δ-opioid

Asimadoline (EMD-61753) is a proprietary small molecule therapeutic, originally discovered by Merck KGaA of Darmstadt, Germany. Asimadoline was originally developed to treat peripheral pain such as arthritis. Asimadoline is an orally administered agent that acts as a kappa opioid receptor agonist. It has shown encouraging clinical efficacy for the treatment of IBS in a barostat study in IBS patients and has the potential for treating other gastrointestinal diseases.

Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.

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

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.

Dermorphin is agonist of μ-opioid receptor (MOR) agonist.

Dermorphin TFA is a new class of opioids-like peptides

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

ADL-5747 (ADL-5747 (free base)) (free base) is a delta opioid receptor agonist used in the treatment of neurological disorders, skin and musculoskeletal disorders, and may be used in the study of postherpetic neuralgia, knee osteoarthritis and pain.

Samidorphan HCl is an orally active and highly potent modulator of the opioid system that binds to μ‐opioid, κ‐opioid, and delta-opioid receptors. Samidorphan HCl is a novel μ-opioid receptor antagonist, a partial agonist for k-opioid and delta-opioid receptors. Samidorphan HCl can be used to prevent and treat schizophrenia.

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.

Trimebutine maleate (Polibutin) is a weak mu-opioid agonist and has antimuscarinic effects. Trimebutine is an agonist of peripheral mu, delta, and kappa opiate receptors served as a spasmolytic drug for therapy of both chronic and acute abdominal pain.

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

[Leu5]-Enkephalin TFA(58822-25-6(free bas)) (Leucyl-enkephalin) is the most potent δ-receptor ago

Alvimopan (LY 246736) is a synthetic trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opioid-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.

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.

Tonazocine, a non-peptide compound, primarily functions as a partial δ-opioid receptor agonist, with additional properties of a μ-receptor antagonist and weak κ-receptor agonist activity.

Oxymorphindole is a δ-opioid receptor agonist.

Norbuprenorphine, the primary active metabolite of buprenorphine, is a potent agonist of the μ, δ, and κ opioid receptors. It is the only known active metabolite of buprenorphine.

Norbuprenorphine HCl is a primary active metabolite of buprenorphine, serving as an effective agonist for the μ, δ, and κ opioid receptors.

10-keto Naltrexone is an antagonist of the μ-, κ-, and δ-opioid receptors, exhibiting inhibition constants (Kis) of 31.1, 102, and 281 nM, respectively, at guinea pig receptors.