Opioid Receptors

PL37 is a potent orally active enkephalinase inhibitor that targets both Neutral Endopeptidase and Aminopeptidase N, providing dual inhibition. This compound exhibits significant anti-hyperalgesic activity through the activation of μ-opioid receptors, demonstrating an ED50 of 13.4 mg/kg for analgesic effects in murine models. PL37 is valuable for research into the mechanisms underlying diabetic neuropathic pain and related pain management strategies.

ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation.

SB-612111 is a potent antagonist of the opiate receptor-like orphan receptor (ORL-1), exhibiting high affinity for human ORL-1 with a Ki of 0.33 nM. It demonstrates selectivity towards μ-, κ-, and δ-opioid receptors, with Ki values of 57.6 nM, 160.5 nM, and 2109 nM, respectively. SB-612111 effectively antagonizes the pronociceptive effects of nociceptin in acute pain models, making it a valuable tool for research into pain modulation and opioid receptor pathways.

Niravoline is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. This compound is notable for inducing a pure water diuresis effect while minimizing electrolyte loss. Additionally, Niravoline has demonstrated efficacy in reducing brain edema following transient forebrain ischemia in rodent models, making it a valuable tool for research in neuroprotection and fluid balance mechanisms.

M119 (NSC 119910) is a selective Gβγ-subunit inhibitor that modulates μ-opioid receptor signaling. This compound has been shown to enhance μ-opioid-dependent antinociception by inhibiting μ-receptor-dependent phospholipase (PLC) activation. M119 is useful in pain research, particularly in studies investigating opioid analgesia, as well as in the assessment of acute tolerance and dependence in animal models.

Neuropeptide AF (human) is an endogenous peptide that acts as an opioid receptor inhibitor. This neuropeptide plays a critical role in modulating pain and stress responses, making it a valuable tool for studies focused on opioid signaling pathways. Research applications include investigations into pain management, addiction, and the physiological effects of endogenous opioid peptides.

rel-SB-612111 hydrochloride is a selective antagonist of the human opiate receptor-like orphan receptor (ORL-1), exhibiting a high binding affinity with a Ki value of 0.33 nM. This compound demonstrates notable selectivity against μ-, κ-, and δ-opioid receptors, with Ki values of 57.6 nM, 160.5 nM, and 2109 nM, respectively. rel-SB-612111 hydrochloride has been shown to effectively inhibit the pronociceptive effects of Nociceptin in acute pain models, making it a valuable tool for research into pain mechanisms and opioid receptor interactions.

Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling.

MOR agonist-1 is a selective μ-opioid receptor (MOR) agonist known for its pronounced analgesic activity. This compound is valuable for research focused on pain modulation and the exploration of pain-related disorders. Its mechanism of action makes it an essential tool for studies investigating opioid pharmacology and therapeutic interventions in pain management.