orphanin fq

Orphanin FQ(1-11) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) displays analgesic properties in CD-1 mice.

Nociceptin (Orphanin FQ) is a 17-amino-acid polypeptide that is structurally related to the opioid peptide dynorphin A.

Orphanin FQ(1-11) TFA, a fragment of orphanin FQ or nociceptin (OFQ/N), acts as a powerful NOP receptor (ORL-1; OP4) agonist with a K i of 55 nM. It lacks affinity for μ, δ, κ1, and κ3 receptors (K i >1000 nM), demonstrating specificity, and exhibits analgesic properties in CD-1 mice [1] [2].

Orphanin FQ(1-11) acetate(178249-41-7 free base) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) acetate(178249-41-7 free base) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) acetate(178249-41-7 free base) displays analgesic properties in CD-1 mice.

SCH-486757 is an agonist of nociceptin-1 (NOP1) and orphanin FQ peptide receptors and is used in the study of cough.

AT-090 is an innovative and highly selective agonist for nociceptin/orphanin FQ peptide receptors (NOP receptors).

NOP antagonist 1 (Compound (-)-31) is an antagonist of the nociceptin/orphanin FQ peptide receptor (NOP) with a Kb value of 8.65 nM. It is applicable in research related to neuropsychiatric disorders.

Sunobinop (S 117957) TFA is an orally active and blood-brain barrier-penetrating selective partial agonist of the human nociceptin/orphanin FQ peptide receptor (NOP), with high affinity for human targets (Ki=3.3 nM; EC50=4.03 nM; Emax=47.8%), without activating μ and κ opioid receptors. In rats, Sunobinop TFA significantly reduces wakefulness and increases non-rapid eye movement (NREM) sleep through NOP receptor activation, without significant side effects on learning, memory, reward, respiration, or intestinal function at effective doses. It also displays competitive antagonist properties in certain signaling pathways [such as β-Arrestin 2 recruitment]. Sunobinop TFA can be employed in research involving insomnia, moderate to severe alcohol use disorder, and incontinence due to bladder overactivity.

(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist (K(i): cloned human ORL1=1.8 nM). J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ [1].

nociceptin/orphanin FQ (NOP) receptor antagonist

BU08028 is a mu opioid peptide (MOP) receptor and nociceptin-orphanin FQ peptide (NOP) receptor agonist.

Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activation and competitively blocks the stimulation of [35S]-GTPγS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in rat brain membranes and sections [1].

[Nphe1]Nociceptin(1-13)NH2 is a novel endogenous ligand for the nociceptin/orphanin FQ (NC) receptor, acting as a selective and competitive antagonist without any agonist effects. It binds specifically to recombinant nociceptin receptors with high affinity (pKi=8.4) and effectively blocks nociceptin's ability to inhibit cyclic AMP accumulation in CHO cells (pA2=6.0), showcasing potential as an analgesic agent.

Nocistatin, an endogenous neuropeptide, serves as a ligand for the orphan opioid receptor-like receptor and functionally antagonizes the neuropeptide nociceptin/orphanin FQ (Noc/OFQ). It inhibits 5-HT release through a G i/o protein-mediated pathway and blocks nociceptin-induced allodynia and hyperalgesia [1] [2].

Highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80). Displays > 8000-fold selectivity over δ, κ, and μ opioid receptors and has relatively long lasting pronociceptive, hypotensive, negative inotrop

Ac-RYYRIK-NH2 acetate is an agonist at nociceptin/orphanin FQ(noc/OFQ) receptors, affecting spontaneous locomotor activity. Ac-RYYRIK-NH2 acetate is a partial agonist on ORL1 transfected in CHO cells, antagonizes the stimulation of [35S]-GTPgammaS binding to G proteins by noc/OFQ in membranes and sections of rat brain.

(S)-MCOPPB is the S-enantiomer of MCOPPB, an orally active selective agonist for the Nociceptin/Orphanin FQ-Receptor. It inhibits signal transduction in mouse brain NOP receptors and is utilized in anxiety disorder research.