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Opioid receptor agonists and antagonists act on mu, delta and kappa receptors and the related nociceptin receptor. All four are G protein-coupled receptors that respond to endogenous peptides such as endorphins, enkephalins and dynorphins. Expression cloning of the delta opioid receptor in 1992 opened the family to molecular study. The nociceptin/orphanin FQ peptide (NOP) receptor, first called opioid receptor-like 1 (ORL1), was matched to its endogenous peptide agonist in 1995. Dynorphin A (1-13) Acetate is a peptide agonist at the kappa receptor, and JDTic is a kappa antagonist. SR-17018 acts as a mu agonist, while alvimopan is a peripherally acting opioid antagonist. MCOPPB trihydrochloride is a NOP agonist, and BAN ORL 24 blocks the same receptor.
Synonyms: Orphanin FQ
Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
Dynorphin A (1-8) is a potent kappa receptor ligand, playing a critical role in opioid signaling. This peptide exhibits significant binding affinity, inhibiting the binding of 3H-Bremazocine to the purified kappa receptor with an IC50 of 303 nM. It serves as a valuable tool for studying kappa opiate pharmacology and exploring its implications in pain modulation and neurobiology.
LY164929 is a highly selective ligand for opioid receptors, specifically targeting the low-affinity binding site of [3H]D-Ala2-D-Leu-5-enkephalin. It demonstrates an exceptional 1,986-fold selectivity over other opioid ligands, making it a valuable tool for studying opioid receptor function and pharmacology. This compound is ideal for research applications involving pain management, addiction studies, and the development of novel analgesics.
Fluorphine is a potent μ-opioid receptor (MOR) ligand that exhibits a binding affinity with a Ki value of 12.5 nM. This compound demonstrates biological activity by promoting GTPγS binding with an EC50 of 75 nM and facilitating β-arrestin 2 recruitment with an EC50 of 377 nM. Fluorphine is primarily used in research to investigate opioid signaling pathways and their physiological effects, including respiratory depression.
Mu Opioid Receptor Antagonist 1 is a selective and orally active ligand that targets the mu opioid receptor (MOR), exhibiting a Ki value of 0.58 nM and an EC50 of 1.15 nM. This compound effectively enhances intestinal motility in models of morphine-induced constipation. It serves as a valuable tool for research focused on opioid-induced constipation (OIC) and its related gastrointestinal effects.
2-(Di-sec-butylamino)-1-(1-(2-fluorobenzyl)-1H-pyrrol-2-yl)ethan-1-ol functions as a selective ligand for opioid receptors. This compound exhibits significant affinity and activity, making it valuable for studies on pain management and analgesic pathways. Its structural similarities to known opioids allow for exploration of the receptor interactions and potential therapeutic applications in opioid research.
CHIR 4531 is a trimer peptide that functions as a mu-opiate receptor ligand, exhibiting a binding affinity characterized by a Ki value of 6 nM. This compound is primarily utilized in research focused on pain management, addiction, and opioid signaling pathways. Its ability to selectively engage the mu-opiate receptor makes it a valuable tool for studying the biological effects of opiates in various experimental contexts.
Ortho-methyl 4-anilino-1-boc-piperidine is an opioid compound that serves as a crucial precursor in synthetic pathways for the development of opioid receptor ligands. This reagent is valuable in chemical research aimed at designing and optimizing new analgesics with potential therapeutic applications in pain management and addiction treatment. Its structural features allow for modifications that can lead to enhanced receptor selectivity and activity.
