opioid receptor

Mu opioid receptor antagonist 3 (compound 26) is a potent and selective mu opioid receptor (MOR) antagonist that penetrates the blood-brain barrier (Ki: 0.24 nM, EC50: 0.54 nM). Mu opioid receptor antagonist 2 can be used to study opioid use disorder (OUD).

Opioid receptor modulator 1 is a modulator of opioid receptor.

μ opioid receptor agonist 2 （Compound H-3）is a MOR receptor agonist. μ opioid receptor agonist 2 can be used for the research of pain and pain related diseases.

σ 1 Receptor/ μ Opioid receiver modulator 1 (Compound 44) is an effective σ 1 receptor antagonist (Ki=1.86 nM) and μ Opioid receptor agonists (Ki=2.1 nM). Opioid receptor modulator 1 shows potent analgesic activity, and can be used for the research of neuropathic pain.

Compound 24, also known as Mu opioid receptor antagonist 7, is a potent, centrally-acting µ-opioid receptor (µOR) antagonist with an inhibitory concentration (IC50) of 29 ± 3.0 nM. It is valuable for pain and opioid use disorder research [1].

Mu opioid receptor antagonist 4 (compound 31) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.38 nM, EC50: 0.38 nM). Mu opioid receptor antagonist 2 can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 2 (compound 25) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM). Mu opioid receptor antagonist 2 can be used to study opioid use disorder (OUD).

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM. It holds promise for research into pain management and neuropsychiatric disorders [1].

μ opioid receptor agonist 1 (Compound H-1a) is an optically pure oxyheterocyclic substituted pyrroloxypyrazole derivative and an MOR receptor agonist that can be used in the study of pain and pain-related disorders.

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier (EC50: 1.14 nM, Ki: 0.37 nM). Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).

Potent, selective agonist of Mu-opioid receptor. Antinociceptive. Stimulates calcium-activated adenylyl cyclases related cAMP production. Expresses chemokines and chemokine receptors through TGF-beta1. Increases food intake of rats.

Aticaprant (LY-2456302) (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).

BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) . BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.

CP 866087 is an opioid receptor antagonist for the study of female sexual dysfunction.

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

CP-866087 is a novel, potent and selective mu-opioid receptor antagonist for the study of female sexual dysfunction.

[DPro10] Dynorphin A (1-11)acetate,porcine is a highly potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine is an n-alkylated derivative with analgesic activity.

Faxeladol, a potent adrenergic absorption inhibitor and serotonin reuptake inhibitor, is a small-molecule Opioid receptor agonist that can be used to study neurological disorders.

Dynorphin B (1-13) acetate acts as an agonist on opioid κ-receptor.

β-Endorphin (1-27) (human) acetate, existing in the hypophysis cerebri and hypothalamus, exhibits antinociception activity. β-Endorphin (1-27) (human) acetate is an agonist of opioid receptor, showing preferred affinity for μ-opioid receptor and δ-opioid

Dermorphin TFA is a new class of opioids-like peptides

[Leu5]-Enkephalin, amide acetate is a δ opioid receptor agonist.

Adrenorphin 3TFA(88377-68-8(free base)) (Metorphamide) is an agonist of μ-opioid receptor(Ki :12 nM).

Dynorphin A (1-10) acetate is an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.

Acetyl tetrapeptide-15 Acetate (Skinasensyl Acetate), a synthetic peptide used in cosmetic products for sensitive skin, is an endomorphin-2 derivative that extends the range of neuronal excitability thresholds in the μ-opioid receptor via an endorphin-like pathway, and can be used to study inflammatory and neuropathic pain produced by skin hyperreactivity. Inflammatory and neuropathic pain produced by skin hyperresponsiveness.

1,1'-(Octane-1,8-diyl)diguanidine dihydrochloride is a synthetic opioid peptide derived from the natural opioid peptide enkephalin. It is a potent agonist of the mu-opioid receptor (MOR) with a Ki of 0.14 nM, making it one of the most potent MOR agonists known to date.

Leuphasyl TFA is an amid peptide, a δ-opioid receptor agonist, is a degradation resistant long-acting Leu-enkephalin analog used to study the signaling pathway of delta opioid receptors. Leuphasyl TFA is a potent, long-acting Leu-enkephalin analog that is resistant to enzymatic degradation

Nociceptin (1-7) acetate is a potent agonist of opioid receptor-like 1 (ORL1) receptor. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia and has antinociceptive activity.

beta-Neoendorphin acetate is an agonist of κ-opioid receptor

Samidorphan HCl is an orally active and highly potent modulator of the opioid system that binds to μ‐opioid, κ‐opioid, and delta-opioid receptors. Samidorphan HCl is a novel μ-opioid receptor antagonist, a partial agonist for k-opioid and delta-opioid receptors. Samidorphan HCl can be used to prevent and treat schizophrenia.

CTAP(TFA) (103429-32-9 free base) is a potent, highly selective, and brain-penetrant antagonist of the μ-opioid receptor with IC50 of 3.5 nM. It displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP(TFA） (103429-32-9 free base) can be used for the study of L-DOPA-induced dyskinesia (LID)

Deltorphin (Dermenkephalin) is Isolated from the skin of Phyllomedusa Sauvage. It also has an affinity to the opioid receptor.

Endomorphins-2 (EM-2) could decrease both the frequency and amplitude of the sEPSC of the motoneurons in lamina IX, which was reversed by the MOR antagonist CTOP. EM-2-IR fibers originated from primary afferent fibers form symmetric synaptic connections with motoneurons innervating skeletal muscles of the lower limbs in lamina IX of the spinal ventral horn and EM-2 might exert inhibitory effects on the activities of these motoneurons through both presynaptic and postsynaptic mechanisms.

Porcine dynorphin A(1-13) acetate (Dynorphin A Porcine Fragment 1-13 acetate) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations. Exposure to dynorphin A (1-13) causes acute increases in [Ca2+]i in individual neurons similar to increases seen with acute NMDA treatment.

Trimebutine CTB salt (GIC-1001) is an opioid receptor agonist used in the study of pain.

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

[Leu5]-Enkephalin acetate(58822-25-6 free base) is an endogenous neuropeptide involved in nociception and an agonist of δ-opioid and μ-opioid receptors (Kis = 4.0 and 3.4 nM, respectively)

JNJ-20788560 is a delta opioid receptor (DOR) agonist with analgesic activity. It is more selective for DOR than for mu opioid receptors (MOR).

CTOP acetate is a somatostatin analogue and a μ-opioid receptor antagonist.

Deltorphin 2 ([D-Ala2]-Deltorphin II) is an agonist of δ opioid receptor with an IC50 of 1 nM.

Nociceptin (1-13), amide is a potent agonist Opioid receptor-like1 (ORL1) receptor with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.

Orphanin FQ(1-11) acetate(178249-41-7 free base) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) acetate(178249-41-7 free base) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) acetate(178249-41-7 free base) displays analgesic properties in CD-1 mice.

Difelikefalin acetate (CR 845 acetate) is a peripherally restricted kappa opioid receptor agonist. CR845 exhibit low P450 CYP inhibition and low penetration into the brain.

GR103545 is a selective agonist of the κ-opioid receptor, which is a radiotracer that can be used as in vivo imaging.

UFP-101 acetate is a selective and competitive antagonist of the NOP receptor (pKi = 10.24) with >3000-fold selectivity over δ, μ, and κ opioid receptors.

ADL-5747 (ADL-5747 (free base)) (free base) is a delta opioid receptor agonist used in the treatment of neurological disorders, skin and musculoskeletal disorders, and may be used in the study of postherpetic neuralgia, knee osteoarthritis and pain.

(D-Ser2)-Leu-Enkephalin-Thr is a delta selective agent of opioid receptor and shows analgesic effects.

Dup 747 is an analgesic that binds with high affinity and selectivity to the kappa-opioid receptor.

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

Norbinaltorphimine dihydrochloride is a selective and potent κ opioid receptor antagonist that induces itch-associated responses in mice.

Loperamide hydrochloride (ADL 2-1294) is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.

Loperamide-d6 is a deuterated compound of Loperamide. Loperamide has a CAS number of 53179-11-6.