δ Opioid Receptor/DOR Agonist

SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a K_i of 1.78 nM and an IC₅₀ of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC₅₀ of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.

DPDPE, an opioid peptide, is a selective δ-opioid receptor?(DOR) agonist?with anticonvulsant effects.

KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC₅₀ of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus.

ADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an K_i and an EC₅₀ value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitory activity to hERG channel with an IC₅₀ value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain.

[Met5]-Enkephalin, amide TFA is an agonist for δ opioid receptors as well as putative ζ (zeta) opioid receptors.

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.

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 (ADL 2-1294) is selective and orally active μ opioid receptor agonist with K_i valuess of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide produces antinociception and antihyperalgesia. Loperamide exhibits peripheral selectivity, enhancing fluid, electrolyte, and glucose absorption, reversing PGE₂ (HY-101952)- and Cholera toxin (HY-P1446)-induced intestinal secretion, and reducing intestinal motility. Loperamide can be used for the researches of inflammatory pain and protracted diarrhoea.

[D-Ala2]leucine-enkephalin, a delta opioid agonist, is a degradation resistant long-acting Leu-enkephalin analog used to study the signaling pathway of delta opioid receptors.

KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist (K_i = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases.

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

DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects.

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

Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin (HY-A0276A)-induced kidney injury. Dalargin shows antiulcer activity.

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

TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a K_i value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke.

NAQ is a potent and selective μ opioid receptor partial agonist, with a K_i of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (K_i=132.50 nM) and the κ receptor (K_i=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence.