mor 1

MOR modulator-1 (compound 6) is a potent and selective modulator of the μ opioid receptor (MOR). Compared to NAT (6α-configuration), MOR modulator-1 demonstrates improved opioid receptor selectivity, enhanced antagonistic effects in vivo, and overall reduced withdrawal symptoms. It connects to the μ, δ, and γ receptors with carboxamide linkers, showing Ki values of 0.25, 41.1, and 1.30 nM respectively.

Compound 114 (D3R MOR antagonist 1) exhibits dual antagonistic activity at dopamine D3 receptors (D3R) and mu-opioid receptors (MOR), with K i values of 46.5 nM and 691 nM, respectively. It offers analgesic benefits through partial agonism at MOR and may decrease the risk of opioid misuse through its D3R antagonistic properties [1].

MOR Agonist-1 is a μ-opioid receptor (MOR) agonist noted for its potent analgesic properties and is utilized in research concerning pain and associated disorders [1].

N-Methylmoranoline is an inhibitor of α-glucosidase.

HINT1-IN-1 (compound 8) is an inhibitor of histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. It influences the cross-regulation between μ-opioid receptors (MOR) and NMDA receptors (NMDAR).

Difelikefalin is a κ-opioid receptor (KOR) agonist.1It activates KOR in HEK293 cells expressing the human receptor (EC50= 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50= 0.048 nM). Difelikefalin is selective for KOR over the μ-opioid receptor (MOR; EC50= >1 μM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively). 1.Schteingart, C.D., Menzaghi, F., Jiang, G., et al.Synthetic peptide amides(2008)

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.

Difelikefalin TFA is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin TFA is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg kg, respectively).

Difelikefalin HCl is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin HCl is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg kg, respectively).

Dynorphin A TFA, an endogenous opioid peptide, plays a role in inhibitory neurotransmission within the central nervous system (CNS). It acts as a highly potent kappa opioid receptor (KOR) agonist and also stimulates other opioid receptors, including mu (MOR) and delta (DOR). Furthermore, Dynorphin A TFA has been observed to induce neuronal death, making it a significant subject in neurological disease research [1] [2].

Compound 121, a D3R MOR antagonist with K i values of 361 nM and 85.2 nM for D3R and MOR respectively, has the potential for analgesic effects through MOR partial agonism and may reduce opioid-misuse liability through D3R antagonism [1].

Compound 46, designated as MOR agonist-2, serves as a D3R antagonist and a MOR agonist with respective K i values of 7.26 nM and 564 nM. This compound holds potential for analgesic effects attributed to its partial agonism at MOR and may decrease opioid misuse liability owing to its antagonistic action at D3R [1].

MOR agonist-3 (Compound 84) is a dual D3R MOR antagonist with Ki values of 382 nM and 55.2 nM, respectively. It shows promise for analgesia via partial agonism at MORs and may mitigate opioid abuse via D3R antagonism. This compound is utilized in research pertaining to inflammation and neuropathic pain [1].

EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K i s of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity with reduced opioid-induced relevant adverse events[1].