Sigma Receptor Antagonist

Sigma Receptor Antagonists (22):

Cat. No.	Product Name	Effect	Purity

HY-101484A

NE-100 hydrochloride	Antagonist	≥98.0%
NE-100 (hydrochloride) is a potent and selective sigma-1 receptor antagonist with an IC₅₀ of 4.16 nM. NE-100 (hydrochloride) exerts antipsychotic activity in vivo[1]. NE-100 (hydrochloride) also suppresses ER stress-induced hippocampal cell death[2].

HY-108510

Rimcazole dihydrochloride	Antagonist	99.96%
Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can reduce locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer.

HY-100985

IPAG	Antagonist	99.84%
IPAG is a potent sigma-1 receptor antagonist with a pK_i of 4.3. IPAG induces apoptosis.

HY-118901

Opipramol	Antagonist	99.91%
Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a K_i value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).

HY-136281

DuP 734	Antagonist	98.82%
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.

HY-134189A

EST73502 monohydrochloride	Antagonist	99.58%
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K_is of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity.

HY-124462

Trifluperidol hydrochloride	Antagonist	99.4%
Trifluperidol hydrochloride is a Sigma-1 receptor antagonist with a K_i value of 3.3 nM. Trifluperidol hydrochloride is used in the study of psychosis.

HY-155616

KSK94	Antagonist
KSK94 is a high-affinity histamine H3 receptor antagonist, with K_is of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain.

HY-147560

σ1 Receptor/μ Opioid receptor modulator 1	Antagonist
σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with K_is of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain.

HY-155614

KSK68	Antagonist
KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with K_is of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain.

HY-149335

Sigma-1 receptor antagonist 5	Antagonist
Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist of sigma receptor (Ki=4.5 nM (σ1R)，10 nM (σ2R)) and histamine H3 (hH₃R，Ki=7.7 nM，IC₅₀=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models.

HY-155615

KSK67	Antagonist
KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with K_is of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain.

HY-163065

σ1 Receptor/μ Opioid receptor modulator 2	Antagonist
σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC₅₀: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (K_i: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models.

HY-162759

Sigma-1 receptor antagonist 6	Antagonist
Sigma-1 receptor antagonist 6 (Compound 12) is an antagonist of the Sigma-1 receptor (σ1R). Sigma-1 receptor antagonist 6 exerts a robust antiallodynic effect by antagonizing σ1R. Sigma-1 receptor antagonist 6 can be used in neuropathic pain animal models to alleviate mechanical allodynia induced by paclitaxel (HY-B0015).

HY-149274

Sigma-1 receptor antagonist 4	Antagonist
Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance.

HY-161873

PW507	Antagonist
PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a K_i of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN).

HY-149854A

AB21 oxalate	Antagonist
AB21 oxalate is a potent and selective S1R antagonist with K_is of 13, 102 nM for S1R and S2R. AB21 oxalate has the effect of reducing mechanical hypersensitivity.

HY-134189

EST73502	Antagonist
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K_is of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.

HY-13575R

Blonanserin (Standard)	Antagonist
Blonanserin (Standard) is the analytical standard of Blonanserin. This product is intended for research and analytical applications. Blonanserin (AD-5423) is a potent and orally active 5-HT_2A (K_i=0.812 nM) and dopamine D2 receptor (K_i=0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

HY-100966

BD-1008 dihydrobromide	Antagonist	98.07%
BD-1008 dihydrobromide is an antagonist of sigma Receptor.

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