Opioid Receptor Agonist

Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). 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.

JO-1870 hydrochloride is a selective opioid receptor agonist. JO-1870 hydrochloride exerts bladder relaxation via activation of opioid receptors. JO-1870 hydrochloride is promising for research of urinary incontinence.

Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects.

Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=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.

Atoxifent is a potent μ-opioid receptor agonist (EC₅₀=0.39 nM). These receptors are found in brain regions that control pain, emotions, habitual learning, and cognition. Atoxifent exhibits strong analgesic effects and a lower risk of respiratory depression. Atoxifent can be used for research in opioid pharmacology and signal transduction.

AR-M 1000390 is an exceptionally selective, potent δ opioid receptor agonist with an EC₅₀ of 7.2±0.9 nM for δ agonist potency.

Noscapine-¹³C,d₃ is a ¹³C- labeled and deuterated labeled Noscapine. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier.

(±)-U-50488 ((±)-trans-(1R,2R)-U-50488) is a selective kappa opioid receptor agonist. (±)-U-50488 can improve symptoms related to status epilepticus, but has no significant effect on spontaneous seizure episodes. (±)-U-50488 can be used for research of epilepsy.

KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a K_i value of 5.3 nM for human KOR, and EC₅₀ values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research.

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 is used in anxiety disorders research.

BW443C is a selective opioid receptor agonist. BW443C has antinociceptive effect.

(rel)-RSD 921 (PD-117302) is a κ-opioid receptor agonist. (rel)-RSD 921 did not have a greater food-inducing effect in obese than in lean Zucker rats; in both obese and lean Zucker rats, lean rats were more sensitive to its initial food-inducing effect but ultimately ate less.

ADL-5747 hydrochloride is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 hydrochloride activates these receptors, thereby playing a role in pain management pathways. ADL-5747 hydrochloride can be used for research into pain management mechanisms.

(RS)-Salsolinol hydrobromide is the hydrobromide form of (±)-Salsolinol (HY-113316). (RS)-Salsolinol hydrobromide is a Dopamine (HY-B0451)-derived endogenous metabolite. (RS)-Salsolinol hydrobromide 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).

KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a K_i of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (K_i = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation.

Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a K_i of 8.6 nM in guinea pig. The K_i values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier.

BU72 is a highly potent and long-acting agonist of μ and κ opioid receptors, and also has a partial agonist effect on δ opioid receptors (EC₅₀ values are 0.054, 0.033, and 0.58 nM, respectively). BU72 has a strong and long-lasting analgesic effect, which is mainly mediated by μ opioid receptors. BU72 has a long-lasting activity and can partially reverse the analgesic effect of morphine. BU72 can be used in the study of opioid dependence.

(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997).

(+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997).

β-Endorphin, equine is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. Analgesic properties.