δ-opioid receptor

JNJ-20788560 is a delta opioid receptor (DOR) agonist with analgesic activity. It is more selective for DOR than for mu opioid receptors (MOR).

SNC 80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist, Ki = 1.78 nM, IC50 = 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.

Loperamide hydrochloride (ADL 2-1294) is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.

ML-335 is a μ-δ isomer-targeted agonist, a μOR-δOR-biased ligand that can serve as a scaffold for the development of unique types of (isomer-biased) drugs.ML-335 is a MOR (μ-opioid receptor)/DOR (δ-opioid receptor) heterodimer, with anti-injury sensory activity and pain inhibitory activity.

β-Endorphin (1-27) (human) acetate, existing in the hypophysis cerebri and hypothalamus, exhibits antinociception activity. β-Endorphin (1-27) (human) acetate is an agonist of opioid receptor, showing preferred affinity for μ-opioid receptor and δ-opioid

BTRX-335140 (CYM-53093) is a potent and selective orally active κ-opioid receptor (KOR) antagonist with antagonistic activity against κOR, μOR, and δOR with IC50 values of 0.8, 110, and 6500 nM, respectively.

DPI-3290 is a specific agonist of opioid receptors (Ki: 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively) with potent antinociceptive activity. DPI-3290 is one of a series of novel centrally acting agents.

Deltorphin acetate is a substance obtained from the skin secretions of a frog, Phyllomedusa bicolor and shows high selectivity and affinity for δ-opioid receptor.

Leuphasyl TFA is an amid peptide, a δ-opioid receptor agonist, is a degradation resistant long-acting Leu-enkephalin analog used to study the signaling pathway of delta opioid receptors. Leuphasyl TFA is a potent, long-acting Leu-enkephalin analog that is resistant to enzymatic degradation

(D-Ser2)-Leu-Enkephalin-Thr is a delta selective agent of opioid receptor and shows analgesic effects.

IPAG is a potent σ-receptor antagonist (pKi=4.3). IPAG can induce cell apoptosis.

EST73502 is an agonist of μ-opioid receptor(Ki = 64 nM) agonist and an antagonist of σ1 receptor (Ki = 118 nM). EST73502 displays antinociceptive activity.

AR-M 1000390 hydrochloride (ARM-390 HCl) , also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic response; reduces CFA-induced hyperalgesia. Brain penetrant following systemic administration.

N-Desmethylclozapine (Desmethylclozapine) is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors.

ADL-5859 (ADL5859 Hydrochloride) is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.

[Leu5]-Enkephalin acetate(58822-25-6 free base) is an endogenous neuropeptide involved in nociception and an agonist of δ-opioid and μ-opioid receptors (Kis = 4.0 and 3.4 nM, respectively)

Deltorphin I is an agonist of δ-opioid receptor.

Deltorphin 2 ([D-Ala2]-Deltorphin II) is an agonist of δ opioid receptor with an IC50 of 1 nM.

BMS986187 is a novel Potent and Selective Positive Allosteric Modulators of the delta-Opioid Receptor.

BMS986188 is a novel Potent and Selective Positive Allosteric Modulator of the delta-Opioid Receptor.

[D-Ala2]leucine-enkephalin acetate ([D-Ala2]leucine-enkephalin acetate (64963-01-5 free base)) is a delta opioid agonist used to study the signaling pathway of delta opioid receptors.

Gluten exorphin C is an opioid peptide derived from wheat gluten, with IC50 values of 40 μM for μ opioid and 13.5 μM for δ opioid activities in the GPI and MVD assays, respectively. Isolated from the pepsin-trypsin-chymotrypsin digest of wheat gluten, it is considered a δ-opioid receptor-selective ligand.

BW-180C (DADLE) is a prototypical δ-opioid receptor agonist that also displays activity at the μ-opioid receptor. Displays antinociceptive activity in vivo.

DPDPE is selective δ-opioid receptor agonist peptide. Inhibits electrically stimulated contraction of mouse vas deferens in vitro (EC50 = 5.2 nM), and is antinociceptive in vivo.