Opioid Receptor Agonist

Asimadoline hydrochloride (Standard) (EMD-61753 hydrochloride (Standard)) is the analytical standard of Asimadoline (hydrochloride) (HY-107384A). This product is intended for research and analytical applications. Asimadoline (EMD-61753) hydrochloride 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 hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).

AZ 12488024 (AZD7268) is a SNC80 (HY-101202) derivative and a δ-opioid receptor agonist. AZ 12488024 is available for research into major depressive disorder.

R-84760 is a selective κ-opioid receptor agonist. R-84760 has antinociceptive effect.

AT-035 is a high affinity and selective NOP agonist.

U-48520 is an agonist for μ-opioid receptor with EC₅₀ of 1561 nM.

Salvinorin A (Divinorin A) propionate is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with K_i value of 4.3 nm. Salvinorin A propionate is a non-nitrogenous neoclerodane isolated from Salvia divinorum.

CYM51010 (Standard) is the analytical standard of CYM51010 (HY-104006). This product is intended for research and analytical applications. 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.

AT-127 is a NOP receptor partial agonist, stimulating NOP/G-protein interaction in a concentration dependent manner.

SCH 221510 (Standard) is the analytical standard of SCH 221510 (HY-107722). This product is intended for research and analytical applications. SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC₅₀ of 12 nM and K_i of 0.3 nM. SCH 221510 shows an anxiolytic-like effect.

Tramadol N-oxide (RWJ 38705) is an analgesic. Tramadol N-oxide sproduces dose-related, long-lasting antinociception. Tramadol N-oxide has affinity for μ opioid receptor (K_i = 38.5 μM) and δ, κ receptors (K_i > 100 μM). Tramadol N-oxide can be used for the study of analgesic effect.

PZM21 (Standard) is the analytical standard of PZM21 (HY-101386). This product is intended for research and analytical applications. PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.

NOP agonist-2 is a selective NOP agonist.

Tianeptine sodium salt (Standard) is the analytical standard of Tianeptine sodium salt (HY-90003A). This product is intended for research and analytical applications. Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.

Hodgkinsine B is an opioid receptor agonist and NMDA receptor antagonist, which has analgesic and anti-injurial effects. In addition, Hodgkinsine B has antiviral, antibacterial and antifungal activities.

Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. 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 (BK_Ca 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).

DPI-287 is a selective delta-opioid receptor (DOP) agonist with a K_i value of 0.39 nM and can be used for pain research.

Difelikefalin hydrochloride (CR-845 hydrochloride; FE-202845 hydrochloride) is an orally active peripherally acting kappa opioid receptor agonist. Difelikefalin hydrochloride reduces acute kidney injury, decreases oliguria, maintains urine flow, inhibits cytokine expression, and improves survival in endotoxemia after ischemia/reperfusion. Difelikefalin hydrochloride suppresses pruritus signals and exhibits neuromodulatory antipruritic activity. Difelikefalin hydrochloride can be used in research related to acute kidney injury, chronic kidney disease-associated pruritus, and atopic dermatitis.

NOP agonist-1(compound 4) is a nociceptin opioid receptor (NOP) partial agonist. NOP agonist-1attenuate parkinsonian disabilities in 6-OHDA hemilesioned rats.

Salvinorin A carbamate is an agonist for κ-opioid receptor with an EC₅₀ of 6.2 nM and a K_i of 3.2 nM.

Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM.