| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Neuromedin N targets dopamine D2 receptors, modulating the binding of dopamine D2 receptor agonists in rat neostriatal membranes. It produces a significant concentration-related increase in the Kd values of [³H]L-(-)-N-propylnorapomorphine binding sites in the concentration range of 1-10 nM, indicating an allosteric modulation of dopamine D2 receptor agonist binding. Neuromedin N also competitively inhibits the binding of neurotensin to rat brain synaptic membranes, albeit with 19-fold lower potency than neurotensin. This suggests that Neuromedin N may interact with neurotensin receptors (NTS1 and NTS2) as well as dopamine D2 receptors. The peptide is derived from the same precursor polypeptide as neurotensin (pro-neurotensin/neuromedin N), indicating shared biosynthetic origins. Its modulatory effects on dopamine receptor signaling suggest potential roles in the regulation of dopaminergic neurotransmission.
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| ln Vitro |
Neuromedin N is 19 times less powerful than neurotensin, competitively inhibits neurotensin's binding to rat brain synaptic membranes, and is quickly inactivated by brain synaptic peptidase [1]. It boosts efficacy when the peptidase inhibitor bestatin is present and competitively inhibits neurotensin binding to rat brain synaptic membranes [2].
In vitro, Neuromedin N competitively inhibits the binding of neurotensin to rat brain synaptic membranes, with a 19-fold lower potency than neurotensin. It is rapidly inactivated by brain synaptic peptidases, but its activity is enhanced in the presence of the peptidase inhibitor bestatin. Neuromedin N also modulates dopamine D2 receptor agonist binding in rat neostriatal membranes, producing a concentration-related increase in the Kd values of [³H]L-(-)-N-propylnorapomorphine binding sites in the concentration range of 1-10 nM. These findings suggest that Neuromedin N can modulate both neurotensin and dopamine receptor systems. The peptide is a valuable tool for studying the interactions between neurotensin and dopamine signaling pathways and their roles in neurological and psychiatric disorders. |
| ln Vivo |
In vivo activity data for Neuromedin N are limited. As a neuropeptide derived from the same precursor as neurotensin, it is expected to have similar but subtly distinct effects on neurotensin- and dopamine-related physiological processes. Neuromedin N may modulate dopaminergic neurotransmission in the brain, potentially affecting motor function, reward, and cognition. However, specific in vivo studies on Neuromedin N have not been extensively published. The peptide's rapid inactivation by brain synaptic peptidases suggests that its in vivo effects may be short-lived and locally restricted. Its activity is enhanced in the presence of peptidase inhibitors, indicating that peptidase activity is a major determinant of its in vivo bioavailability. Further in vivo studies would be required to fully characterize the physiological roles of Neuromedin N.
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| Enzyme Assay |
In vitro receptor binding assays for Neuromedin N typically involve competition binding studies using radiolabeled neurotensin or dopamine D2 receptor ligands. A typical protocol for neurotensin binding: rat brain synaptic membranes are prepared by homogenization and differential centrifugation. Membranes are incubated with [³H]-neurotensin (0.5-2 nM) and varying concentrations of Neuromedin N (0.1 nM to 10 μM) in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl₂, 0.1% BSA, 0.1 mM bacitracin, 1 μM bestatin) for 30-60 minutes at 4°C. Non-specific binding is determined in the presence of 1 μM unlabeled neurotensin. Bound radioactivity is separated by rapid filtration and quantified by scintillation counting. IC₅₀ and Kᵢ values are calculated from competition curves. For dopamine D2 receptor binding, rat neostriatal membranes are incubated with [³H]L-(-)-N-propylnorapomorphine (0.5-2 nM) and Neuromedin N (1-1000 nM), and Kd changes are assessed. Each concentration is tested in triplicate, and experiments are repeated at least three times.
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| Cell Assay |
In vitro cell-based assays for Neuromedin N are performed using neuronal cell lines or primary neuronal cultures. A typical protocol: cells (e.g., SH-SY5Y neuroblastoma cells or rat primary cortical neurons) are seeded in 96-well plates at 20,000-50,000 cells/well and cultured for 24-48 hours. Cells are treated with Neuromedin N at concentrations ranging from 0.1 nM to 10 μM for 15-60 minutes. Signaling readouts include neurotensin receptor-mediated calcium mobilization (measured using Fluo-4 or Fura-2 AM), ERK phosphorylation (measured by phospho-ERK ELISA or Western blot), or modulation of dopamine D2 receptor signaling (measured by cAMP accumulation or β-arrestin recruitment assays). For neurotensin receptor functional assays, cells expressing NTS1 or NTS2 are used, and calcium mobilization is measured upon stimulation with Neuromedin N. Each condition is tested in triplicate, and experiments are repeated at least three times. Positive controls include neurotensin and specific receptor agonists.
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| Animal Protocol |
In vivo animal studies for Neuromedin N have not been extensively reported. If conducted, a typical protocol would involve administering Neuromedin N to rodents via intracerebroventricular or intravenous injection at doses of 0.1-10 μg. Endpoints would depend on the hypothesized biological activity: for neurotensin-related effects, body temperature, nociception, or locomotor activity would be monitored; for dopamine-related effects, motor behavior, reward-related behaviors, or dopamine release would be assessed. Due to rapid peptidase-mediated degradation, co-administration with peptidase inhibitors (e.g., bestatin) may be necessary to observe significant effects. However, specific in vivo studies for Neuromedin N have not been published. The peptide is primarily used as a research tool for in vitro studies of neurotensin and dopamine receptor modulation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Neuromedin N have not been characterized due to its nature as a neuropeptide. As a peptide, Neuromedin N is susceptible to rapid degradation by peptidases in the gastrointestinal tract and plasma, resulting in poor oral bioavailability. The peptide has a short half-life in circulation and in brain tissue due to rapid inactivation by brain synaptic peptidases. Its activity is enhanced in the presence of the peptidase inhibitor bestatin, indicating that peptidase-mediated degradation is a major determinant of its bioavailability. Neuromedin N is derived from the same precursor as neurotensin and is likely to have similar pharmacokinetic properties. The peptide is typically administered via injection for in vitro and in vivo studies. It should be stored at -20°C or -80°C for long-term stability and protected from repeated freeze-thaw cycles.
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| Toxicity/Toxicokinetics |
Pharmacokinetic properties of Neuromedin N have not been characterized due to its nature as a neuropeptide. As a peptide, Neuromedin N is susceptible to rapid degradation by peptidases in the gastrointestinal tract and plasma, resulting in poor oral bioavailability. The peptide has a short half-life in circulation and in brain tissue due to rapid inactivation by brain synaptic peptidases. Its activity is enhanced in the presence of the peptidase inhibitor bestatin, indicating that peptidase-mediated degradation is a major determinant of its bioavailability. Neuromedin N is derived from the same precursor as neurotensin and is likely to have similar pharmacokinetic properties. The peptide is typically administered via injection for in vitro and in vivo studies. It should be stored at -20°C or -80°C for long-term stability and protected from repeated freeze-thaw cycles.
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| References |
[1]. Li XM, et al. Neuromedin N is a potent modulator of dopamine D2 receptor agonist binding in rat neostriatal membranes. Neurosci Lett. 1993 Jun 11;155(2):121-4.
[2]. Checler F, et al. Neuromedin N: high affinity interaction with brain neurotensin receptors and rapid inactivation by brain synaptic peptidases. Eur J Pharmacol. 1986 Jul 31;126(3):239-44. |
| Additional Infomation |
Toxicological data for Neuromedin N are limited as the peptide is a naturally occurring neuropeptide and research tool. At physiological concentrations, Neuromedin N is well-tolerated. High doses may affect neurotensin and dopamine receptor signaling, potentially leading to alterations in motor function, cognition, or autonomic regulation. The peptide has not undergone formal toxicology testing for regulatory purposes. Standard laboratory safety precautions should be followed when handling Neuromedin N: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The peptide should be stored at -20°C or -80°C and protected from light and moisture. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. Researchers should consult the safety data sheet (SDS) before handling.
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| Molecular Formula |
C38H63N7O8
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| Molecular Weight |
745.96
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| Exact Mass |
745.474
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| CAS # |
92169-45-4
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| PubChem CID |
9940301
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| Appearance |
White to off-white solid powder
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| LogP |
4.446
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
53
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| Complexity |
1210
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C(N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@H](C(=O)O)CC(C)C)CC1C=CC(O)=CC=1)(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H](N)CCCCN
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| InChi Key |
RZMLVIHXZGQADB-YLUGYNJDSA-N
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| InChi Code |
InChI=1S/C38H63N7O8/c1-7-23(5)31(36(50)42-29(38(52)53)20-22(3)4)43-34(48)28(21-25-14-16-26(46)17-15-25)41-35(49)30-13-11-19-45(30)37(51)32(24(6)8-2)44-33(47)27(40)12-9-10-18-39/h14-17,22-24,27-32,46H,7-13,18-21,39-40H2,1-6H3,(H,41,49)(H,42,50)(H,43,48)(H,44,47)(H,52,53)/t23-,24-,27-,28-,29-,30-,31-,32-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S,3S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid
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| Synonyms |
KIPYIL; Neuromedin-N; Neuromedin N
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~67.03 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (67.03 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3406 mL | 6.7028 mL | 13.4055 mL | |
| 5 mM | 0.2681 mL | 1.3406 mL | 2.6811 mL | |
| 10 mM | 0.1341 mL | 0.6703 mL | 1.3406 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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