Catalog No.
Product Name
Application
Product Information
Citations
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NPY Y2Antagonist
NPY Y2 Antagonist 2 is a selective inhibitor of the neuropeptide Y receptor Y2, exhibiting pKi values of 6.8 nM and 7.2 nM in human and rat brain tissues, respectively. This compound effectively blocks the NPY Y2-mediated negative feedback, leading to increased endogenous NPY release and enhanced activation of Y1 receptors. Its ability to penetrate the blood-brain barrier, along with moderate in vivo clearance and a favorable brain/plasma ratio, makes NPY Y2 Antagonist 2 a valuable tool for investigating mood disorders, alcohol withdrawal-related anxiety, and social anxiety linked to nicotine withdrawal. -
Neuropeptide FF Receptor Agonist
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. -
NPY5 Receptor Antagonist
SCH 430765 is a potent and selective antagonist of the neuropeptide Y5 (NPY5) receptor. This compound plays a significant role in modulating appetite and energy homeostasis, making it valuable for research into obesity and related metabolic disorders. Its ability to inhibit NPY5 receptor activity provides insights into potential therapeutic strategies for weight management and obesity-related conditions. -
NPY Y2 Antagonist
NPY Y2 Antagonist 1 is a selective antagonist of the neuropeptide Y receptor Y2 (NPY Y2), primarily functioning through competitive inhibition. This compound exhibits significant biological activity in modulating neuropeptide Y signaling pathways, making it invaluable for research focused on neurobiology and related therapeutic areas. Its application extends to studying the physiological roles of NPY receptors in various biological processes and potential implications in metabolic disorders and appetite regulation. -
Neurotensin Receptor Activator
[Lys8, Lys9]-Neurotensin (8-13) is a neurotensin analog that primarily activates the G protein-coupled receptors NTS1 and NTS2. This compound demonstrates potent analgesic activity, with binding affinities (Ki values) of 0.33 nM and 0.95 nM for the human NTS1 and NTS2 receptors, respectively. It is utilized in research applications investigating pain modulation and neuropeptide signaling pathways. -
Neurotensin Receptor Agonist
JMV 449 acetate is a highly potent agonist of the neurotensin receptor. It demonstrates an IC50 of 0.15 nM in inhibiting 125I-neurotensin binding to neonatal mouse brain tissue and an EC50 of 1.9 nM in inducing contractions in the guinea-pig ileum. Additionally, JMV 449 acetate exhibits significant, long-lasting hypothermic and analgesic effects in mouse models, making it valuable for research in pain management and neuropharmacology. -
Neurotensin Octapeptide
Xenopsin is a neurotensin-like octapeptide derived from the skin of Xenopus laevis. It primarily functions as an inhibitor of Tetragastrin-stimulated gastric acid secretion, making it valuable for studies related to gastrointestinal physiology and acid regulation. Research applications include investigations into peptide signaling pathways and gastrointestinal disorders. -
Neurotensin Analog
Acetyl neurotensin (8-13) is a neurotensin analog that retains full binding affinity and pharmacological activity. This compound is primarily utilized in research exploring neurotensin receptor interactions and their implications in various physiological processes. Its use may aid in the investigation of neuroinflammatory conditions, pain modulation, and appetite regulation. -
Neurotensin Receptor Inhibitor
VGD071 is a neurotensin receptor inhibitor that specifically targets sortilin. This compound exhibits potential for modulating neurotensin signaling pathways, which may be relevant in the context of breast cancer research. VGD071 is suitable for preclinical studies and investigations into the role of neurotensin receptors in tumorigenesis and cancer progression. -
Neurotensin Receptor Modulator
[D-Trp11]-Neurotensin is a neurotensin receptor modulator that acts as a selective antagonist in perfused rat hearts while exhibiting full agonistic activity in guinea pig atria and rat stomach strips. This compound has demonstrated the ability to inhibit neurotensin-induced hypotension, making it a valuable tool for studying neurotensin receptor dynamics and their physiological effects. Its diverse biological activity supports various research applications, including cardiovascular and gastrointestinal studies. -
Neurotensin Receptor Agonist
Neurotensin(8-13) TFA is an active fragment of the neuropeptide neurotensin, specifically acting as an agonist of neurotensin receptors. This compound has been shown to decrease the density of cell-surface NT1 receptors (NTR1), impacting various signaling pathways. It is useful in research applications focused on neurobiology, pharmacology, and the study of neurotensin-related pathways in health and disease. -
Neurotensin Receptor Agonist
Contulakin G is an O-glycosylated neurotensin analog that functions as an agonist of the neurotensin receptor. This compound exhibits notable antinociceptive properties, making it valuable in pain modulation research. Its unique characteristics allow for exploration in neurobiology and potential therapeutic applications targeting pain relief mechanisms. -
Neurotensin Receptor
SR 142948-C3-NHMe is a selective antagonist of the neurotensin receptor. This compound has demonstrated significant inhibitory activity against neurotensin signaling pathways, making it a valuable tool for studying neurotensin-related physiological processes. It is applicable in research focused on neuropharmacology, pain modulation, and various CNS disorders, providing insight into neurotensin's role in these conditions. -
Neurotensin Receptor Agonist
JMV 449 is a potent neurotensin receptor agonist, demonstrating an IC50 of 0.15 nM for the inhibition of [125I]-neurotensin binding in neonatal mouse brain assays. Additionally, it shows an EC50 of 1.9 nM in inducing contractions in the guinea pig ileum. JMV 449 exhibits significant hypothermic and analgesic effects in murine models, making it a valuable tool for research in pain management and neuropharmacology. -
Neurotensin Inhibitor
L-156903 is a potent neurotensin inhibitor that selectively disrupts the binding of neurotensin to brain tissue. This compound is valuable for studying the neurotensinergic system and its role in various neurological conditions. Its inhibitory action can contribute to research aimed at understanding the mechanisms underlying neuropsychiatric disorders and potential therapeutic interventions. -
Opioid Receptor Agonist
CCI-1008 is an opioid receptor agonist that exhibits significant activity in targeting the µ-opioid receptor. It is primarily utilized in research related to nervous system diseases, exploring mechanisms of pain modulation and addiction. This compound serves as a valuable tool for investigating therapeutic strategies aimed at managing pain and opioid-related disorders. -
κ Opioid Receptor Antagonist
Norbinaltorphimine dihydrochloride selectively antagonizes the κ-opioid receptor, making it an important tool for research on opioid signaling pathways. Its potent inhibitory action allows for the investigation of κ-opioid receptor-related biological processes and potential therapeutic applications in pain management and addiction studies. Researchers can utilize this compound to explore the effects of opioid receptor modulation in various experimental settings. -
Opioid receptor Antagonist
Naloxone is an antagonist of opioid receptors, primarily acting to reverse the effects of opioid overdose. It effectively alleviates respiratory depression caused by opioid toxicity, restoring normal breathing. Research applications include studies on opioid overdose treatment, respiratory pharmacodynamics, and the examination of opioid receptor interactions. Naloxone may also induce pulmonary edema and cardiac arrhythmias as potential side effects. -
Opioid Receptor Antagonist
Naltrexone is a long-acting antagonist of opioid receptors, including μ, κ, and δ subtypes. It effectively blocks the euphoric effects of exogenous opioids and diminishes alcohol cravings by antagonizing these receptors. Clinically, low doses of Naltrexone are utilized for chronic pain management, the treatment of inflammatory conditions, and potentially inhibiting tumor growth. Additionally, it is employed to alleviate intractable pruritus associated with psoriasis and atopic dermatitis, while its combination with Bupropion may contribute to reduced food cravings and body weight management. -
δ-opioid Receptor Agonist
SNC80 is a highly selective and potent non-peptide δ-opioid receptor agonist, demonstrating a Ki of 1.78 nM and an IC50 of 2.73 nM. This compound selectively activates the μ-δ heteromer in HEK293 cells, exhibiting an EC50 of 52.8 nM. SNC80 is characterized by its antinociceptive, antihyperalgesic, and antidepressant-like activities, making it a valuable tool for research in the treatment of various headache disorders. -
DOR Agonist
DPDPE is a selective δ-opioid receptor (DOR) agonist known for its anticonvulsant properties. This opioid peptide is utilized in research to explore its potential therapeutic effects in pain management and seizure disorders. Its specificity for DORs makes DPDPE a valuable tool for investigating opioid receptor signaling pathways and their implications in neurological studies. -
μ-Opioid Receptor Agonist
Endomorphin 1 is a selective agonist of the μ-opioid receptor, exhibiting a high affinity with a Ki value of 1.11 nM. It also shows moderate affinities for kappa3 binding sites, with Ki values ranging from 20 to 30 nM. This compound is known for its antinociceptive properties, making it relevant for research focused on pain modulation and opioid receptor signaling pathways. -
μ-opioid Receptor Antagonist
Naldemedine tosylate is a selective μ-opioid receptor antagonist, classified as a peripherally acting mu-opioid receptor antagonist (PAMORA). It exhibits high binding affinities for human μ-, δ-, and κ-opioid receptors, making it a valuable reagent for studying opioid-related pathways. Its primary application includes research on opioid-induced constipation (OIC). Additionally, Naldemedine tosylate has the potential to interact with the 3CLpro protease encoded by the SARS-CoV2 genome, suggesting further avenues for investigation in viral studies. -
Kappa-opioid Receptor Antagonist
Nor-Binaltorphimine is a selective antagonist of the kappa-opioid receptor, known for its role in modulating nociception and mood regulation. This compound exhibits prolonged effects in vivo, making it a valuable tool in research related to pain management, addiction, and psychiatric disorders. Its specificity for kappa-opioid receptors supports studies focused on understanding their physiological and pathological roles. -
KOR Agonist
(-)-U-50488 hydrochloride is a selective agonist of the kappa-opioid receptor (KOR), exhibiting a binding affinity (Kd) of 2.2 nM, significantly higher than its affinity for the μ-opioid receptor (MOR) at 430 nM. This compound serves as a more active enantiomer compared to its (+) counterpart and the racemic mixture. In research applications, (-)-U-50488 hydrochloride demonstrates potent and sustained anti-HIV activity in infected blood monocyte-derived macrophages (MDM), making it a valuable tool for studying kappa-opioid receptor functions and their therapeutic potential in HIV-related research. -
µ-Opioid Receptor Positive Allosteric Modulator
BMS-986122 is a selective positive allosteric modulator of the mu-opioid receptor (µ-OR) that enhances the activity of orthosteric agonists. This compound effectively increases β-arrestin recruitment, inhibits adenylyl cyclase, and activates G protein signaling pathways. BMS-986122 demonstrates the ability to potentiate DAMGO-mediated [35S]GTPγS binding in mouse brain membranes, making it a valuable tool for research in pain management and opioid pharmacology. -
Opioid Receptor Agonist
BW-180C, a δ opioid receptor (DOR) agonist, is a member of the enkephalin family. This compound exhibits neuroprotective properties and reversibly inhibits cellular transcription in neurons while preserving cell integrity. BW-180C is valuable for research applications focused on neuroprotection and opioid receptor signaling. -
Kappa Receptor Ligand
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. -
Opioid Receptor Antagonist
Naloxone methiodide is a peripherally restricted, nonselective competitive antagonist of opioid receptors. Its lack of ability to penetrate the blood-brain barrier allows for targeted effects in peripheral tissues. This compound is primarily used in research applications investigating opioid receptor activity and the modulation of peripheral opioid effects, making it valuable for studying pain management and opioid-related responses. -
ORL1 Receptor Antagonist
(±)-J-113397 is a selective non-peptidyl antagonist of the ORL1 receptor, exhibiting a Ki value of 1.8 nM for cloned human ORL1. It effectively inhibits nociceptin/orphanin FQ-stimulated GTPγS binding in CHO cells expressing ORL1, with an IC50 of 5.3 nM. This compound is valuable for investigating the physiological roles and functions of the nociceptin/orphanin FQ system in various biological contexts. -
δ-opioid Receptor Agonist
SNC162 is a potent δ-opioid receptor agonist with an IC50 of 0.94 nM. This compound demonstrates significant antidepressant-like and antinociceptive properties, making it a valuable tool in the investigation of pain management and mood disorders. Its efficacy in modulating δ-opioid receptor activity supports research into therapeutic applications for treatment-resistant depression and chronic pain syndromes. -
KOR Agonist
(±)-U-50488 hydrochloride is a selective agonist of the κ opioid receptor (KOR). It exhibits significant analgesic and anti-inflammatory properties, making it valuable for studies related to pain management and opioid receptor signaling pathways. This compound is ideal for research applications investigating the role of KOR in various physiological processes and potential therapeutic interventions. -
δ-opioid Receptor Antagonist
TAN-452 is a selective, orally active δ-opioid receptor antagonist, exhibiting a Ki of 0.47 nM and a Kb of 0.21 nM. This reagent also shows antagonistic properties toward μ-opioid receptors, with a Ki of 36.56 nM, and κ-opioid receptors, with a Ki of 5.31 nM. TAN-452 is designed to attenuate morphine-induced side effects while maintaining analgesic efficacy, making it valuable for research in pain management and opioid-related studies. Its low brain penetrability further supports peripheral applications, minimizing central nervous system interactions. -
MOR Activator
(±)-Salsolinol hydrochloride is a potent μ-opioid receptor (MOR) activator derived from dopamine. This compound modulates neuronal activity by reducing GABAergic transmission and enhancing the excitability of dopamine neurons. Its effects on neuronal firing rates in the posterior ventral tegmental area (pVTA) make it valuable for research applications focused on opioid signaling and dopamine-related pathways. -
Morphine (μ) Receptor Agonist
Morphiceptin is a potent and selective agonist for the morphine (μ) receptors, exhibiting significant morphine-like activity. This synthetic peptide, derived from a fragment of the milk protein β-casein, possesses high specificity for μ receptors while showing minimal interaction with enkephalin receptors. Morphiceptin is primarily utilized in research focused on pain management and opioid receptor signaling pathways, providing valuable insights into receptor pharmacology. -
Mu-opioid Receptor Antagonist
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with a reported IC50 of 5.4 nM. This compound not only inhibits μ-opioid receptor activity but also demonstrates anti-leishmanial properties, making it relevant for studies on pain management and parasitic infections. Its unique profile supports research applications in opioid receptor modulation and leishmaniasis treatment development. -
κ-opioid Agonist
CR 665 is a peripherally selective κ-opioid agonist that targets the kappa opioid receptor, exhibiting an EC50 value of 10.9 nM. This compound is primarily utilized in research focused on peripheral pain mechanisms, making it a valuable tool for studying pain modulation and analgesic pathways. Its selective action offers potential for exploring new analgesic therapies with reduced central side effects. -
Opioid Receptor Agonist
Adrenorphin is an opioid octapeptide that functions primarily as a potent agonist of the μ-opioid receptor, exhibiting a binding affinity with a Ki value of 12 nM. This compound is significant for its role in research related to pain modulation, addiction, and neuroprotection. Its properties make it an essential tool for studying opioid receptor dynamics and related biological pathways. -
ORL1 Receptor Antagonist
J-113397 is a potent and selective nonpeptidyl antagonist of the ORL1 receptor, exhibiting a binding affinity with a Ki of 1.8 nM for cloned human ORL1. This compound is notable for its lack of agonistic activity on other opioid receptors, making it a valuable tool for studying the physiological and pharmacological roles of the ORL1 receptor. J-113397 is applicable in research focused on pain modulation, addiction, and various neurodegenerative diseases. -
Opioid Receptor Antagonist
(+)–N-Allylnormetazocine hydrochloride is an opioid receptor antagonist targeting σ1 and σ2 receptors, exhibiting Ki values of 300 nM and 27 μM, respectively. This benzomorphan compound demonstrates psychotomimetic effects and is of particular interest in the study of neurological diseases. It serves as a valuable reagent for research into opioid receptor interactions and their implications in various neuropharmacological conditions. -
Opioid Receptor Modulator
Samidorphan is an opioid receptor modulator with a high affinity for μ-opioid, κ-opioid, and δ-opioid receptors. It functions as an antagonist at μ-opioid receptors while serving as a partial agonist at κ- and δ-opioid receptors. This unique profile allows Samidorphan to primarily act as an opioid antagonist in vivo, demonstrating potential for improving depressive behaviors in animal models. Its mechanistic action makes it a valuable tool for research in the fields of pain management, addiction, and mood disorders. -
Opioid Receptor Agonist
Ro 64-6198 is a selective nonpeptide agonist of the nociceptin/orphanin FQ peptide (NOP) receptor, exhibiting a high affinity with an EC50 value of 25.6 nM. It shows over 100-fold selectivity for the NOP receptor compared to classic opioid receptors. This compound is valuable for research applications related to stress, anxiety, addiction, neuropathic pain, cough modulation, and appetite regulation. -
κ-opioid Agonist
Asimadoline hydrochloride is a selective κ-opioid agonist that exhibits peripheral activity with IC50 values of 5.6 nM in guinea pig tissues and 1.2 nM in human recombinant assays. This compound has limited blood-brain barrier permeability, making it suitable for targeting peripheral anti-inflammatory pathways. Asimadoline hydrochloride has demonstrated effectiveness in alleviating allodynia in diabetic rat models and offers potential therapeutic applications in the treatment of irritable bowel syndrome (IBS). -
κ2 Opioid Receptor Agonist
GR 89696 is a selective κ2 opioid receptor agonist known for its ability to modulate pain and itch responses. This compound has demonstrated potential in preventing pruritus, making it a valuable tool for research in pain management and neurological disorders. Its specificity for the κ2 receptor may facilitate studies aimed at understanding opioid receptor pathways and developing therapeutic strategies for itch-related conditions. -
μ Opioid Receptor Antagonist
CTAP is a potent and highly selective μ opioid receptor antagonist, exhibiting an IC50 of 3.5 nM. It demonstrates over 1200-fold selectivity against δ opioid receptors (IC50 = 4500 nM) and somatostatin receptors. CTAP is valuable for research applications focusing on L-DOPA-induced dyskinesia, as well as studies related to opiate overdose and addiction mechanisms. -
NOP Agonist
SCH 221510 is a selective and potent nociceptin opioid receptor (NOP) agonist, demonstrating an EC50 of 12 nM and a Ki of 0.3 nM. This compound exhibits anxiolytic-like effects, making it valuable for research applications in anxiety and other neuropsychiatric disorders. Its orally active nature enhances its utility in preclinical studies targeting the NOP signaling pathway. -
κ-Opioid Receptor Agonist
ICI-199441 hydrochloride is a potent and selective κ-opioid receptor agonist that exhibits significant analgesic properties. This compound has been shown to enhance cardiac resistance to ischemia/reperfusion injury, making it valuable in studies related to cardiovascular protection and pain management. Its specific targeting of the κ-opioid receptor underscores its potential utility in research applications focusing on the modulation of pain pathways and ischemic heart conditions. -
Kappa Opioid Receptor Antagonist
5'-Guanidinonaltrindole hydrochloride is a potent and selective κ-opioid receptor antagonist, exhibiting a Ki of 0.18 nM for the human κ-opioid receptor. This compound is employed in research to explore the roles of κ-opioid receptors in pain modulation, mood disorders, and addiction pathways. Its high affinity makes it a valuable tool for studies investigating the pharmacological effects of κ-opioid receptor inhibition. -
Opioid Receptor Agonist
[Leu5]-Enkephalin, amide is a selective agonist of the δ-opioid receptor. This compound exhibits significant analgesic properties and is involved in modulating pain pathways. It is commonly used in research to study opioid receptor signaling and its implications in pain management and addiction. -
Opioid Receptor Agonist
BPR1M97 is a dual-acting agonist for the mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor, exhibiting Ki values of 1.8 nM and 4.2 nM, respectively. This compound demonstrates significant potency and effective penetration of the blood-brain barrier, resulting in pronounced antinociceptive effects. BPR1M97 serves as a useful tool for research in pain management and opioid receptor biology.
