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CP-809101 (CP809101) is a selective 5-HT2C receptor agonist with antipsychotic activity. It activates human 5-HT2C/5-HT2B/5-HT2A receptors with pEC50 of 9.96/7.19/6.81, respectively. CP-809101 reduces motor impulsivity and reinstatement of food seeking behavior in male rats. CP-809101 (0.3-3 mg/kg SC) reduced responding for both nicotine and food and blocked the discriminative stimulus properties of nicotine in a similar manner to lorcaserin and Ro 60-0175.
ln Vivo |
In rats, CP-809101 (0.1-56 mg/kg; subcutaneous injection; single dose) dose-dependently suppresses the conditioned avoidance response [1]. ADHD caused by d-amphetamine (which is induced in a dose-dependent manner) and PCP (phencyclidine hydrochloride) is countered by CP-809101 (0.56, 1.78, 5.6, 17.8 mg/kg; subcutaneous injection; single dose) [ 1]. With an ED50 value of 2.2 mg/kg, CP-809101 (0.56, 1.78, 5.6, 17.8 mg/kg; subcutaneous injection; single dosage) decreases spontaneous locomotor activity in a dose-dependent manner [1]. CP-809101 (0.3, 1, 3 mg/kg; subcutaneous injection; single dosage) inhibits the discriminative stimulus characteristics of nicotine and decreases responses to food and nicotine [2].
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Animal Protocol |
Animal/Disease Models: Male CF rat (conditioned avoidance response (CAR) model) [1].
Doses: 0.1-56 mg/kg Route of Administration: subcutaneous injection; single. Experimental Results: Dose-dependent inhibition of conditioned avoidance response, with ID50 value of 4.8 mg/kg. Animal/Disease Models: Male CD rat (PCP or d-amphetamine-induced hyperactivity model) [1]. Doses: 0.56, 1.78, 5.6, 17.8 mg/kg Route of Administration: subcutaneous injection; single. Experimental Results: Antagonizes the hyperactivity caused by PCP, with an ED50 value of 2.4 mg/kg. Antagonizes d-amphetamine-induced ADHD with an ED50 value of 2.7 mg/kg in a dose-dependent manner. Animal/Disease Models: Male CD rat (spontaneous movement model) [1]. Doses: 0.56, 1.78, 5.6, 17.8 mg/kg Route of Administration: subcutaneous injection; single. Experimental Results: Inhibition of spontaneous locomotor activity in a dose-dependent manner (ED50=2.7 mg/kg). Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rat (280-400 g) [2]. Doses: 0.3, 1, 3 mg/kg Route of Administration: subcutaneous injection; single. Experimental Results: Rats demonstrated dose-r |
References |
[1]. Siuciak JA, et al. CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity. Neuropharmacology. 2007 Feb;52(2):279-90.
[2]. Higgins GA, et al. Evaluation of chemically diverse 5-HT₂c receptor agonists on behaviours motivated by food and nicotine and on side effect profiles. Psychopharmacology (Berl). 2013 Apr;226(3):475-90. |
Molecular Formula |
C15H17N4OCL.HCL
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Molecular Weight |
341.236
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CAS # |
479683-64-2
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Related CAS # |
CP-809101 hydrochloride;1215721-40-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
ClC1=CC(COC2=NC(N3CCNCC3)=CN=C2)=CC=C1
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.9305 mL | 14.6524 mL | 29.3049 mL | |
5 mM | 0.5861 mL | 2.9305 mL | 5.8610 mL | |
10 mM | 0.2930 mL | 1.4652 mL | 2.9305 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.