2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor
  5. Opioid Receptor Isoform
  6. Opioid Receptor Activator

Opioid Receptor Activator

Opioid Receptor Activators (16):

Cat. No. Product Name Effect Purity
  • 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-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-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 Ki 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-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-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-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 Ki 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.
  • HY-15122AR
    Sinomenine hydrochloride (Standard)
    		Activator
    Sinomenine hydrochloride (Standard) is the analytical standard of Sinomenine hydrochloride. This product is intended for research and analytical applications. 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-129237
    Azo-enkephalin
    		Activator
    Azo-enkephalin is an endorphin analog with significant analgesic activity. Azo-enkephalin can be used in the development of opioid analgesics.
  • HY-176106
    1-Naphthyl U-47700
    		Activator
    1-Naphthyl U-47700 is an α-isomer. 1-Naphthyl U-47700 is a racemic mixtures of the trans-isomers [R,R and S,S]. 1-Naphthyl U-47700 activates MOR in a concentration-dependent manner (EC50 > 23 μM).