sigma-1 receptor antagonist 1

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

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].

Sigma-1 receptor antagonist 6 (Compound 12), a σ1R antagonist, demonstrates significant antiallodynic effects by targeting the Sigma-1 receptor (σ1R). This compound is effective in animal models for neuropathic pain, particularly for reducing mechanical allodynia caused by paclitaxel.

Tiospirone (BMY 13859-1 free base) is a 5-HT2 receptor antagonist and dopamine blocker that inhibits D2, 5-HT1a, 5-HT7, and sigma receptors.Tiospirone is used in the study of neurological disorders such as schizophrenia.

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.

BD-1047 dihydrobromide (BD1047.2HBr) , a selective functional antagonist of sigma receptors, has antipsychotic activity in animal models predictive of efficacy in schizophrenia.

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).

S1RA hydrochloride (E-52862 hydrochloride) is an effective and specific sigma-1 receptor(σ1R, Ki: 17 nM) antagonist, and has good selectivity against σ2R (Ki > 1000 nM).

Volinanserin (MDL100907) (MDL 100907) is a potent and selective antagonist of the serotonin receptor 5-HT2 (Ki: 0.36 nM) and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 adrenergic and sigma receptors.

BD1063 dihydrochloride is a potent and selective sigma 1 (σ1) receptor antagonist (Ki = 9 nM).

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.

σ1 Receptor antagonist-1 is a selective σ1 receptor antagonist.

Dextromethorphan is a noncompetitive NMDA receptor antagonist and sigma-1 agonist that was approved by the FDA in 1958 for use as a cough suppressant.

IPAG is a potent σ-receptor antagonist (pKi=4.3). IPAG can induce cell apoptosis.

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.

BD 1008 Free Base is a selective sigma receptor antagonist, with a reported binding affinity of Kᵢ = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor.

CM304 is a highly selective sigma-1 receptor antagonist.

EST64454 hydrochloride (EST64454) is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for Pain Management.