5-HT2C Receptor (pEC50 = 9.96); 5-HT2B Receptor (pEC50 = 7.19); 5-HT2A Receptor (pEC50 = 6.81)

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].

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.

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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.

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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).

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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

[1]. CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity. Neuropharmacology. 2007 Feb;52(2):279-90.

[2]. 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.

CP-809,101 is a potent, functionally selective 5-HT(2C) receptor agonist with near-100% efficacy in vitro. This study aimed to evaluate the efficacy of this selective 5-HT(2C) receptor agonist in an animal model predicting the efficacy and risk of side effects of antipsychotic drugs. Similar to existing antipsychotics, CP-809,101 dose-dependently inhibits conditioned avoidance response (CAR, ED(50) = 4.8 mg/kg, subcutaneous injection). Concomitant administration of the 5-HT(2C) receptor antagonist SB-224,282 completely antagonized the inhibitory effect of CP-809,101 on CAR. CP-809,101 antagonized PCP- and d-amphetamine-induced hyperactivity with ED50 values of 2.4 and 2.9 mg/kg (subcutaneous injection), respectively, and also reversed apomorphine-induced prepulse inhibition defects. At doses up to 56 mg/kg, CP-809,101 did not induce rigidity. Therefore, the results of this study indicate that the pharmacological properties of the 5-HT2C receptor agonist CP-809,101 are similar to those of atypical antipsychotics with a low incidence of extrapyramidal symptoms. CP-809,101 was inactive in two animal models of antidepressant-like activity (forced swimming test and learned helplessness model). However, CP-809,101 showed activity in novel object recognition (an animal model of cognitive function). These data suggest that 5-HT(2C) receptor agonists may be a novel approach for treating psychosis and improving cognitive impairment associated with schizophrenia. [1] Selective 5-HT2C receptor agonists, such as lorcaserin, are being developed for the treatment of obesity. Studies have shown that they may also have the potential to treat addictive behaviors, including nicotine dependence, although the number of such drugs evaluated is small. Objective: The primary objective of this study was to evaluate the effects of the highly selective 5-HT2C receptor agonist CP-809101 on food-motivated behaviors (operational FR5 and progressive ratio reinforcement programs, palatability-induced feeding) and nicotine-motivated behaviors (intravenous self-administration, drug discrimination) in rats, and to compare these effects with those of the structurally different 5-HT2C receptor agonists lorcaserin and Ro 60-0175. Secondary objectives were to assess the side effect profiles of lorcaserin and CP-809101 and to determine the plasma concentrations of lorcaserin at doses (1 mg/kg) that reduce food and nicotine fortification, for comparison with plasma concentrations reported in human trials. Results: CP-809101 (0.3–3 mg/kg subcutaneously) reduced responses to nicotine and food and blocked the discriminative stimuli of nicotine in a manner similar to that of lorcaserin and Ro 60-0175. Reduced activity, chewing, and ptosis were observed after administration of high doses of CP-809101 and lorcaserin. Plasma concentrations of lorcaserin were similar to those reported in obesity trials. Conclusion: These studies support the use of 5-HT2C receptor agonists as a treatment for nicotine dependence. Plasma exposure levels following acute lorcaserin treatment suggest that equivalent doses can be used to evaluate the efficacy of these drugs in obesity and smoking cessation trials. Finally, the side effect profiles of lorcaserin and CP-809101 may differ, suggesting that tolerability to 5-HT2C agonists may vary. [2]

C15H17N4OCL.HCL

341.236

304.1090

479683-64-2

CP-809101 hydrochloride;1215721-40-6

9901086

Typically exists as solid at room temperature

1.3±0.1 g/cm3

486.6±45.0 °C at 760 mmHg

248.1±28.7 °C

0.0±1.2 mmHg at 25°C

1.597

3.02

1

5

4

21

314

0

ClC1=CC(COC2=NC(N3CCNCC3)=CN=C2)=CC=C1

PCWGGOVOEWHPMG-UHFFFAOYSA-N

InChI=1S/C15H17ClN4O/c16-13-3-1-2-12(8-13)11-21-15-10-18-9-14(19-15)20-6-4-17-5-7-20/h1-3,8-10,17H,4-7,11H2

2-[(3-chlorophenyl)methoxy]-6-piperazin-1-ylpyrazine

A2EXW95647; Pyrazine, 2-((3-chlorophenyl)methoxy)-6-(1-piperazinyl)-; 2-[(3-chlorophenyl)methoxy]-6-piperazin-1-ylpyrazine; UNII-A2EXW95647; CHEMBL494947; 6'-(3-Chlorobenzyloxy)-3,4,5,6-tetrahydro-2H-(1,2')bipyrazine;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)