmacokinetic properties.

S2/IAPinh is a conjugate composed of an inhibitor of apoptosis proteins inhibitor (IAPinh) and a ligand of sigma 2 SW43. It demonstrates anti-proliferative and apoptosis-inducing activity by degrading inhibitor of apoptosis proteins (clAP-1).

S1R agonist 3 is a potent and selective sigma-1 receptor (S1R) agonist with a Ki of 1.5 nM. It reduces hyperactive behavior in wfs1abKO zebrafish larvae without affecting the motor skills of wild-type wfs1abWT larvae. Additionally, S1R agonist 3 can reverse learning and memory impairment induced by Aβ25-35. S1R ligand 1 is applicable for Alzheimer's disease research.

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

RLH 033 is a selective ligand for the sigma 1 recognition site.

PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand with a Ki value of 0.08 nM for σ1 and 1377 nM for σ2, exhibiting negligible affinity for other receptors, ion channels, and enzymes, and demonstrating potential antipsychotic activity.

CM398 is an orally active chemical compound that acts as a highly selective ligand for the sigma-2 receptor (K i =0.43 nM), demonstrating a significant ratio of selectivity between sigma-1 and sigma-2 receptors (1000-fold). Moreover, CM398 exhibits notable affinity towards dopamine (K i =32.90 nM) and serotonin transporters (K i =244.2 nM). In addition, CM398 has shown promising efficacy as an anti-inflammatory analgesic in a mouse model of inflammatory pain induced by formalin [1].

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].