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σ1 receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (4) Adrenergic Receptor (1) Apoptosis (3) Dopamine Receptor (3) Histamine Receptor (4) iGluR (2) mAChR (4) Opioid Receptor (5) Potassium Channel (2) SARS-CoV (2) Sigma Receptor (36)
By Research Areas:	Cancer (4) Infection (2) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (34)

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-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-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-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 ^[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-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) ^[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-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-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-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-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 ^[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-14222

UMB24	Sigma Receptor	Neurological Disease
UMB24 is a potent antagonist of σ2 receptor, with K_i values of 170 nM anf 322 nM for σ2 receptor and σ1 receptor, respectively. UMB24 attenuats cocaine-induced convulsions and locomotor activity, but not lethality ^[1].

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 ^[1] [4].

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-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-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-131914B

EST64454 maleate	Others	Inflammation/Immunology
EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.

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-100985

IPAG	Sigma Receptor	Cancer
IPAG is a potent **sigma-1 receptor** antagonist with a pK_i of 4.3 ^[1]. 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 ^[1].

HY-18101A

BD1063 dhydrochloride 3 Publications Verification	Sigma Receptor	Metabolic Disease
BD1063 dhydrochloride is a potent and selective **sigma 1 receptor** antagonist.

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-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 ^[1].

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-16996A

BD-1047 dihydrobromide Maximum Cited Publications 6 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-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-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 ^[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-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-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-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].

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-101043

4-PPBP maleate	Sigma Receptor iGluR	Neurological Disease
4-PPBP maleate is a potent **σ 1 receptor** ligand and agonist. 4-PPBP maleate is a non-competitive, selective **NR1a/2B NMDA receptors** (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection ^[1] .

HY-10684

Pridopidine ACR16; ASP2314; FR310826	Dopamine Receptor	Neurological Disease
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards **sigma 1 receptor** (S1R) with K_i between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.

HY-111210

Pridopidine hydrochloride ACR16 hydrochloride; ASP2314 hydrochloride; FR310826 hydrochloride	Dopamine Receptor	Neurological Disease
Pridopidine (ACR16) hydrochloride, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards **sigma 1 receptor** (S1R) with K_i between 70 and 80 nM, which is ~100-fold higher than its affinity toward D2R.

HY-161873

PW507	Sigma Receptor	Neurological Disease
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) ^[1].

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