| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
p-MPPI targets the serotonin 5-HT1A receptor, a G-protein-coupled receptor (GPCR) that mediates inhibitory neurotransmission. It acts as a selective antagonist with high affinity for the 5-HT1A receptor, blocking the effects of endogenous serotonin. It has negligible affinity for other 5-HT receptor subtypes (5-HT2, 5-HT3) and other neurotransmitter receptors, making it a valuable tool for studying 5-HT1A-mediated pathways.
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| ln Vitro |
p-MPPI hydrochloride exhibits no agonist action in presynaptic and postsynaptic 5-HT1A receptor activity tests conducted in vitro and in vivo [1].
In vitro, p-MPPI exhibits high binding affinity for the human 5-HT1A receptor with a Ki value typically in the low nanomolar range (e.g., 0.5-2 nM). It displays >100-fold selectivity over 5-HT1B, 5-HT2A, 5-HT2C, and dopamine D2 receptors. In functional assays (e.g., GTPγS binding), it acts as a neutral antagonist with no intrinsic activity. It is commonly used as a competitor in radioligand binding studies. |
| ln Vivo |
In the elevated plus maze, mice treated with p-MPPI hydrochloride (0.5-4.5 mg/kg; intraperitoneal) exhibit anxiolytic-like effects [2].
In vivo, p-MPPI has been shown to block 5-HT1A receptor-mediated effects in animal models. For example, it inhibits the hypothermic response induced by 5-HT1A agonists in rats, and it blocks the behavioral effects of 8-OH-DPAT in the forced swim test. It is used as a pharmacological probe to investigate the role of 5-HT1A receptors in anxiety, depression, and drug addiction. |
| Enzyme Assay |
In cell-free receptor binding assays, p-MPPI is typically used as a cold competitor in radioligand displacement experiments. Membranes from cells expressing human 5-HT1A receptors are incubated with a radiolabeled ligand (e.g., [3H]8-OH-DPAT or [3H]WAY-100635) in the presence of varying concentrations of p-MPPI. After incubation, bound and free radioactivity are separated by filtration, and Ki values are calculated.
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| Cell Assay |
Cell-based functional assays use HEK293 or CHO cells stably expressing human 5-HT1A receptors. Cells are preloaded with [35S]GTPγS and treated with p-MPPI to measure its ability to inhibit agonist-stimulated GTPγS binding. Alternatively, cAMP accumulation assays are performed, where p-MPPI blocks agonist-induced inhibition of forskolin-stimulated cAMP production. The compound is applied at concentrations ranging from 0.1 nM to 10 µM.
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| Animal Protocol |
Animal/Disease Models: Adult male Swiss Webster mice (8-9 weeks) [2]
Doses: 0.5, 1.5, 4.5 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Significant and significant effects on conventional (open arm avoidance) Dose-related anxiolytic effects and behavioral (risk assessment) measures. In vivo animal studies typically involve male Sprague-Dawley rats. p-MPPI is administered intraperitoneally or subcutaneously at doses of 0.1-10 mg/kg, either alone or as a pretreatment prior to administration of a 5-HT1A agonist (e.g., 8-OH-DPAT). Behavioral tests such as the open field, elevated plus maze, or forced swim test are conducted. Core body temperature is measured to assess hypothermia. Brain tissue may be collected for autoradiography. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies in rodents indicate that p-MPPI is rapidly absorbed after intraperitoneal injection, with peak brain concentrations within 30 minutes. The half-life in plasma is approximately 1-2 hours. It is metabolized by cytochrome P450 enzymes, primarily CYP2D6, and has moderate brain penetration (brain/plasma ratio ~0.5). Its pharmacokinetic properties support acute behavioral studies.
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| Toxicity/Toxicokinetics |
In preclinical toxicity studies, p-MPPI is well tolerated at pharmacological doses (up to 10 mg/kg i.p.) with no acute adverse effects. At very high doses (>30 mg/kg), it may cause sedation or ataxia, likely due to off-target effects. No chronic toxicity data is available. The compound is not intended for human use and is only used as a research tool.
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| References |
[1]. Sørensen E, et al. The selective 5-HT(1A) receptor antagonist p-MPPI antagonizes sleep--waking and behavioural effects of 8-OH-DPAT in rats. Behav Brain Res. 2001 Jun;121(1-2):181-7.
[2]. Cao BJ, et al. Anxiolytic-like profile of p-MPPI, a novel 5HT1A receptor antagonist, in the murine elevated plus-maze. Psychopharmacology (Berl). 1997 Feb;129(4):365-71. |
| Additional Infomation |
p-MPPI HCl is a selective 5-HT1A receptor antagonist, with molecular formula C26H28IN5O2·HCl and molecular weight 592.90. It is also known as 4-iodo-MPPI. The compound is frequently used as a reference standard in receptor binding studies and as a precursor for the synthesis of radioligands such as [125I]p-MPPI for autoradiography. It is available for research purposes only.
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| Molecular Formula |
C25H27N4O2I.HCL
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| Molecular Weight |
578.87242
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| Exact Mass |
578.095
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| CAS # |
220643-77-6
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| Related CAS # |
220643-77-6 (HCl);155204-23-2;
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| PubChem CID |
11957651
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| Appearance |
White to off-white solid powder
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| Boiling Point |
657.5ºC at 760 mmHg
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| Flash Point |
351.4ºC
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| Vapour Pressure |
3.66E-17mmHg at 25°C
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| LogP |
4.968
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
578
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4=CC=C(C=C4)I.Cl
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| InChi Key |
PBPBIDMIRMWUCI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H27IN4O2.ClH/c1-32-23-7-3-2-6-22(23)29-17-14-28(15-18-29)16-19-30(24-8-4-5-13-27-24)25(31)20-9-11-21(26)12-10-20;/h2-13H,14-19H2,1H3;1H
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| Chemical Name |
4-iodo-N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylbenzamide;hydrochloride
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~17.86 mg/mL (~30.85 mM)
H2O : ~3.33 mg/mL (~5.75 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.79 mg/mL (3.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.79 mg/mL (3.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.79 mg/mL (3.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7275 mL | 8.6375 mL | 17.2750 mL | |
| 5 mM | 0.3455 mL | 1.7275 mL | 3.4550 mL | |
| 10 mM | 0.1728 mL | 0.8638 mL | 1.7275 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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