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Isoforms Recommended:	Sigma 1 Receptor

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Sigma-1 receptor

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By Targets:	Sigma Receptor (72) 5-HT Receptor (6) Adrenergic Receptor (1) Akt (3) Apoptosis (3) Cholinesterase (ChE) (1) Cytochrome P450 (1) Dopamine Receptor (4) Ferroptosis (1) Histamine Receptor (5) iGluR (2) mAChR (6) Monoamine Oxidase (1) NO Synthase (3) Opioid Receptor (5) Potassium Channel (2) SARS-CoV (2)
By Research Areas:	Cancer (12) Cardiovascular Disease (5) Infection (2) Inflammation/Immunology (8) Metabolic Disease (1) Neurological Disease (65)

Targets Recommended: Sigma Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-131914

EST64454	Sigma Receptor
EST64454 (compound 9k) is a selective, orally active *sigma-1* receptor antagonist with K_i 22 nM. EST64454 can be used to study 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-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-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-134004

Pentoxyverine Carbetapentane	Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (Carbetapentane) is an orally active **sigma-1 receptor agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic** antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .

HY-B1055

Pentoxyverine citrate Carbetapentane citrate	Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (Carbetapentane) citrate is an orally active **sigma-1 receptor agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic** antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .

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-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-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-134004R

Pentoxyverine (Standard)	Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active **sigma-1 receptor agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic** antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .

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-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-B1055R

Pentoxyverine citrate (Standard)	Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance [4].

HY-116463

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

HY-131914A

EST64454 hydrochloride	Sigma Receptor	Neurological Disease
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 .

HY-155484

SOMCL-668	Sigma Receptor	Neurological Disease
SOMCL-668 is a selective and potent **sigma-1 receptor** allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research .

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-16996A

BD-1047 dihydrobromide 5+ Cited Publications	Sigma Receptor	Neurological Disease
BD-1047 (dihydrobromide) is a selective functional antagonist of **sigma-1 receptor**, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia .

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-B1733

Phenyltoloxamine Bistrimin; Histionex	Histamine Receptor Sigma Receptor Cytochrome P450	Neurological Disease Inflammation/Immunology
Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent **Sigma-1 receptor** binding affinity (K_i: 160 nM) .

HY-105296

Blarcamesine 3 Publications Verification	Sigma Receptor mAChR	Cancer
Blarcamesine is an orally bioavailable **Sigma-1 receptor** agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .

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-153091

BMY 14802	Adrenergic Receptor 5-HT Receptor Sigma Receptor	Neurological Disease
BMY 14802 is a **sigma-1 receptor** (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .

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-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-116463D

(Rac)-E1R	Sigma Receptor	Neurological Disease
(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a **sigma-1 receptor positive allosteric modulator (Sig1R PAM**) used for the research of cognition/memory disorders .

HY-101484A

NE-100 hydrochloride	Sigma Receptor	Neurological Disease
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-18099A

S1RA hydrochloride 1 Publications Verification E-52862 hydrochloride	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a K_i value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (K_i >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC₅₀ value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .

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-116463A

(2R,3S)-E1R	Sigma Receptor	Neurological Disease
(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a **sigma-1 receptor positive allosteric modulator (Sig1R PAM**) for the treatment of cognition/memory disorders .

HY-116463B

(2S,3S)-E1R	Sigma Receptor	Neurological Disease
(2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a **sigma-1 receptor positive allosteric modulator (Sig1R PAM**) for the treatment of cognition/memory disorders .

HY-116463C

(2R,3R)-E1R	Sigma Receptor	Neurological Disease
(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a **sigma-1 receptor positive allosteric modulator (Sig1R PAM**) for the treatment of cognition/memory disorders .

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-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-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-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-134189A

EST73502 monohydrochloride	Sigma Receptor Opioid Receptor	Neurological Disease
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-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 .

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Sigma-1 receptor

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