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.

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.

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.

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.

DPDPE TFA 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.

μ/κ/δopioid receptor agonist1 is an agonist for the μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR). It produces potent and long-lasting analgesic effects in the tail flick test through peripheral MOR and KOR activation.

ZT 52656A is a selective agonist of kappa opioid, and used for the prevention or alleviation of pain in the eye.

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

Apitegromab (SRK-015) is a new myostatin inhibitor, an antibody targeting myostatin precursor, which can be used to study neuromuscular diseases including spinal muscular atrophy.