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

CP-809101 

Cat. No.: HY-15543
Handling Instructions

CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.

For research use only. We do not sell to patients.

CP-809101 Chemical Structure

CP-809101 Chemical Structure

CAS No. : 479683-64-2

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Description

CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively. IC50 Value: 9.96(pEC50 for 5-HT2C); 7.19(pEC50 for 5-HT2B); 6.81(pEC50 for 5-HT2A) Target: 5-HT2C Receptor CP-809101 is a potent, functionally selective 5-HT2C agonist that displays approximately 100% efficacy in vitro. The aim of the present studies was to assess the efficacy of a selective 5-HT2C agonist in animal models predictive of antipsychotic-like efficacy and side-effect liability. Similar to currently available antipsychotic drugs, CP-809101 dose-dependently inhibited conditioned avoidance responding (CAR, ED50 = 4.8 mg/kg, sc). CP-809101 antagonized both PCP- and d-amphetamine-induced hyperactivity with ED50 values of 2.4 and 2.9 mg/kg (sc), respectively and also reversed an apomorphine induced-deficit in prepulse inhibition. At doses up to 56 mg/kg, CP-809101 did not produce catalepsy. Thus, the present results demonstrate that the 5-HT2C agonist, CP-809101, has a pharmacological profile similar to that of the atypical antipsychotics with low extrapyramidal symptom liability. CP-809101 was inactive in two animal models of antidepressant-like activity, the forced swim test and learned helplessness.

IC50 & Target

5-HT2C Receptor

9.96 (pEC50)

5-HT2B Receptor

7.19 (pEC50)

5-HT2A Receptor

6.81 (pEC50)

Molecular Weight

304.77

Formula

C₁₅H₁₇ClN₄O

CAS No.

479683-64-2

SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

CP-809101CP809101CP 8091015-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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CP-809101
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HY-15543
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