2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor

Opioid Receptor

Receptor

Opioid Receptor

Related Products

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Opioid receptors are a group of G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. Opioid receptors are distributed widely in the brain, and are found in the spinal cord and digestive tract. Opioid receptors are molecules, or sites, within the body that are activated by opioid substances. Opioid receptors inhibit the transmission of impulse in excitatory pathways within the human body system. These pathways include the serotonin, catecholamine, and substance P pathways, which are all implicated in pain perception and feelings of well-being. Opioid receptors are further subclassified into mu, delta, and kappa receptors. All the classes, while exhibiting differing modes of action, share some basic similarities. They all are driven by the potassium pump mechanism, which is found on the plasma membrane of the majority of cells.

Opioid Receptor Isoform Specific Products:

Opioid Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P1329A
    CTOP TFA
    		Antagonist 99.84%
    CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity.
    CTOP TFA
  • HY-139690
    CCG258747
    		Inhibitor 98.96%
    CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
    CCG258747
  • HY-12844
    Ro 64-6198
    		Agonist 99.82%
    Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia.
    Ro 64-6198
  • HY-136208
    TAN-452
    		Antagonist 99.44%
    TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
    TAN-452
  • HY-107741
    SNC162
    		Agonist 99.72%
    SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like and antinociceptiv effects.
    SNC162
  • HY-13044
    ADL-5859 hydrochloride
    		Agonist 99.77%
    ADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain.
    ADL-5859 hydrochloride
  • HY-P3870A
    DALDA acetate
    		Agonist 99.78%
    DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects.
    DALDA acetate
  • HY-P1087
    Adrenorphin
    		Agonist
    Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
    Adrenorphin
  • HY-101416
    Vanilpyruvic acid
    		98.28%
    Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
    Vanilpyruvic acid
  • HY-107721
    (±)-J-113397
    		Antagonist 98.59%
    (±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ.
    (±)-J-113397
  • HY-P1299A
    UFP-101 TFA
    		Antagonist 99.36%
    UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect.
    UFP-101 TFA
  • HY-104006
    CYM51010
    		Agonist 99.12%
    CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms.
    CYM51010
  • HY-N0398
    Sec-O-Glucosylhamaudol
    		Inhibitor 99.81%
    Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.
    Sec-O-Glucosylhamaudol
  • HY-115066
    GSK1521498 free base
    		Antagonist 98.55%
    GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents.
    GSK1521498 free base
  • HY-13243
    Alvimopan
    		Antagonist 98.66%
    Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus.
    Alvimopan
  • HY-B0380
    Trimebutine
    		Agonist 99.42%
    Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine
  • HY-124959
    Spiradoline mesylate
    		Agonist 99.95%
    Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier.
    Spiradoline mesylate
  • HY-101205
    ICI 199441
    		Agonist 99.39%
    ICI 199441 is a potent and selective κ-opioid receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion.
    ICI 199441
  • HY-114072
    J-113397
    		Antagonist 99.00%
    J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.
    J-113397
  • HY-P1337
    Dynorphin B (1-13)
    		Agonist 98.09%
    Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.
    Dynorphin B (1-13)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

μ Opioid Receptor/MOR

κ Opioid Receptor/KOR

δ Opioid Receptor/DOR

NOP Receptor/ORL1

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Please try each isoform separately.

Opioid Receptor Inhibitors, Agonists, Antagonists, Activators & Modulators
Product Nameμ Opioid Receptor/MORκ Opioid Receptor/KORδ Opioid Receptor/DORNOP Receptor/ORL1Purity    
DAMGO
μ Opioid Receptor/MOR
   99.90%
Matrine
μ Opioid Receptor/MOR
κ Opioid Receptor/KOR
  ≥98.0%
Isotodesnitazene
μ Opioid Receptor/MOR
   99.78%
Sinomenine
μ Opioid Receptor/MOR
   99.94%
Aticaprant 
κ Opioid Receptor/KOR
  99.87%
Norbinaltorphimine dihydrochloride 
κ Opioid Receptor/KOR
  98.91%
Dynorphin A 
κ Opioid Receptor/KOR
  
Sinomenine hydrochloride
μ Opioid Receptor/MOR
   99.89%
β-Endorphin, human  
δ Opioid Receptor/DOR
 98.09%
JTC-801   
NOP Receptor/ORL1
98.91%
SNC80  
δ Opioid Receptor/DOR
 99.82%
Difelikefalin 
κ Opioid Receptor/KOR
  99.50%
BMS-986122
μ Opioid Receptor/MOR
   99.94%
Endomorphin 1
μ Opioid Receptor/MOR, Ki: 1.11 nM
   99.92%
Corydaline
μ Opioid Receptor/MOR
   99.70%
Alvimopan dihydrate
μ Opioid Receptor/MOR
   98.66%
LY2940094   
NOP Receptor/ORL1
99.91%
SB-612111 hydrochloride   
NOP Receptor/ORL1
99.26%
PZM21
μ Opioid Receptor/MOR
   99.46%
CTAP TFA
μ Opioid Receptor/MOR, IC50: 3.5 nM
 
δ Opioid Receptor/DOR, IC50: 4500 nM
 99.60%
DPDPE  
δ Opioid Receptor/DOR
 99.83%
Navacaprant
μ Opioid Receptor/MOR, IC50: 110 nM
κ Opioid Receptor/KOR, IC50: 0.8 nM
δ Opioid Receptor/DOR, IC50: 6500 nM
 99.97%
Dermorphin
μ Opioid Receptor/MOR
   99.96%
Naldemedine tosylate
μ Opioid Receptor/MOR
   
[Met5]-Enkephalin, amide TFA  
δ Opioid Receptor/DOR
 99.58%
N-Desmethylclozapine  
δ Opioid Receptor/DOR
 98.99%
BMS-986187  
δ Opioid Receptor/DOR
 98.93%
Dynorphin A (1-8) 
κ Opioid Receptor/KOR
  99.88%
Porcine dynorphin A(1-13) 
κ Opioid Receptor/KOR
  99.85%
U-69593 
κ Opioid Receptor/KOR
  99.73%
Deltorphin I  
δ Opioid Receptor/DOR
 
Morphiceptin
μ Opioid Receptor/MOR
   
Endomorphin 2 TFA
μ Opioid Receptor/MOR
   99.43%
BAN ORL 24   
NOP Receptor/ORL1
99.68%
Trimebutine maleate
μ Opioid Receptor/MOR
   99.91%
Dynorphin A (1-10) (TFA) 
κ Opioid Receptor/KOR
  
Deltorphin 2 TFA  
δ Opioid Receptor/DOR
 99.93%
DAMGO TFA
μ Opioid Receptor/MOR
   99.60%
CTOP TFA
μ Opioid Receptor/MOR
   99.84%
Ro 64-6198   
NOP Receptor/ORL1
99.82%
TAN-452  
δ Opioid Receptor/DOR
 99.44%
SNC162  
δ Opioid Receptor/DOR
 99.72%
ADL-5859 hydrochloride  
δ Opioid Receptor/DOR
 99.77%
Adrenorphin
μ Opioid Receptor/MOR
   
(±)-J-113397   
NOP Receptor/ORL1
98.59%
UFP-101 TFA   
NOP Receptor/ORL1
99.36%
CYM51010
μ Opioid Receptor/MOR
   99.12%
Sec-O-Glucosylhamaudol
μ Opioid Receptor/MOR
   99.81%
GSK1521498 free base
μ Opioid Receptor/MOR
   98.55%
Trimebutine
μ Opioid Receptor/MOR
   99.42%
ICI 199441 
κ Opioid Receptor/KOR
  99.39%
J-113397
μ Opioid Receptor/MOR, Ki: 1000 ± 160 nM
κ Opioid Receptor/KOR, Ki: 640 ± 87 nM
δ Opioid Receptor/DOR, Ki: >10000 nM
NOP Receptor/ORL1, Ki: 1.8 ± 0.24 nM
99.00%
Naloxonazine dihydrochloride
μ Opioid Receptor/MOR, IC50: 5.4 nM
   98.1%
Dynorphin B (1-13) TFA 
κ Opioid Receptor/KOR
  
KNT-127  
δ Opioid Receptor/DOR
 99.60%
Endomorphin 1 acetate
μ Opioid Receptor/MOR, Ki: 1.11 nM
   99.92%
SR17018
μ Opioid Receptor/MOR
   98.01%
MT-7716 hydrochloride   
NOP Receptor/ORL1
99.06%
AR-M 1000390 hydrochloride  
δ Opioid Receptor/DOR
 98.20%
[D-Ala2]leucine-enkephalin  
δ Opioid Receptor/DOR
 98.64%
5'-Guanidinonaltrindole hydrochloride
human μ-opioid receptor, Ki: 36.9 nM
human μ-opioid receptor, pA2: 8.49
   98.72%
TAN-67 dihydrobromide  
δ Opioid Receptor/DOR, Ki: 0.647 nM
 99.20%
LY255582
μ Opioid Receptor/MOR, Ki: 0.4 nM
κ Opioid Receptor/KOR, Ki: 2.0 nM
δ Opioid Receptor/DOR, Ki: 5.2 nM
 ≥98.0%
Asimadoline hydrochloride 
κ Opioid Receptor/KOR
  99.82%
β-Endorphin, equine TFA
μ Opioid Receptor/MOR
 
δ Opioid Receptor/DOR
 
DIPPA hydrochloride 
κ Opioid Receptor/KOR
  99.7%
Nociceptin (1-13), amide TFA   
NOP Receptor/ORL1
99.67%
Deltorphin 2  
δ Opioid Receptor/DOR
 
BMS-986121
μ Opioid Receptor/MOR
   98.89%
Bevenopran
μ Opioid Receptor/MOR
   99.82%
DPDPE TFA  
δ Opioid Receptor/DOR
 99.94%
Gluten Exorphin C
μ Opioid Receptor/MOR
 
δ Opioid Receptor/DOR
 99.86%
Cebranopadol ((1α,4α)stereoisomer)   
NOP Receptor/ORL1
LY2444296 
κ Opioid Receptor/KOR
  99.59%
Dalargin  
δ Opioid Receptor/DOR
 99.52%
Samidorphan-d5
μ Opioid Receptor/MOR
κ Opioid Receptor/KOR
δ Opioid Receptor/DOR
 
Alvimopan monohydrate
μ Opioid Receptor/MOR
   99.18%
GSK1521498 free base (hydrochloride)
μ Opioid Receptor/MOR
   
CTAP
μ Opioid Receptor/MOR, IC50: 3.5 nM
 
δ Opioid Receptor/DOR, IC50: 4500 nM
 
AT-076
μ Opioid Receptor/MOR, IC50: 1.67 nM
κ Opioid Receptor/KOR, IC50: 1.14 nM
δ Opioid Receptor/DOR, IC50: 19.6 nM
NOP Receptor/ORL1, IC50: 1.75 nM
SC13
μ Opioid Receptor/MOR
   
SalA-VS-07 
κ Opioid Receptor/KOR
  
NAQ
μ Opioid Receptor/MOR, Ki: 0.55 nM
κ Opioid Receptor/KOR, Ki: 26.45 nM
δ Opioid Receptor/DOR, Ki: 132.50 nM
 
KOR agonist 4
human μ-opioid receptor, Ki: 280 nM
human κ-opioid receptor (hKOR), EC50: 14 nM
human κ-opioid receptor (hKOR), Ki: 4.8 nM
δ Opioid Receptor/DOR, Ki: 3900 nM
 
N-Desmethylclozapine-d8  
δ Opioid Receptor/DOR
 
Nociceptin (1-13), amide   
NOP Receptor/ORL1
Mu opioid receptor antagonist 4
μ Opioid Receptor/MOR
   
SB-612111   
NOP Receptor/ORL1
Bilaid C
human μ-opioid receptor, Ki: 210 nM
   
Dermorphin TFA
μ Opioid Receptor/MOR
   
DALDA
μ Opioid Receptor/MOR, Ki: 1.69 nM
κ Opioid Receptor/KOR, Ki: 4230 nM
δ Opioid Receptor/DOR, Ki: 19200 nM
 
KOR/DOR agonist 1
μ Opioid Receptor/MOR, Ki: 0.93 nM
κ Opioid Receptor/KOR, Ki: 0.14 nM
δ Opioid Receptor/DOR, Ki: 0.2 nM
 
Acetalin-3
μ Opioid Receptor/MOR
   
KOR agonist 3
μ Opioid Receptor/MOR, EC50: 720 nM
κ Opioid Receptor/KOR, EC50: 0.88 nM
  
DS34942424
μ Opioid Receptor/MOR
   
Acetyl tetrapeptide-15
μ Opioid Receptor/MOR
   99.49%
Bilaid A1e
μ Opioid Receptor/MOR, Ki: 750 nM
   
LY2048978
μ Opioid Receptor/MOR, Ki: 0.287 nM
κ Opioid Receptor/KOR, Ki: 0.471 nM
δ Opioid Receptor/DOR, Ki: 1.05 nM
 
Mu opioid receptor antagonist 5
μ Opioid Receptor/MOR
   
(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) 
κ Opioid Receptor/KOR
  
Mu opioid receptor antagonist 3
μ Opioid Receptor/MOR
   
AP-238
μ Opioid Receptor/MOR, EC50: 248 nM
   
KOR agonist 2 
κ Opioid Receptor/KOR, Ki: 1.9 nM
  
AT-121 hydrochloride
μ Opioid Receptor/MOR
   
MT-7716 free base   
NOP Receptor/ORL1
Nociceptin(1-7)   
NOP Receptor/ORL1
Mu opioid receptor antagonist 2
μ Opioid Receptor/MOR
   
Dynorphin A TFA 
κ Opioid Receptor/KOR
  
rel-SB-612111 hydrochloride   
NOP Receptor/ORL1
PIPE-3297 
κ Opioid Receptor/KOR, EC50: 1.1 nM
  
[DPen2, Pen5] Enkephalin  
δ Opioid Receptor/DOR
 
GSK1521498
μ Opioid Receptor/MOR
   
Trap-101 hydrochloride   
NOP Receptor/ORL1
Anrikefon 
κ Opioid Receptor/KOR
  
β-Funaltrexamine hydrochloride
μ Opioid Receptor/MOR
   
ZP 120C   
NOP Receptor/ORL1
3-Carboxamidonaltrexone
μ Opioid Receptor/MOR, Ki: 1.9 nM
κ Opioid Receptor/KOR, Ki: 22 nM
δ Opioid Receptor/DOR, Ki: 110 nM
 
KOR agonist 1
μ Opioid Receptor/MOR, EC50: 701.2 nM
κ Opioid Receptor/KOR, EC50: 3.4 nM
δ Opioid Receptor/DOR, EC50: 1649 nM
 
[Met5]-Enkephalin, amide  
δ Opioid Receptor/DOR
 
TRPV1 antagonist 11
μ Opioid Receptor/MOR, Ki: 60.3 nM
   
Mu opioid receptor antagonist 7
μ Opioid Receptor/MOR, IC50: 29 ± 3.0 nM
   
DPI-3290 
κ Opioid Receptor/KOR
δ Opioid Receptor/DOR
 
N-Benzylnaltrindole hydrochloride  
δ Opioid Receptor/DOR
 
Dynorphin A (1-10) 
κ Opioid Receptor/KOR
  
Akuammidine 
κ Opioid Receptor/KOR
  
Mu opioid receptor antagonist 1
μ Opioid Receptor/MOR
   
K-Opioid receptor agonist-1
μ Opioid Receptor/MOR, Ki: 43 nM
κ Opioid Receptor/KOR, Ki: 0.25 nM
δ Opioid Receptor/DOR, Ki: 58 nM
 
Ac-RYYRWK-NH2 TFA   
NOP Receptor/ORL1
μ opioid receptor agonist 3
μ Opioid Receptor/MOR, EC50: 0.82 nM
   
BAM-12P 
human κ-opioid receptor (hKOR), EC50: 101 nM
human κ-opioid receptor (hKOR), pEC50: 6.99
  
Naloxegol-d5 oxalate
μ Opioid Receptor/MOR
   
Nociceptin(1-7) TFA   
NOP Receptor/ORL1
MOR modulator-1
μ Opioid Receptor/MOR, Ki: 0.25 nM
κ Opioid Receptor/KOR, Ki: 1.3 nM
δ Opioid Receptor/DOR, Ki: 41.1 nM
 
UFP-101   
NOP Receptor/ORL1
Acetalin-1
μ Opioid Receptor/MOR
   
CTOP
μ Opioid Receptor/MOR
   
Axelopran
human μ-opioid receptor, pKi: 9.8
guinea pig κ-opioid receptor, pKi: 9.9
δ Opioid Receptor/DOR, pKi: 8.8
 
Trimebutine-d3 hydrochloride
μ Opioid Receptor/MOR
   
δ opioid receptor antagonist 1  
δ Opioid Receptor/DOR, Ki: 1.7 nM
 
Opioid receptor agonist 1
μ Opioid Receptor/MOR, Ki: 5 nM
κ Opioid Receptor/KOR, Ki: 212 nM
δ Opioid Receptor/DOR, Ki: 24 nM
 
MOR agonist-2
μ Opioid Receptor/MOR
   
α-Endorphin (human)
μ Opioid Receptor/MOR
   
Dermorphin Analog
μ Opioid Receptor/MOR
   
Trimebutine-d5 fumarate
μ Opioid Receptor/MOR
   
DSLET  
δ Opioid Receptor/DOR
 
NPFF1-R antagonist 1
μ Opioid Receptor/MOR, Ki: 3560 ± 364 nM
κ Opioid Receptor/KOR, Ki: 1390 ± 147 nM
δ Opioid Receptor/DOR, Ki: 1540 ± 132 nM
 
FEKAP 
κ Opioid Receptor/KOR, Ki: 0.43 nM
  
Trimebutine maleate (Standard)
μ Opioid Receptor/MOR
   
RX809055AX
μ Opioid Receptor/MOR
 
δ Opioid Receptor/DOR
 
R-84760 
κ Opioid Receptor/KOR
  
U-48520
μ Opioid Receptor/MOR, EC50: 1561 nM
   
Salvinorin A propionate 
κ Opioid Receptor/KOR
  
CHIR 4531
μ Opioid Receptor/MOR, Ki: 6 nM
   
Picraline
μ Opioid Receptor/MOR, Ki: 132 μM
κ Opioid Receptor/KOR, Ki: 2.38 μM
δ Opioid Receptor/DOR, Ki: 98.8 μM
 
Trimebutine (Standard)
μ Opioid Receptor/MOR
   
BNTX  
δ Opioid Receptor/DOR
 
Salvinorin A carbamate 
κ Opioid Receptor/KOR, EC50: 6.2 nM
  
Endomorphin 2
μ Opioid Receptor/MOR