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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
58 Results for "
σ1 receptor antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (58)
58 Results for "σ1 receptor antagonist" in MCE Product Catalog:
4
4 Cited Publications
Synonyms: DHEA sulfate; Prasterone sulfate
Category:
Human Gut Microbiota Metabolites Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Steroids
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4
4 Cited Publications
Synonyms: DHEA sulfate sodium; Prasterone sulfate sodium
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4
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S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice [1] .
4
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S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >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] .
3
3 Cited Publications
Cat. No.: HY-18101A
CAS No.: 206996-13-6
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BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence [1] .
1
1 Cited Publications
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NE-100 hydrochloride is an orally active and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE-100 hydrochloride can improve cognitive impairment and has neuroprotective and antipsychotic activities. NE-100 hydrochloride can be used for research on nervous system diseases [1] .
1
1 Cited Publications
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σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=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].
1
1 Cited Publications
Cat. No.: HY-113416R
CAS No.: 651-48-9
Synonyms: DHEA sulfate (Standard); Prasterone sulfate (Standard)
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Pentoxyverine (Carbetapentane) 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 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] .
Cat. No.: HY-B1055
CAS No.: 23142-01-0
Synonyms: Carbetapentane citrate
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Pentoxyverine (Carbetapentane) citrate is an orally active and blood-brain barrier permeability 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] .
Synonyms: ACR16; ASP2314; FR310826
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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 Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
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BD-1008 is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 blocks the self-administration behavior of σ agonists.BD-1008 can be used for the study of addiction therapy that target the σ receptor [1] .
Synonyms: (+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride
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(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki 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] .
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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 (Ki = 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].
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Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively [1].
Synonyms: DHEA sulfate sodium-d6; Prasterone sulfate sodium-d6
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PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki 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] .
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Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki 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].
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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] .
Cat. No.: HY-P1341
CAS No.: 343268-91-7
Synonyms: Orexin A (17-33) (human, mouse, rat, bovine)
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
