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Results for "

σ1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) Adrenergic Receptor (1) Akt (2) Apoptosis (3) Cholinesterase (ChE) (1) Cytochrome P450 (1) Dopamine Receptor (3) Ferroptosis (1) Histamine Receptor (5) iGluR (1) mAChR (4) Monoamine Oxidase (1) NO Synthase (2) Opioid Receptor (5) Potassium Channel (2) SARS-CoV (2) Sigma Receptor (55)
By Research Areas:	Cancer (9) Cardiovascular Disease (3) Infection (2) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (51)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 ^[1].

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 ^[1].

HY-108512

PD 144418	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 ^[1] .

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 ^[1].

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 ^[1].

HY-108512A

PD 144418 oxalate	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 ^[1] .

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 ^[1].

HY-116586

AF710B	Sigma Receptor	Neurological Disease
AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease ^[1].

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 ^[1] .

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 ^[1] .

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-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 ^[1] .

HY-18099

S1RA 1 Publications Verification E-52862	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with K_is of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT_2B receptor (K_i= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice ^[1] .

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 ^[1].

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 ^[1].

HY-B1813A

(±)-Vesamicol hydrochloride (±)-AH5183 hydrochloride	Sigma Receptor	Neurological Disease
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a K_i of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with K_is of 26 nM and 34 nM, respectively ^[1] .

HY-151562

AChE/BuChE/MAO-B-IN-1	Cholinesterase (ChE) Monoamine Oxidase	Neurological Disease
AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC₅₀s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ₁ and σ₂ receptors with K_i values of 42.8 nM (human σ₁ receptor) and 191 nM (rat σ₂ receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research ^[1].

HY-101376

(+)-N-Allylnormetazocine hydrochloride (+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride	Opioid Receptor	Neurological Disease
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with K_i values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease ^[1] .

HY-18100A

PRE-084 hydrochloride Maximum Cited Publications 7 Publications Verification	Sigma Receptor Akt NO Synthase	Cardiovascular Disease Neurological Disease
PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC₅₀ of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway ^[1] .

HY-18100

PRE-084	Sigma Receptor Akt NO Synthase	Cardiovascular Disease Neurological Disease
PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC₅₀ of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway ^[1] .

HY-130344

SKF 83959 1 Publications Verification	Dopamine Receptor Sigma Receptor	Neurological Disease
SKF83959 is a potent and selective dopamine *D₁-like* receptor partial agonist. SKF83959 K_i values for rat D₁, D₅, D₂ and D₃ receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression ^[1] .

HY-107708

threo-Ifenprodil hemitartrate	iGluR Sigma Receptor Potassium Channel	Neurological Disease
threo Ifenprodil hemitartrate is a σ receptor agonist, with K_is of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC₅₀=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC ₅₀ of 88 nM, showing antiarrhythmic activity ^[1] .

HY-103412

SKF 83959 hydrobromide 1 Publications Verification	Dopamine Receptor Sigma Receptor	Neurological Disease
SKF83959 hydrobromide is a potent and selective dopamine *D₁-like* receptor partial agonist. SKF83959 hydrobromide K_i values for rat D₁, D₅, D₂ and D₃ receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression ^[1] .

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 ^[1] .

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 ^[1] .

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 ^[1].

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 ^[1].

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 ^[1].

HY-108511A

PB28	Sigma Receptor Apoptosis SARS-CoV	Infection Cancer
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 is also a σ1 antagonist with a K_i of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC₅₀ values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity ^[1] .

HY-108511

PB28 dihydrochloride	Sigma Receptor Apoptosis SARS-CoV	Infection Cancer
PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a K_i of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC₅₀ values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity ^[1] .

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 ^[1].

HY-101864

Blarcamesine hydrochloride 2 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-100985

IPAG

IPAG is a potent sigma-1 receptor antagonist with a pK_i of 4.3 ^[1]. IPAG induces apoptosis .

IPAG
IPAG is a potent sigma-1 receptor antagonist with a pK_i of 4.3 ^[1]. IPAG induces apoptosis .

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 ^[1].

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-116463

E1R

Sigma Receptor Neurological Disease

E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity ^[1].

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

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 ^[1].

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 ^[1].

HY-16996A

BD-1047 dihydrobromide 5 Publications Verification	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 ^[1].

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) ^[1] .

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 ^[1] .

HY-120842

RLH-033	mAChR	Neurological Disease
RLH-033 is a potent and selective ligand for the *sigma 1* recognition site. RLH-033 has high affinity for sigma 1 sites labeled by [ ³H](+)-pentazocine with a K_i of 50 pM ^[1].

HY-105296

Blarcamesine 2 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 ^[1].

HY-B2215

Dimemorfan phosphate 1 Publications Verification	Sigma Receptor	Neurological Disease Inflammation/Immunology
Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.

HY-18101A

BD1063 dhydrochloride

1 Publications Verification

Sigma Receptor Metabolic Disease

BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.

BD1063 dhydrochloride 1 Publications Verification	Sigma Receptor	Metabolic Disease
BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.

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 ^[1].

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 ^[1] .

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 ^[1].

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 ^[1].

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