Opioid Receptors

Cat. No.

A62381

CAS No.

425623-55-8

(-)-9-Hydroxycorynantheidine

Synonyms: 9-O-Desmethyl mitragynine

(-)-9-Hydroxycorynantheidine is a selective partial agonist of the μ-opioid receptor. It exhibits significant biological activity by inhibiting electrically stimulated twitch contractions in the guinea-pig ileum, making it relevant for research into opioid receptor function and pharmacology. This compound is useful for studies assessing the effects of μ-opioid receptor modulation in various biological contexts.

Cat. No.

A62391

CAS No.

83471-50-5

α-Casein (90-95)

α-Casein (90-95) is a partial agonist of opioid receptors, exhibiting significant biological activity through its effects on mast cells and prostate cancer cells. It inhibits the secretion of β-hexosaminidase from rat peritoneal mast cells with an IC50 of 0.1 μM and demonstrates antiproliferative effects on LNCaP, DU145, and PC3 prostate cancer cells with IC50 values of 0.94 nM, 137 nM, and 6.92 nM, respectively. This reagent activates Gi-like proteins via a receptor-independent mechanism and promotes intracellular calcium release. α-Casein (90-95) is valuable for investigating mechanisms underlying allergic diseases and prostate cancer.

Cat. No.

A62411

CAS No.

1126793-40-5

Sunobinop

Synonyms: S 117957; IMB 115

Sunobinop is a selective partial agonist of the human nociceptin/orphanin FQ receptor (NOP), exhibiting high affinity for human targets (Ki=3.3 nM; EC50=4.03 nM; Emax=47.8%) while not engaging μ or κ opioid receptors. This compound significantly reduces wakefulness and enhances non-rapid eye movement sleep in rodent models, demonstrating a favorable side effect profile with no notable impacts on learning, memory, respiration, or intestinal function. Sunobinop also acts as a competitive antagonist in certain signaling pathways, particularly β-arrestin 2 recruitment, making it a valuable tool for research into conditions such as insomnia, alcohol use disorder, and overactive bladder-induced urinary incontinence.

Cat. No.

A62426

CAS No.

2445895-33-8

SalA-VS-07

SalA-VS-07 is a G protein-biased partial agonist specifically targeting the kappa-opioid receptor (KOR). It demonstrates significant analgesic properties and is utilized in research exploring pain management and various related disorders. This compound serves as a valuable tool for studies investigating the therapeutic potentials of KOR modulation.

Cat. No.

A62461

CAS No.

709024-69-1

SR14150

SR14150 is a partial agonist of the nociceptin/orphanin FQ peptide (NOP) receptor, exhibiting high affinity. This compound demonstrates significant analgesic properties, potentially facilitating the advancement of novel multi-target opioids aimed at enhancing pain relief while minimizing adverse effects. Additionally, SR14150's interaction with various opioid receptors may offer innovative therapeutic strategies for chronic pain management.

Cat. No.

A62463

CAS No.

200959-47-3

Ac-RYYRWK-NH2

Ac-RYYRWK-NH2 is a selective partial agonist for the nociceptin receptor (NOP). This compound demonstrates high binding affinity to rat cortical membranes with a Kd value of 0.071 nM, while showing no significant affinity for µ-, κ-, or δ-opioid receptors. Ac-RYYRWK-NH2 is useful for studying nociceptin signaling pathways and exploring potential therapeutic applications in pain management and neurobiology.

Cat. No.

A62466

CAS No.

143257-97-0

Sameridine

Synonyms: NIH 10908 free base

Sameridine is a weak partial agonist of the μ-opioid receptor, primarily utilized in analgesic applications. Exhibiting local anesthetic and analgesic properties, Sameridine provides a unique profile with minimal respiratory depression at low doses, though higher doses may suppress ventilatory response. This compound is valuable for research focused on exploring analgesic effects and opioid receptor pharmacology.

Cat. No.

A62534

CAS No.

200959-48-4

Ac-RYYRIK-NH2

Ac-RYYRIK-NH2 serves as a potent partial agonist of the ORL1 receptor, exhibiting a dissociation constant (Kd) of 1.5 nM in CHO cell models. This compound mimics the action of endogenous ligands, facilitating research into ORL1-related pathways. Additionally, it acts as a specific antagonist for G protein activation, competitively inhibiting [35S]-GTPgS binding stimulated by nociceptin/orphanin FQ in rat brain membranes and sections. Applications include studies of pain modulation, neuropharmacology, and the underlying mechanisms of ORL1 receptor signaling.

Cat. No.

A62547

CAS No.

383123-18-0

ZP 120C

ZP 120C is a potent partial agonist of the ORL1 receptor. It effectively inhibits electrically induced contractions, making it valuable for studies related to neuromodulation. This compound is particularly useful in research investigating hyponatremia and hypokalemia.

Cat. No.

A62554

CAS No.

857262-16-9

SR-16434

Synonyms: SR-16435 free base

SR-16434 is a partial agonist of the nociceptin/orphanin FQ (NOP) and μ-opioid receptors, exhibiting high binding affinity with Ki values of 7.49 for the NOP receptor and 2.70 for the μ-opioid receptor. This compound demonstrates significant analgesic properties, making it a valuable tool for studying pain mechanisms and developing new pain management strategies. Its dual receptor activity provides insights into the interplay between nociceptive and opioid signaling pathways in research applications.

Cat. No.

A62578

CAS No.

408305-09-9

Ac-RYYRWK-NH2 TFA

Ac-RYYRWK-NH2 TFA serves as a potent and selective partial agonist for the nociceptin receptor (NOP). It exhibits significant binding affinity, with a Kd of 0.071 nM for rat cortical membranes (ORL1), while demonstrating no affinity for μ-, κ-, or δ-opioid receptors. This compound is valuable for research investigating nociceptin signaling pathways and their implications in pain modulation and various neurological disorders.

Cat. No.

A62667

CAS No.

2099680-72-3

AT-127

AT-127 is a partial agonist of the nociceptin/orphanin FQ peptide (NOP) receptor, promoting NOP/G-protein interactions in a concentration-dependent manner. Its biological activity indicates potential applications in pain modulation and neuropharmacology research. This compound serves as a valuable tool for investigating the role of NOP receptors in various physiological and pathological processes.

Cat. No.

A62697

CAS No.

2099681-43-1

NOP agonist-1

NOP Agonist-1 is a partial agonist for the nociceptin opioid receptor (NOP). This compound has demonstrated the ability to attenuate parkinsonian disabilities in 6-OHDA hemilesioned rat models. Its applications in research may provide insights into the therapeutic potential of NOP modulation in movement disorders and pain management.

Cat. No.

A62700

CAS No.

23407-35-4

Corynantheidine

Synonyms: (-)-Corynantheidine

Corynantheidine is a mu-opioid receptor (MOR) partial agonist, demonstrating analgesic effects through MOR activation in preclinical models. This compound is primarily utilized in research focused on pain management and the exploration of opioid receptor activity. Its ability to modulate pain responses makes it a valuable tool for studying the mechanisms underlying analgesia and opioid signaling.