CP-809101
Based on 2 publication(s) in Google Scholar
CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.
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- CAS No.: 479683-64-2
- 화학식: C15H17ClN4O
- 분자량:304.77
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CP-809101
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT2C Receptor 9.96 (pEC50) |
5-HT2B Receptor 7.19 (pEC50) |
5-HT2A Receptor 6.81 (pEC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.0019 μM
Compound: CP 809101
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Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
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[PMID: 23301527] |
| HEK293 | EC50 |
0.0081 μM
Compound: CP 809101
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Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
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[PMID: 23301527] |
| HEK293 | EC50 |
0.076 μM
Compound: CP 809101
|
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
|
[PMID: 23301527] |
| HEK293 | EC50 |
0.14 μM
Compound: CP 809101
|
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
|
[PMID: 23301527] |
CP-809101 (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) antagonizes PCP (phencyclidine hydrochloride)-induced and d-amphetamine-induced hyperactivity (the latter in a dose-dependent manner)[1].
CP-809101 (0.56, 1.78, 5.6, 17.8 mg/kg; s.c.; single) dose-dependently decreases spontaneous locomotor activity with an ED50 value of 2.2 mg/kg[1].
CP-809101 (0.3, 1, 3 mg/kg; s.c.; single) reduces responding for both nicotine and food and blocked the discriminative stimulus properties of nicotine[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CF rats (conditioned avoidance responding (CAR) model)[1].
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Dosage:0.1-56 mg/kg
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Administration:Subcutaneous injection; single.
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Result:Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID50 value of 4.8 mg/kg.
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Animal Model:Male CD rats (PCP or d-amphetamine-induced hyperactivity model)[1].
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Dosage:0.56, 1.78, 5.6, 17.8 mg/kg
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Administration:Subcutaneous injection; single.
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Result:Antagonized PCP-induced hyperactivity, with an ED50 value of 2.4 mg/kg.
Antagonized d-amphetamine-induced hyperactivity, with an ED50 value of 2.7 mg/kg, and in a dose-dependent manner.
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Animal Model:Male CD rats (spontaneous locomotor model)[1].
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Dosage:0.56, 1.78, 5.6, 17.8 mg/kg
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Administration:Subcutaneous injection; single.
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Result:Inhibited spontaneous locomotor activity in a dose-dependent manner (ED50=2.7 mg/kg).
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Animal Model:Adult male Sprague-Dawley rats (280-400 g)[2].
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Dosage:0.3, 1, 3 mg/kg
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Administration:Subcutaneous injection; single.
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Result:Produced a dose-related decrease in responding for food and nicotine self-administration in rats.
Chemical Information
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CAS No. 479683-64-2
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분자량 304.77
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화학식 C15H17ClN4O
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SMILES
ClC1=CC(COC2=NC(N3CCNCC3)=CN=C2)=CC=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Brain
Hippocampal excitation-inhibition balance underlies the 5-HT2C receptor in modulating depressive behaviours. [Abstract]2024 Nov 4;147(11):3764-3779. PMID: 38701344 -
순도&문서
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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