sigma 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).

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

Sigma-1 receptor antagonist 1 is an effective and selective antagonist of sigma-1 receptor. Sigma-1 receptor antagonist 1 exhibits antineuropathic pain activity and can be used in the treatment of neuropathic pain studies.

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

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.

Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances morphine's analgesic effects and reverses morphine-induced analgesic tolerance, potentially preventing morphine tolerance [1].

Sigma-1 receptor antagonist 5 (compound 12), a 4-pyridylpiperidine derivative, exhibits analgesic properties through its antagonistic action on sigma receptors (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and the histamine H3 receptor (hH3R, Ki=7.7 nM, IC50=215 nM). It effectively attenuates Capsaicin-induced nociception and demonstrates significant antinociceptive effects in both nociceptive and neuropathic pain models [1].

E1R is a positive sigma-1 receptor (Sig1R PAM) allosteric modulator. It has a cognition-enhancing activity.

(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator for treating cognition and memory disorders.

(2S,3S)-E1R (Compound 2d) is an enantiomer of (2R,3R)-E1R, a sigma-1 receptor positive allosteric modulator for the treatment of cognition/memory disorders.

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.

AF-710B is a specific variant of M1 muscarinic and Sigma-1 receptor agonist used in the study of neurological disorders such as Alzheimer's disease dementia and schizophrenia.

SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.SKF83959 is a potent variant modulator of the sigma (σ)-1 receptor, which ameliorates cognitive dysfunction for the study depression and Alzheimer's disease.

Opipramol (Ensidon) is a compound with antidepressant activity that attenuates cocaine-seeking behavior in a rat model of self-administration.Opipramol is a sigma (σ) receptor agonist with anxiolytic activity and may be used in the study of neurological disorders.

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).

S1R agonist 2 is a selective S1R agonist with a Ki of 88 nM for S2R and 1.1 nM for S1R and is protective against ROS and NMDA-induced neurotoxicity.

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.

L-693,403 maleate has analgesic activity.

OPC-14523, a 5-HT1A receptor agonist, is used potentially for the treatment of depression and neuropathic pain.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Ditolylguanidine (Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).