Opioid Receptor Agonist

α-Casein (90-95) TFA is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) TFA inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC₅₀= 0.1 μM. α-Casein (90-95) TFA inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC₅₀ of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) TFA activates G_i-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) TFA can be used in the study of the mechanisms of allergic diseases and prostate cancer.

Loperamide-d₆ (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea.

N-Desmethylclozapine-d₈ (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist.

α-Casein (90-95) is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC₅₀= 0.1 μM. α-Casein (90-95) inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC₅₀ of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) activates G_i-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) can be used in the study of the mechanisms of allergic diseases and prostate cancer.

Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC₅₀s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).

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

Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.

(S)-MCOPPB is the S-form of MCOPPB (HY-13101). MCOPPB is an orally active and selective agonist of Nociceptin/Orphanin FQ-Receptor. MCOPPB inhibits signaling through the NOP receptor in the mouse brain. MCOPPB can be used for anxiety disorders study.

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

JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia.

ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.

CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC₅₀s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively.

Loperamide oxide (Standard) is the analytical standard of Loperamide oxide. This product is intended for research and analytical applications. Loperamide oxide (R-58425) is a orally active prodrug of the Loperamide (HY-156131). Loperamide oxide incubation with the contents of the intestinal lumen inhibits fluid secretion under aerobic conditions.

GR 89696 free base is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus.

CCI-1008 is an opioid receptor agonist. CCI-1008 can be used for research on nervous system diseases.

Iprindole hydrochloride, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole hydrochloride shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole hydrochloride induces lamellar body formation but devoid of lamellar bodies. Iprindole hydrochloride can be used for the research of depression.

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.

[Leu5]-Enkephalin TFA is a pentapeptide with morphine like properties. [Leu5]-Enkephalin TFA is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.

SC13 is an orally active, selective Flap structure-specific endonuclease 1 (FEN1) inhibitor and mu opioid receptor (MOR) activator. SC13 impairs DNA damage repair and induces apoptosis in cancer cells. SC13 activates cGAS-STING signaling, increases chemokine secretion, and promotes CAR-T cell infiltration at solid tumour sites. SC13 can be used for the research of solid tumours and pain.

BRL-52656 is a blood-brain barrier (BBB)-penetrable KOR receptor agonist that exhibits a biphasic effect. At low doses, BRL-52656 decreases blood pressure, whereas high doses have the opposite effect in spontaneously hypertensive rats. Additionally, BRL-52656 induces water diuresis by inhibiting the secretion of vasopressin (AVP).