Opioid Receptor Activator

Opioid Receptor Activators (25):

Cat. No.	Product Name	Effect	Purity

HY-15122

Sinomenine	Activator	99.96%
Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.

HY-P0073

Tyr-Gly-Gly-Phe-Met-OH	Activator	99.56%
Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.

HY-15122A

Sinomenine hydrochloride	Activator	99.89%
Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.

HY-B0188A

Mianserin hydrochloride	Activator	99.95%
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.

HY-N2392

Kukoamine A	Activator	99.88%
Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE₂, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease.

HY-111664

(R)-(+)-Citronellal	Activator	98.72%
(R)-(+)-Citronellal ((+)-Citronellal) is a monoterpenoid compound and is one of the main components of essential oils from plants such as lemon grass. (R)-(+)-Citronellal has antibacterial, antifungal, and insecticidal activities. (R)-(+)-Citronellal alleviates the bitterness of caffeine by antagonizing the bitter taste receptors Tas2r43 (IC₅₀ = 84 μM) and Tas2R46. (R)-(+)-Citronellal generates analgesic activity by activating the opioid receptor (broad-spectrum opioid receptor) pathway, and its effect is particularly significant for inflammatory pain.

HY-B0188

Mianserin	Activator	99.42%
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.

HY-120613

BMS-986187	Activator	99.66%
BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC₅₀ of 0.03 μM and a pK_B of 6.02 (～1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC₅₀=3 μM).

HY-15122R

Sinomenine (Standard)	Activator
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.

HY-128038

N-Desmethyl-loperamide	Activator	98.36%
N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a K_i value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein.

HY-P0318

Hemorphin-7	Activator
Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).

HY-117702

RB 101	Activator
RB 101 is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor. RB 101 blocks enkephalin breakdown, elevates extracellular enkephalin levels and activate δ-opioid receptor and dopamine D1 receptor. RB 101 can be used for the research of pain, depressive syndromes, and diabetic neuropathy.

HY-U00031

Axomadol	Activator	99.74%
Axomadol (EN3324) is a centrally active analgesic agent with opioid agonistic properties and inhibitory effects on the reuptake of monoamines.

HY-B0188S

Mianserin-d₃	Activator
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). 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.

HY-B0188AR

Mianserin hydrochloride (Standard)	Activator
Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride 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.

HY-181103

ERG-IN-6	Activator
ERG-IN-6 (compound (+)-(S)-5a) is a μ-opioid receptor activator with an EC₅₀ of 0.12 nM. ERG-IN-6 also is a hERG (Kv11.1) potassium channel inhibitor with an IC₅₀ of 0.681 μM. ERG-IN-6 can be used for the research of pain.

HY-115500

PL265	Activator
PL265 is an orally active dual enkephalinase inhibitor. PL265 is a prodrug of PL254, which can simultaneously and efficiently inhibit neutral endopeptidase (Neprilysin) and Aminopeptidase N. PL265 can effectively protect and significantly increase the local concentration of enkephalins (such as Met-Enkephalin and Leu-Enkephalin) released by cells at the pain or inflammation sites, thereby activating μ and δ opioid receptors to produce a potent analgesic effect. PL254 can also inhibit leukotriene A4 hydrolase (LTA4H), which may contribute to its additional anti-inflammatory effect by reducing the production of pro-inflammatory mediator leukotriene B4 (LTB4). PL265 can be used in non-addictive chronic pain research.

HY-P5907

Helianorphin-19	Activator
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a K_i of 21 nM and an EC₅₀ of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain.

HY-121854A

Bromadoline maleate	Activator
Bromadoline maleate is an opioid analgesic selective for the μ-opioid receptor, exhibiting analgesic activity in various biological fluids. Bromadoline maleate has been successfully quantified alongside its N-demethylated metabolites in human and canine samples.

HY-19267

Ro-48-6791	Activator
Ro-48-6791 is a compound that may have the activity of activating opioid receptors. Computational studies have found that it may bind to and activate opioid receptors, and may mediate or increase their related physiological effects and side effects.

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