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).

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.

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.

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

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

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].