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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Pirenperone targets the serotonin 5-HT2A receptor (SR-2A), a G protein-coupled receptor involved in various physiological processes, including neurotransmission, vasoconstriction, and platelet aggregation. As a selective antagonist, pirenperone blocks serotonin-mediated signaling at the 5-HT2A receptor. It has also been described as a selective 5-HT1A receptor antagonist in some sources. The compound displays moderate affinity for other targets.
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| ln Vitro |
Pirenperone is a selective 5-HT2 serotonin receptor blocker (antagonist). Its activity can be assessed using radioligand binding assays and functional assays measuring receptor-mediated signaling. The compound's affinity for 5-HT2A receptors and its selectivity over other serotonin receptor subtypes have been characterized in various in vitro studies.
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| ln Vivo |
Pirenperone is used in vivo in animal models to study the role of serotonin 5-HT2 receptors in various physiological and pathological processes. Its effects on serotonin-mediated behaviors have been evaluated in rodent models. The compound's potential therapeutic effects have been investigated in research related to psychiatric disorders and other conditions.
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| Enzyme Assay |
Non-cellular receptor binding assays for pirenperone involve competitive radioligand binding displacement studies using membrane preparations from cells expressing the human 5-HT2A receptor. The membranes are incubated with a radiolabeled 5-HT2A-selective ligand (e.g., [³H]ketanserin) and varying concentrations of pirenperone. Following incubation and filtration, the radioactivity is measured to determine the IC50, which is then converted to a Ki value using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cellular assays for pirenperone involve treating cells expressing the 5-HT2A receptor with the compound and measuring receptor-mediated signaling. Functional assays typically measure intracellular calcium mobilization (as 5-HT2A receptors are coupled to Gq proteins). Cells are loaded with a calcium-sensitive dye (e.g., Fluo-4) and stimulated with serotonin in the presence of varying concentrations of pirenperone. The inhibition of the calcium response is quantified to determine the IC50 for antagonism.
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| Animal Protocol |
In vivo animal experiments with pirenperone involve administering the compound to rodents and assessing its effects on serotonin-mediated behaviors. Behavioral assays such as the head-twitch response (induced by 5-HT2A agonists), locomotor activity, and prepulse inhibition are used to evaluate the effects of 5-HT2A receptor blockade. The compound's potential therapeutic effects are assessed in models of psychiatric disorders.
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| ADME/Pharmacokinetics |
Pirenperone has a molecular weight of 393.45-393.46 and a molecular formula of C23H24FN3O2. It is a solid at room temperature and is typically stored as a powder at -20°C for up to 3 years or at 4°C for 2 years. Purity is ≥98% by HPLC. The compound is soluble in 0.1 M HCl (11 mg/mL) and DMSO. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Pirenperone is a research compound for laboratory use only and is not intended for human therapeutic or diagnostic use. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation. Appropriate personal protective equipment should be used.
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| Additional Infomation |
3-[2-[4-[(4-fluorophenyl)-oxymethyl]-1-piperidinyl]ethyl]-2-methyl-4-pyrido[1,2-a]pyrimidinone is an aromatic ketone.
Pirenperone (CAS 75444-65-4) is a quinazoline derivative and a selective antagonist of the serotonin 5-HT2A receptor. It is commonly used in medical research for its potential therapeutic effects. Pirenperone is also described as a selective 5-HT1A receptor antagonist. The compound is available from various commercial suppliers for research applications. |
| Molecular Formula |
C23H24N3O2F
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|---|---|
| Molecular Weight |
393.45396
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| Exact Mass |
393.185
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| CAS # |
75444-65-4
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| PubChem CID |
4847
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
556.3ºC at 760 mmHg
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| Flash Point |
290.2ºC
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| Index of Refraction |
1.629
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| LogP |
3.217
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
782
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(CCN2CCC(CC2)C(=O)C3=CC=C(C=C3)F)C(=O)N4C=CC=CC4=N1
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| InChi Key |
HXCNRYXBZNHDNE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24FN3O2/c1-16-20(23(29)27-12-3-2-4-21(27)25-16)11-15-26-13-9-18(10-14-26)22(28)17-5-7-19(24)8-6-17/h2-8,12,18H,9-11,13-15H2,1H3
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| Chemical Name |
3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-2-methylpyrido[1,2-a]pyrimidin-4-one
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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 |
| 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 : ~25 mg/mL (~63.54 mM)
0.1 M HCL : 16.67 mg/mL (~42.37 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5416 mL | 12.7081 mL | 25.4162 mL | |
| 5 mM | 0.5083 mL | 2.5416 mL | 5.0832 mL | |
| 10 mM | 0.2542 mL | 1.2708 mL | 2.5416 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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