Neuropeptide FF Receptor

RF9 is a potent and selective Neuropeptide FF receptor antagonist, with Kis of 58??5 and 75??9 nM for hNPFF1R and hNPFF2R, respectively.

RFRP-3 (Neuropeptide VF(124-131))(human), a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM.

BIBP3226 is a selective antagonist of the neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptors, exhibiting K_i values of 1.1 nM, 79 nM, and 108 nM for rat NPY Y1, human NPFF2, and rat NPFF, respectively. This compound has demonstrated anxiogenic-like effects, making it a valuable tool for research in neuropharmacology, particularly in studies exploring anxiety-related disorders and the modulation of neuropeptide signaling pathways.

Neuropeptide SF (mouse, rat) is a potent agonist of the neuropeptide FF receptors, exhibiting Ki values of 48.4 nM for NPFF1 and 12.1 nM for NPFF2. This compound enhances the sustained current of heterologously expressed acid-sensing ion channel 3 (ASIC3), making it a valuable tool in studies related to pain modulation and neuropeptide signaling. Neuropeptide SF is ideal for research investigating neurophysiological processes and receptor interactions within neural pathways.

Neuropeptide AF (cattle) is an amidated octadecapeptide that targets RFamide neuropeptide receptors. It serves as a ligand for Mas-related gene receptor A4 (MrgprA4) with an EC50 of approximately 60 nM and MrgprC11 with an EC50 around 300 nM. Additionally, it activates the G protein-coupled receptors NPFF1 and NPFF2, exhibiting EC50 values ranging from 25-325 nM and 1-5 nM, respectively. Neuropeptide AF (cattle) demonstrates anti-opiate properties and plays a significant role in pain modulation research applications.

CPN-351 is a selective antagonist of the human neuropeptide FF receptor 1 (NMUR1), exhibiting a pA2 of 7.35. Its antagonistic potency towards NMUR1 is significantly greater than its effect on NMUR2, being approximately ten times more effective. CPN-351 is a valuable tool for investigating inflammatory processes and the role of neuropeptide signaling in various biological systems.

Neuropeptide FF (NPFF) functions as an agonist for the NPFF1 and NPFF2 receptors, exhibiting Ki values of 2.82 nM and 0.21 nM, respectively. This octapeptide plays a crucial role in mediating various physiological processes, including the modulation of pain, opioids, autonomic function, and neuroendocrine responses. It is involved in the regulation of memory and the control of food and water intake, while also demonstrating significant antiopioid and analgesic properties. Neuropeptide FF is particularly relevant for research into opioid tolerance, morphine-induced analgesia, abstinence syndrome, and pain-related conditions, including inflammatory and neuropathic pain.

AC-263093 free base is an activator of the neuropeptide FF receptor 2 (NPFFR2), exerting functional activation while inhibiting NPFF receptor 1 (NPFFR1), with pKi values of 6.9 and 7.0, respectively. This compound holds potential in the investigation of mechanisms to reverse opioid tolerance, making it valuable for research related to pain management and neuropharmacology.

NPFF1-R antagonist 1 is a potent antagonist of the neuropeptide FF (NPFF) receptor, specifically targeting the NPFF1-R subtype. This compound, a piperidine analogue, demonstrates a selective blockade with a Ki of 211 nM for NPFF1-R and 3270 nM for NPFF2-R, indicating a remarkable 15-fold selectivity. It is suitable for research applications exploring neuropeptide signaling pathways and potential neurological disorders linked to NPFF receptor activity.

AC-099 hydrochloride is a selective full agonist of the neuropeptide FF receptor 2 (NPFF2R) with an EC50 of 1189 nM, and a partial agonist of NPFF1R with an EC50 of 2370 nM. This compound has demonstrated the ability to attenuate hypersensitivity induced by spinal nerve ligation in rat models. AC-099 hydrochloride is valuable for research focusing on pain modulation and the neuropeptide signaling pathways associated with nociception.

Neuropeptide FF (5-8) is a derivative of Neuropeptide FF that acts as a potent antagonist of NPFF-related receptors. This peptide, with the sequence Q-P-Q-R-F-NH2, exhibits a Ki value of 20.9 nM, indicating its strong binding affinity. It is primarily used in research to study pain modulation, stress responses, and neuroendocrine functions in various biological models.

DP32 is a bifunctional compound that serves as an antagonist of the neuropeptide FF receptor (NPFFR) while simultaneously acting as an agonist at the mu-opioid receptor (MOP). This unique dual activity makes DP32 a valuable tool in analgesia-related research, offering insights into pain modulation pathways and potential therapeutic applications in pain management. Researchers can utilize DP32 to explore the interplay between opioid signaling and neuropeptide regulation in various biological contexts.

NPFFR2 modulator-1 is a selective modulator of the neuropeptide FF receptor 2 (NPFFR2). This compound influences various signaling pathways associated with pain modulation and may provide insights into neuroinflammatory responses. It is valuable for researchers investigating neuropeptide interactions and their roles in pain perception and related disorders.

AC-099 is a selective agonist for the neuropeptide FF receptor 2 (NPFF2R) with an EC50 of 1189 nM and a partial agonist for NPFF1R, exhibiting an EC50 of 2370 nM. This compound demonstrates significant potential in modulating pain responses, as evidenced by its ability to attenuate spinal nerve ligation-induced hypersensitivity in rat models. AC-099 serves as a valuable tool in pain research and for exploring the roles of NPFF receptors in the central nervous system.

BIBP3226 TFA is a potent and selective antagonist of the neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptors. It exhibits inhibition constants (Kis) of 1.1 nM, 79 nM, and 108 nM for the rat NPY Y1, human NPFF2, and rat NPFF receptors, respectively. BIBP3226 TFA is utilized in research focused on anxiety and neuropeptide signaling pathways, providing valuable insights into the role of these receptors in various biological processes.

RFRP-1 (human) is a potent Neuropeptide FF (NPFF) receptor agonist that targets human gonadotropin-releasing hormone (GnRH) neurons and gonadotropes, effectively inhibiting gonadotropin release. This compound demonstrates high affinity for the NPFF receptors, with EC50 values of 0.0011 nM for NPFF2 and 29 nM for NPFF1. RFRP-1 (human) is valuable in research applications related to hormonal regulation and neuroendocrine signaling.