87 Results for "

threshold

" in MedChemExpress (MCE) Product Catalog:
Products (87)

87 Results for "threshold" in MCE Product Catalog:

25
25 Publications Verification
Cat. No.: HY-B1302
CAS No.: 6151-40-2
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures .
loading...
    loading...
24
24 Cited Publications
Cat. No.: HY-B1751
CAS No.: 56-54-2
Quinidine (15% dihydroquinidine) is an orally active antiarrhythmic agent. Quinidine (15% dihydroquinidine) reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine (15% dihydroquinidine) exerts sustained block and open-channel block effects on IK(f). Quinidine (15% dihydroquinidine) alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine (15% dihydroquinidine) can be used in studies related to uterine sarcoma and seizures .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-P10234A
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

Poneratoxin acetate is the acetate salt form of Poneratoxin (HY-P10234). Poneratoxin acetate is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-N0745
CAS No.: 94596-28-8
Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A) . Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-15292
CAS No.: 927871-76-9
Purity:  99.77%
Target:  

Calcium Channel

Research Areas:  

Cardiovascular Disease

S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca 2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-14218
CAS No.: 97-39-2
Purity:  99.66%
Synonyms: 1,3-Di-o-tolylguanidine; DTG
Target:  

Sigma Receptor

Research Areas:  

Neurological Disease

Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki 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 .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-B0188A
CAS No.: 21535-47-7
Synonyms: Org GB 94
Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-103175
CAS No.: 524944-72-7
Purity:  ≥99.0%
PSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-B0188
CAS No.: 24219-97-4
Synonyms: Mianserine
Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-N5084
CAS No.: 205370-59-8
Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a TRPV1 antagonist and HDAC7 inhibitor. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside blocks TRPV1-mediated calcium influx, suppresses phosphorylation of p65, IκBα, p38, JNK, and ERK1/2, inhibiting NF-κB and MAPK signaling cascades. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside reduces production and gene expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside exhibits potent analgesic activity, elevates thermal pain threshold and mechanical pain threshold in murine models. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside restores CD8 + T cell infiltration into bladder cancer tumors and improves bladder cancer immunotherapy efficacy. Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside can be used for the researches of painand bladder cancer .
loading...
    loading...
Cat. No.: HY-W105835
CAS No.: 3344-18-1
Synonyms: Trimagnesium dicitrate
Research Areas:  

Neurological Disease

Magnesium citrate (Trimagnesium dicitrate) is an orally active magnesium-containing compound that can cross the blood-brain barrier (BBB). Magnesium citrate can be used as an intestinal cleanser and is studied for its application in laxatives. Magnesium citrate can also increase the pain threshold and is studied for pain-relief purposes .
loading...
    loading...
Cat. No.: HY-W011235
CAS No.: 57226-68-3
Norfluoxetine hydrochloride is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K2P potassium channel inhibitor. Norfluoxetine hydrochloride exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine hydrochloride inhibits high-threshold voltage-gated Ca 2+ currents in neurons with an EC50 of 20.4 μM. Norfluoxetine hydrochloride can be used in research related to depression, ischemic stroke, and epilepsy .
loading...
    loading...
Cat. No.: HY-P1626
CAS No.: 928007-64-1
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

Acetyl tetrapeptide-15 is a synthetic peptide. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway. Acetyl tetrapeptide-15 is used in the cosmetics for sensitive skin .
loading...
    loading...
Cat. No.: HY-B1233
CAS No.: 543-82-8
Synonyms: 2-Amino-6-methylheptane; 1,5-Dimethylhexylamine; 6-Methyl-2-heptylamine
Octodrine (2-Amino-6-methylheptane) is a central nervous stimulant that increases the uptake of dopamine and noradrenaline. Octodrine is found to increase the pain threshold, cardiac rate (positive chronotropic effect) and myocardial contractility (positive inotropic effect) .
loading...
    loading...
Cat. No.: HY-W067716
CAS No.: 59981-63-4
Synonyms: (S)-Spinacine
Spinacine ((S)-Spinacine) is a GABA uptake inhibitor. Spinacine enhances synaptic GABA effects via inhibition of gamma-aminobutyric acid uptake in cerebral cortex slices. Spinacine inhibits reflex responses of ventral roots in isolated spinal cord. Spinacine inhibits motor activity and reduces approaches to water dispensers in conflict situations. Spinacine raises pain sensitivity threshold via subarachnoidal injection .
loading...
    loading...
Cat. No.: HY-18961
CAS No.: 622864-54-4
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .
loading...
    loading...
Cat. No.: HY-125928
CAS No.: 354812-16-1
Purity:  ≥98.0%
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

AA43279 is an in gamma-aminobutyric acid (GABA) fast-firing interneurons located activator for Nav1.1 channel (SCN1A) with an EC50 of 9.5 μM. AA43279 enhances specific neuronal firing activity in vitro, and exhibits anticonvulsant activity in rat MEST model .
loading...
    loading...
Cat. No.: HY-135556
CAS No.: 83891-03-6
Norfluoxetine is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K2P potassium channel inhibitor. Norfluoxetine exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine inhibits high-threshold voltage-gated Ca 2+ currents in neurons with an EC50 of 20.4 μM. Norfluoxetine can be used in research related to depression, ischemic stroke, and epilepsy .
loading...
    loading...
Cat. No.: HY-121650A
CAS No.: 13575-86-5
Purity:  98.0%
ADTN hydrobromide is a long-acting dopamine agonist. ADTN hydrobromide significantly decreases the behavioral visual threshold of DA-IPC-depleted zebrafish .
loading...
    loading...
Cat. No.: HY-179215
CAS No.: 2093928-29-9
Target:  

GABA Receptor

Research Areas:  

Neurological Disease

OV329 hydrochloride is a potent GABA aminotransferase inactivator. OV329 hydrochloride is a Vigabatrin (HY-15399) analogue. OV329 hydrochloride can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 hydrochloride exhibits anticonvulsant and antiepileptic activities. OV329 hydrochloride can be used for the research of neurological disease, such as seizure .
loading...
    loading...