ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

BAN ORL 24 is a potent, selective, competitive ORL1 non-peptide agonist. Displays 1000-fold selectivity over classical opioid receptors.

branopadol(GRT-6005) is a novel first in class compounds with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor.

BU09059 is a potent, selective, short-acting kappa-opioid receptor antagonist with Ki of 1.72 nM, displays 15- and 616-fold selectivity over μ- and δ-receptors respectively.

CERC-501(LY-2456302) is a potent, selective antagonist of the kappa opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR), respectively.

Eluxadoline is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist.

JDTic 2Hcl is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.

Meptazinol Hcl(WY-22811 Hcl) is a unique centrally active opioid analgesic.

Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.

NFEPP is a novel potent, selective pH-dependent μ-opioid receptor (MOR) agonist with a low pKa, shows significantly lower affinity compared with fentanyl at pH 7.4.

PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.

Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.

Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.

LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.

β-Casomorphin, bovine TFA (β-Casomorphin-7 (bovine) TFA) is a opioid peptide with an IC50 of 14 μM in an Opioid receptors binding assay.

β-Casomorphin, human TFA (Human β-casomorphin 7 TFA) is an opioid peptide, acts as an agonist of opioid receptor.

Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP,?μ-,?κ-, and?δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous?system?diseases.

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.

Loperamide phenyl is an impurity of Loperamide. Loperamide is an opioid receptor agonist.

Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties.

[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).

[(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).

[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.

[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.

Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice.

Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice.

Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors.

Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors.

Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.

Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.

Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin. Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.

Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin. Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.

[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.

[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.

CTOP TFA is a peptide that acts as a μ-opioid receptor antagonist.

Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors,? such as mu (MOR) and delta (DOR).

Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors,? such as mu (MOR) and delta (DOR).

DPDPE, an opioid peptide, is a selective δ-opioid receptor?(DOR) agonist?with anticonvulsant effects.

DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor?(DOR) agonist?with anticonvulsant effects.

CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID).

PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats.

PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats.

Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).

EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.

Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of cebranopadol. Cebranopadol is a potent agonist activity on ORL-1.

UFP-101 TFA is a potent, selective, and competitive antagonist of the 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.

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.

LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.

Deltorphin 2 TFA is a selective peptide agonist for the δ opioid receptor.

Nociceptin (1-13), amide TFA is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.

BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs.

DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant.

DAMGO (DAGO) is a potent and selective μ opioid receptor agonist with ki of 17 nM.

Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1).

SC13 is a novel mitragynine analog with low-efficacy Mu opioid receptor agonism that displays antinociception with attenuated adverse effects.

DS34942424 is an orally potent analgesic without mu opioid receptor agonist activity.

Riminkefon is a kappa opioid receptor agonist.

Tegileridine is the potent agonist of opioid receptor (MOR). Tegileridine is an oxa spiro derivative which reduces the side effects mediated by β-arrestin. Tegileridine has the potential for the research of pains and pains-related diseases (extracted from patent WO2017063509A1).

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.

Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. 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.

BPR1M97 is a dual-acting mu-opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively.BPR1M97 elicited full agonist properties for all cell-based assays tested in MOP-expressing cells.BPR1M97 acted as a G protein-biased agonist for NOP.BPR1M97 initiated faster antinociceptive effects after subcutaneous injection and elicited better analgesia in cancer-induced pain than morphine.BPR1M97 caused less respiratory, cardiovascular, and gastrointestinal dysfunction, compared with morphine.

R995045 is a novel δ-opioid receptor (δOR) agonist with pKi of 5.94, cAMP pIC50 of 6.01, >10-fold selectivity over µOR and κOR.R995045 acts as a negative allosteric modulator for leu-enkephalin potency in the cAMP glosensor assay.

VISTA inhibitor M351-056 is a small molecule compound having affinity with VISTA.

Eptazocine (Sedapain) is a κ-opioid receptor agonist and μ-opioid receptor antagonist. Eptazocine has the effect of relieving pain.

BW373U86 (SNC86) is a δ-opioid receptor agonist with an IC50 of 1.49 nM. BW373U86 shows antidepressant-like effects.

SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like effects and produces a selective enhancement of the antinociceptive effects of fentanyl in rhesus monkeys.

[Leu5]Enkephalin a five amino acid endogenous peptide that acts as an agonist at opioid receptors.

ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia.

NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence.

(S,S)-J-113397 is an isomer of J-113397. J-113397 is an Opioid Receptor antagonist.

Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function.

(Rac)-SNC80 is a racemate of SNC80. SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

AT-039 is a potent, selective agonist of nociceptin opioid peptide (NOP) receptor, AT-039 is useful for treatment of hypertension and/or volume overload/hyponatraemic states.

LY2817412 is a potent, selective andorally active nociceptin/orphanin FQ (NOP) receptor antagonist with Ki of 0.176 nM, Kb of 0.273 nM in functional assay of receptor-mediated G-protein activation using [35S]-GTPγS binding.

MP135 is a potent, μ-δ opioid receptor heteromer-selective agonist with EC50 of 0.8 nM in GTPγS assays, shows functional selectivity for μ-δ heteromers over homomeric μOR and δOR and low β-arrestin2 recruitment activity.

A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.

PIPE-3297 is a fully efficacious and selective kappa opioid receptor (KOR) agonist with functional GTPγS EC50 of 1.1 nM, Emax=91%, does not elicit β-arrestin-2 recruitment functional response.

PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.

ZYKR1 is a potent, and peripherally restricted kappa opioid receptor (KOR)-selective agonist with EC50 of 0.061 nM in cAMP assays, highly selective over the mu and delta opioid receptors (EC50>10 μM).

Icalcaprant is a kappa-opioid receptor antagonist.