Opioid Receptor Agonist

Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.

BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [³⁵S]GTPγS binding in mouse brain membranes.

N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine 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 is also a δ-opioid agonist.

Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.

(±)-Salsolinol hydrochloride is the hydrochloride form of (±)-Salsolinol (HY-113316). (±)-Salsolinol hydrochloride is a Dopamine (HY-B0451)-derived endogenous metabolite. (±)-Salsolinol hydrochloride activates μ-opioid receptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA).

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

(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist.

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

MCOPPB trihydrochloride is a NOP/ORL1 G protein-coupled receptor agonist and autophagy inhibitor that can cross the blood-brain barrier. MCOPPB trihydrochloride clears senescent cells, regulates locomotion, lipid storage and immune responses, and inhibits fibrosis and angiogenesis. MCOPPB trihydrochloride blocks autophagic flux, induces changes in locomotion and lipid storage, and activates the stress-responsive immune transcription network, thereby improving post-infarction cardiac function and exerting anxiolytic effects. MCOPPB trihydrochloride can be applied to research fields such as aging-related diseases and ischemic heart failure.

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).

DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a K_d of 3.46 nM for native μ-OPR.

Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate 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 maleate 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 maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

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.

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

SNC162 is a delta-opioid receptor agonist with an IC₅₀ of 0.94 nM. SNC162 has antidepressant-like and antinociceptiv effects.

Loperamide (hydrochloride) (Standard) is the analytical standard of Loperamide (hydrochloride). This product is intended for research and analytical applications. Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.

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

DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a K_i of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects.

Noscapine ((S,R)-Noscapine) hydrochloride is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.

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.