Search Result

Results for "

pain threshold

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) 5-HT Receptor (2) Adenosine Receptor (1) Apoptosis (1) Caspase (1) CGRP Receptor (1) DAGL (1) Dopamine Receptor (2) Epigenetic Reader Domain (1) ERK (4) GABA Receptor (2) HDAC (1) Heme Oxygenase (HO) (1) Interleukin Related (2) JNK (1) Keap1-Nrf2 (1) NF-κB (1) Opioid Receptor (4) p38 MAPK (2) Potassium Channel (1) Reference Standards (1) Sodium Channel (3) TNF Receptor (1) Toll-like Receptor (TLR) (1) TRP Channel (2)
By Research Areas:	Cancer (2) Cardiovascular Disease (1) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (19)

By Targets:

11β-HSD (1)

5-HT Receptor (2)

Adenosine Receptor (1)

Apoptosis (1)

Caspase (1)

CGRP Receptor (1)

DAGL (1)

Dopamine Receptor (2)

Epigenetic Reader Domain (1)

ERK (4)

GABA Receptor (2)

HDAC (1)

Heme Oxygenase (HO) (1)

Interleukin Related (2)

JNK (1)

Keap1-Nrf2 (1)

NF-κB (1)

Opioid Receptor (4)

p38 MAPK (2)

Potassium Channel (1)

Reference Standards (1)

Sodium Channel (3)

TNF Receptor (1)

Toll-like Receptor (TLR) (1)

TRP Channel (2)

By Research Areas:

Cancer (2)

Cardiovascular Disease (1)

Inflammation/Immunology (5)

Metabolic Disease (1)

Neurological Disease (19)

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W105835

Magnesium citrate Trimagnesium dicitrate	Toll-like Receptor (TLR)	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 .

HY-103175

PSB36 1 Publications Verification	Adenosine Receptor	Cardiovascular Disease Neurological Disease Inflammation/Immunology
PSB36 is a highly selective A₁ adenosine receptor antagonist, with a K_i of 0.12 nM and a K_d 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 .

HY-N0745

Senkyunolide I	Caspase ERK Keap1-Nrf2 Heme Oxygenase (HO) Apoptosis	Neurological Disease Inflammation/Immunology
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 .

HY-N5084

Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside	TRP Channel HDAC p38 MAPK JNK ERK NF-κB TNF Receptor Interleukin Related	Neurological Disease Inflammation/Immunology Cancer
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 .

HY-P1626

Acetyl tetrapeptide-15	Opioid Receptor	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 .

HY-B1233

Octodrine 2-Amino-6-methylheptane; 1,5-Dimethylhexylamine; 6-Methyl-2-heptylamine	Dopamine Receptor	Others
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) .

HY-W067716

Spinacine (S)-Spinacine	GABA Receptor	Neurological Disease
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 .

HY-101546A

Cavidine (+)-Cavidine	p38 MAPK ERK Interleukin Related	Neurological Disease Inflammation/Immunology
Cavidine ((+)-Cavidine) is an analgesic and anti-inflammatory agent. Cavidine can be isolated from Corydalis ternata f. yanhusuo (Y.H.Chou & Chun C.Hsu) Y.C.Zhu. Cavidine reduces the expression of inflammatory factors IL-1β, IL-6 and TNF-α, and inhibits calcium ion influx. Cavidine inhibits the phosphorylation of p38 and ERK1/2. Cavidine increases mechanical and thermal pain thresholds in chronic pain models. Cavidine can be used for the research of chronic pain .

HY-B1233A

Octodrine hydrochloride 2-Amino-6-methylheptane hydrochloride; 1,5-Dimethylhexylamine hydrochloride; 6-Methyl-2-heptylamine hydrochloride	Dopamine Receptor	Neurological Disease
Octodrine (2-Amino-6-methylheptane) is a central nervous activator 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) .

HY-110302

6'-GNTI dihydrochloride	Opioid Receptor	Neurological Disease
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .

HY-P10234A

Poneratoxin acetate 3 Publications Verification	Sodium Channel	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 .

HY-10635

ABT-102	TRP Channel	Inflammation/Immunology Cancer
ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain .

HY-N2433

Paederosidic acid methyl ester	Potassium Channel	Neurological Disease
Paederosidic acid methyl ester is a ATP‐sensitive K ⁺ channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K ⁺ channel in the brain and spinal cord level .

HY-120496

Clofutriben ASP3662	11β-HSD	Neurological Disease Metabolic Disease
Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with K_i values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain .

HY-P10234

Poneratoxin	Sodium Channel	Neurological Disease
Poneratoxin 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 .

HY-W067716R

Spinacine (Standard) (S)-Spinacine (Standard)	Reference Standards GABA Receptor	Neurological Disease
Spinacine (Standard) is the analytical standard of Spinacine (HY-W067716). This product is intended for research and analytical applications. 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 .

HY-111011

CR 665 acetate JNJ 38488502 acetate; FE 200665 acetate	Opioid Receptor	Neurological Disease
CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.

HY-P1336A

Deltorphin I TFA Deltorphin 1 TFA; Deltorphin C TFA; [D-Ala2] Deltorphin I TFA	Opioid Receptor	Neurological Disease
Deltorphin I TFA (Deltorphin 1 TFA; Deltorphin C TFA; [D-Ala2] Deltorphin I TFA) is a high-affinity, selective δ-opioid receptor agonist that targets the δ1 and δ2 opioid receptor subtypes. Deltorphin I TFA produces analgesic effects in the rat spinal cord. Deltorphin I TFA increases the pain threshold in rats. Deltorphin I TFA can be used in studies related to nociception (acute pain) .

HY-183652

5-HT2C-agonist-14	5-HT Receptor Sodium Channel	Neurological Disease
5-HT2C-agonist-14 is a 5-HT2C receptor agonist with an EC₅₀ of 2.9 μM against human receptors. It also acts as a voltage-gated sodium channel inhibitor and is a blood-brain barrier permeable compound. 5-HT2C-agonist-14 elevates seizure threshold, suppresses seizure progression and alleviates pain-related behaviors. It can be used in the research of epilepsy and pain-related diseases .

HY-181482

A1480LS	DAGL	Neurological Disease
A1480LS is a peripherally restricted, orally active covalent and irreversible inhibitor of DAGLα and DAGLβ, with IC₅₀ values of 6 nM and 4 nM against human targets, respectively, and IC₅₀ values ≤15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy .

HY-179684

PCC0105005	CGRP Receptor 5-HT Receptor ERK Epigenetic Reader Domain	Neurological Disease
PCC0105005 is a dual-target CGRP Receptor antagonist (IC₅₀ = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC₅₀ = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine .

Cat. No.	Product Name	Target	Research Area