CP-809101

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CP-809101 is a potent and highly selective 5-HT_2C receptor agonist, with pEC₅₀s of 9.96, 7.19 and 6.81 M for human 5HT_2C, 5HT_2B and 5HT_2A 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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CP-809101 Chemical Structure

CAS No. : 479683-64-2

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Other In-stock Forms of CP-809101:

CP-809101 hydrochloride

Other Forms of CP-809101:

CP-809101 hydrochloride In-stock

1 Publications Citing Use of MCE CP-809101

•Brain. 2024 May 3:awae143. [Abstract]

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•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT_2C Receptor

9.96 (pEC₅₀)

5-HT_2B Receptor

7.19 (pEC₅₀)

5-HT_2A Receptor

6.81 (pEC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.0019 μM Compound: CP 809101	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	[PMID: 23301527]
HEK293	EC₅₀	0.0081 μM Compound: CP 809101	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	[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]

In Vivo

CP-809101 (0.1-56 mg/kg; s.c.; single) inhibits the conditioned avoidance response of rats in a dose-dependent manner^[1].
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.

Animal Model:	Male CF rats (conditioned avoidance responding (CAR) model)^[1].
Dosage:	0.1-56 mg/kg
Administration:	Subcutaneous injection; single.
Result:	Resulted in a dose-dependent inhibition of the conditioned avoidance response with an ID₅₀ value of 4.8 mg/kg.

Animal Model:	Male CD rats (PCP or d-amphetamine-induced hyperactivity model)^[1].
Dosage:	0.56, 1.78, 5.6, 17.8 mg/kg
Administration:	Subcutaneous injection; single.
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.

Animal Model:	Male CD rats (spontaneous locomotor model)^[1].
Dosage:	0.56, 1.78, 5.6, 17.8 mg/kg
Administration:	Subcutaneous injection; single.
Result:	Inhibited spontaneous locomotor activity in a dose-dependent manner (ED₅₀=2.7 mg/kg).

Animal Model:	Adult male Sprague-Dawley rats (280-400 g)^[2].
Dosage:	0.3, 1, 3 mg/kg
Administration:	Subcutaneous injection; single.
Result:	Produced a dose-related decrease in responding for food and nicotine self-administration in rats.

Molecular Weight

304.77

Formula

C₁₅H₁₇ClN₄O

CAS No.

479683-64-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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]

CP-809101 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CP-809101479683-64-2CP809101CP 8091015-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorantipsychoticconditioned avoidance respondinghyperactivitynicotine dependencenicotineInhibitorinhibitorinhibit

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