2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. CP-809101

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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CP-809101 Chemical Structure

CP-809101 Chemical Structure

CAS No. : 479683-64-2

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Description

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[1][2].

IC50 & Target

5-HT2C Receptor

9.96 (pEC50)

5-HT2B Receptor

7.19 (pEC50)

5-HT2A Receptor

6.81 (pEC50)

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.
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
References
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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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