Sigma Receptor Inhibitor

EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a K_i of 22 nM. EST64454 hydrochloride has the potential for the research of the pain.

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

Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects.

Sigmar1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sigmar1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [³H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC₅₀ of 3.15 μM. KB-5492 free base is an anti-ulcer agent.

KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [³H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC₅₀ of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent.

Sigmar1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sigmar1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. RC-106 has antiproliferative activity against cancer cells including glioblastoma (GB) and multiple myeloma (MM).

H3R antagonist 6 (Compounds 3) (H3-2406) is a Histamine receptor 3 (H3R) antagonist with an IC₅₀ of 5.6 nM. H3R antagonist 6 labeled with 18F has high radiochemical yield, molar activity and moderate brain uptake, but with an off-target binding to the Sigma-1 receptor. H3R antagonist 6 can be used as a PET radioligand for positron emission tomography imaging for central nervous system (CNS) disorders research.

CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC₅₀s of 311 and 14.1 nM, respectively.

4-AcO-DALT hydrochloride is a tryptamine compound with psychoactive effects. 4-AcO-DALT hydrochloride inhibits 5-HT receptors, alpha receptors, dopamine receptors, histamine receptor 1 (H1), muscarinic M2 receptor and Sigma 2 receptor. 4-AcO-DALT hydrochloride shows K_i values of 582 nM, 2689 nM, 2099 nM, 2116 nM, 958 nM, 137 nM, 824 nM, 479 nM, 406 nM, 874 nM, 4190 nM, 482 nM, 214 nM, 803 nM, 4522 nM, 1907 nM for 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7A, H1, Sigma 2, α2A, α2B, α2C, D2, D3 receptors.

SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC₅₀ of 20.3 nM and K_i of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC₅₀ of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs.

σ1R-IN-1 ((R,R)-1a) is a potent σ-1R inhibitor with an IC₅₀ of 110 nM. σ1R-IN-1 is promising for research of neuropsychiatric disorders.

BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC₅₀ = 101 nM) and serotonin transporter (SERT) (IC₅₀ = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC₅₀ of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC₅₀ = 7.7 μM), L-type calcium channel (IC₅₀ = 3.6 μM), σ receptor (IC₅₀ = 2 μM), and sodium channel (IC₅₀ = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease.

SIGMAR1 Human Pre-designed siRNA Set A contains three designed siRNAs for SIGMAR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

RTI-371 is a highly selective atypical dopamine transporter (DAT) inhibitor that crosses the blood-brain barrier. RTI-371 exhibits potent inhibitory activity in cell lines transfected with human DAT (IC₅₀ = 8.7 nM) and shows high binding affinity for rat DAT with a K_i value of 7.81 nM. RTI-371 also acts as a positive allosteric modulator of the human cannabinoid 1 receptor (hCB1 receptor), enhancing the activity of cannabinoid receptor agonists in a concentration-dependent manner. RTI-371 can be used for the research of Parkinson's disease.