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sigma receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Sigma Receptor (101) 5-HT Receptor (9) Adenylate Cyclase (1) Adrenergic Receptor (2) Akt (3) Apoptosis (8) Cholinesterase (ChE) (1) Cytochrome P450 (1) Dopamine Receptor (8) ERK (1) Ferroptosis (1) Histamine Receptor (6) iGluR (2) Isotope-Labeled Compounds (1) mAChR (6) Monoamine Oxidase (1) NO Synthase (3) Opioid Receptor (9) Potassium Channel (2) Proteasome (1) SARS-CoV (3)
By Research Areas:	Cancer (22) Cardiovascular Disease (7) Endocrinology (1) Infection (3) Inflammation/Immunology (13) Metabolic Disease (1) Neurological Disease (92)

123

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Sigma Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-125819

Sigma-1 receptor antagonist 2	Sigma Receptor	Neurological Disease
Sigma-1 receptor antagonist 2 is a potent and selective **sigma 1 receptor** (σ1 R) antagonist with K_is of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively .

HY-125820

Sigma-1 receptor antagonist 3	Sigma Receptor Potassium Channel	Neurological Disease
Sigma-1 receptor antagonist 3 (compound135) is a potent and selective **Sigma-1 (σ1) receptor antagonist with a K_i** of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC₅₀ of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain .

HY-125821

Sigma-1 receptor antagonist 1	Sigma Receptor	Neurological Disease
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective **sigma-1 receptor (σ1R)** antagonist, with a high binding affinity to σ1R receptor (K_i = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain .

HY-10815

*σ1 Receptor* antagonist-1** 1 Publications Verification	Sigma Receptor Apoptosis	Neurological Disease Cancer
σ1 Receptor antagonist-1 is a highly potent and selective **sigma 1 receptor antagonist (pK_i*=10.28). σ1 Receptor* antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .

HY-111669

CT1812 1 Publications Verification sigma-2 receptor antagonist 1	Sigma Receptor	Neurological Disease
CT1812 (Sigma-2 receptor antagonist 1) is an orally active and brain penetrant *sigma-2* receptor antagonist with a K_i of 8.5 nM. CT1812 can be used for the research of Alzheimer’s disease .

HY-162759

Sigma-1 receptor antagonist 6	Sigma Receptor	Neurological Disease
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-108513

*σ1 Receptor* antagonist 4**	Sigma Receptor	Neurological Disease
σ1 Receptor antagonist 4 (compound TC1) is a selective **sigma1 (σ1) receptor antagonist with a K_i** of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (K_i of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters .

HY-149335

Sigma-1 receptor antagonist 5	Sigma Receptor Histamine Receptor	Neurological Disease
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-147560

*σ1 Receptor/μ Opioid receptor* modulator 1**	Sigma Receptor Opioid Receptor	Neurological Disease
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-168562

*σ1 Receptor* ligand 1**	Sigma Receptor	Neurological Disease Cancer
σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a K_i of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .

HY-163065

*σ1 Receptor/μ Opioid receptor* modulator 2**	Opioid Receptor Sigma Receptor	Neurological Disease
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-149274

Sigma-1 receptor antagonist 4	Sigma Receptor	Neurological Disease
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-100966

BD-1008 dihydrobromide	Sigma Receptor	Neurological Disease
BD-1008 dihydrobromide is an antagonist of **sigma Receptor** .

HY-101626

Sigma-LIGAND-1	Sigma Receptor	Neurological Disease
Sigma-LIGAND-1 is a selective **sigma receptor ligand with an IC₅₀*s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 has a K_i* of 4000 nM at the dopamine D₂ receptor .

HY-101626A

Sigma-LIGAND-1 hydrochloride	Sigma Receptor	Neurological Disease
Sigma-LIGAND-1 hydrochloride is a selective **sigma receptor ligand with an IC₅₀*s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a K_i* of 4000 nM at the dopamine D₂ receptor .

HY-108514

(±)-PPCC hemioxalate	Sigma Receptor	Neurological Disease Cancer
(±)-PPCC hemioxalate is a compound that has the ability to regulate the activity of the *sigma-1* receptor. (±)-PPCC hemioxalate can selectively bind *sigma-1* protein (s1), and then activate s1 receptor leading to dissociation of s1-BIP complex to regulate ER-mitochondrial calcium signaling, which plays an important role in cell bioenergy and cell survival. (±)-PPCC hemioxalate can be used to study *sigma-1* receptors in cocaine addiction, forgetting, pain, depression, Alzheimer's disease, stroke, and cancer .

HY-118901

Opipramol Ensidon; G-33040	Sigma Receptor	Neurological Disease
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-118901R

Opipramol (Standard)	Sigma Receptor	Neurological Disease
Opipramol (Standard) is the analytical standard of Opipramol. This product is intended for research and analytical applications. 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-108509

BMY-14802 hydrochloride BMY-14802-1; BMS 181100 hydrochloride	Sigma Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active **sigma receptor antagonist with an IC₅₀ of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A** and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects .

HY-B1216

Oxeladin citrate	Sigma Receptor	Cardiovascular Disease Others Neurological Disease
Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective **sigma 1 receptor agonist (K_i** = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research .

HY-B1216R

Oxeladin citrate (Standard)	Sigma Receptor	Cardiovascular Disease Others Neurological Disease
Oxeladin (citrate) (Standard) is the analytical standard of Oxeladin (citrate). This product is intended for research and analytical applications. Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (Ki = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research .

HY-135608

BD-1008	Others	Others
BD-1008 is a selective antagonist of the sigma receptors, demonstrating a binding affinity of K? = 2 ± 1 nM for the sigma-1 receptor and exhibiting fourfold selectivity over the sigma-2 receptor.

HY-117420

CM764	Sigma Receptor	Cancer
CM764 is an activator for **sigma receptor with K_i** of 86.6 and 3.5 nM for sigma-1 receptor and sigma-2 receptor. CM764 increases cytoplasmic calcium, NAD ⁺/NADH, and ATP levels, and decreases the concentration of ROS .

HY-118279

KSCM-1	Sigma Receptor	Neurological Disease
KSCM-1 is a selective **sigma-1 receptor ligand with a K_i** of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors .

HY-14221

Siramesine Lu 28-179	Sigma Receptor	Cancer
Siramesine (Lu 28-179) is a potent **sigma-2 receptor** agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .

HY-14221A

Siramesine hydrochloride 4 Publications Verification Lu 28-179 hydrochloride	Sigma Receptor Ferroptosis	Cancer
Siramesine (Lu 28-179) hydrochloride is a potent **sigma-2 receptor** agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .

HY-14221B

Siramesine fumarate LU-28-179 fumarate	Sigma Receptor	Cancer
Siramesine (Lu 28-179) fumarate is a potent **sigma-2 receptor** agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .

HY-155615

KSK67	Sigma Receptor Histamine Receptor	Neurological Disease
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-14218

Ditolylguanidine 2 Publications Verification 1,3-Di-o-tolylguanidine; DTG	Sigma Receptor	Neurological Disease
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 *receptor) with K_i* values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer .

HY-155614

KSK68	Sigma Receptor Histamine Receptor	Neurological Disease
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-14813

Cutamesine SA4503; AGY 94806	Sigma Receptor	Neurological Disease
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.

HY-155616

KSK94	Sigma Receptor Histamine Receptor	Neurological Disease
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-120236

KSCM-5	Others	Neurological Disease
KSCM-5 is a sigma receptor ligand with high affinity activity on sigma-1 receptor. The Ki value of KSCM-5 is about 34nM, showing significant selectivity. KSCM-5 has potential application value in compound development, especially for diseases related to sigma receptors .

HY-100155

4-IBP	Sigma Receptor	Cancer
4-IBP is a selective σ1 agonist, binding to σ1 receptors with high affinity (Ki = 1.7 nM) and with slightly weaker affinity to σ2 receptors (Ki = 25.2 nM).

HY-169185

Sigma-2 Radioligand 2	Sigma Receptor	Cancer
Sigma-2 Radioligand 2 (compund 4) exhibits low nanomolar affinity (Ki(σ2)=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500) for the σ2 receptor .

HY-101864

Blarcamesine hydrochloride 3 Publications Verification Anavex 2-73	Sigma Receptor	Neurological Disease Cancer
Blarcamesine hydrochloride (Anavex 2-73) is a **Sigma-1 Receptor agonist with an IC₅₀** of 860 nM.

HY-108512

PD 144418 1 Publications Verification	Sigma Receptor	Neurological Disease
PD 144418 is a highly affinity, potent and selective **sigma 1 (σ1) receptor ligand (K_i** values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity .

HY-B2087

Glycerol phenylbutyrate HPN-100	Sigma Receptor	Cardiovascular Disease
Glycerol phenylbutyrate is a **sigma-2 (σ2)** receptor ligand, with a pK_i of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger agent .

HY-100985

IPAG	Sigma Receptor	Cancer
IPAG is a potent **sigma-1 receptor antagonist with a pK_i of 4.3 . IPAG induces apoptosis** .

HY-124462

Trifluperidol hydrochloride R 2498	Sigma Receptor	Neurological Disease
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-108512A

PD 144418 oxalate 1 Publications Verification	Sigma Receptor	Neurological Disease
PD 144418 oxalate is a highly affinity, potent and selective **sigma 1 (σ1) receptor ligand (K_i** values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity .

HY-111081

(±)-PPCC	Sigma Receptor	Neurological Disease
(±)-PPCC is a *sigma-1* agonist that mainly interacts with *sigma-1* receptors with K_i of 1.5 nM. (±)-PPCC has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats .

HY-116594A

OPC-14523 hydrochloride	Sigma Receptor 5-HT Receptor	Neurological Disease
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 .

HY-111081C

(±)-PPCC oxalate	Sigma Receptor	Neurological Disease
(±)-PPCC oxalate is a *sigma-1* agonist that mainly interacts with *sigma-1* receptors with K_i of 1.5 nM. (±)-PPCC oxalate has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats .

HY-A0172

Captodiame Captodiamine	5-HT Receptor Dopamine Receptor Sigma Receptor	Neurological Disease
Captodiame (Captodiamine) is a 5-HT_2c receptor antagonist and *sigma-1* and D3 dopamine receptor agonist. Captodiame shows antidepressant effect .

HY-163075

SYB4	Others	Others
SYB4 (compound 5) is a PET tracer which suitable for imaging the **Sigma-2 Receptor** in the brain of nonhuman primates .

HY-116594

OPC-14523 free base	Sigma Receptor 5-HT Receptor	Neurological Disease
OPC-14523 free base 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 free base shows antidepressant-like activity .

HY-134189

EST73502	Opioid Receptor Sigma Receptor	Neurological Disease
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-121867

KSCM-11	Others	Others
KSCM-11 is a ligand of thesigma receptor .

HY-116463

E1R	Sigma Receptor	Neurological Disease
E1R is a positive allosteric modulator of **sigma-1 receptors (Sig1R PAM**) with cognition-enhancing activity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13716

Noscapine 1 Publications Verification (S,R)-Noscapine	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Source classification Quinoline Alkaloids Papaver somniferum Linn. Plants Inflammation/Immunology Disease Research Fields Papaveraceae	Opioid Receptor Apoptosis
Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating **sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis**. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .

HY-13716R

Noscapine (Standard)	Structural Classification Alkaloids Source classification Quinoline Alkaloids Papaver somniferum Linn. Plants Papaveraceae	Opioid Receptor Apoptosis
Noscapine (Standard) is the analytical standard of Noscapine. This product is intended for research and analytical applications. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier [4] .

Cat. No.	Product Name	Chemical Structure

HY-13716S

Noscapine-13C,d3

Noscapine-13C,d3 is a deuterated labeled Noscapine . Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .

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