CAS 479683-64-2|CP-809101

Introduction：Basic information about CAS 479683-64-2|CP-809101, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. CP-809101 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	CP-809101
CAS Number	479683-64-2	Molecular Weight	304.77
Density	1.3±0.1 g/cm3	Boiling Point	486.6±45.0 °C at 760 mmHg
Molecular Formula	C₁₅H₁₇ClN₄O	Melting Point	/
MSDS	/	Flash Point	248.1±28.7 °C

Names

Name	2-[(3-chlorophenyl)methoxy]-6-piperazin-1-ylpyrazine
Synonym	More Synonyms

CP-809101 BiologicalActivity

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 ReceptorCP-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.
Related Catalog	Signaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Neurological Disease
References	[1]. Higgins GA, Silenieks LB, Lau W, 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. [2]. Strong PV, Christianson JP, Loughridge AB, et al. 5-hydroxytryptamine 2C receptors in the dorsal striatum mediate stress-induced interference with negatively reinforced instrumental escape behavior. Neuroscience. 2011 Dec 1;197:132-44. doi: 10.1016/j.neur [3]. Fletcher PJ, Tampakeras M, Sinyard J et al. Characterizing the effects of 5-HT(2C) receptor ligands on motor activity and feeding behaviour in 5-HT(2C) receptor knockout mice. Neuropharmacology. 2009 Sep;57(3):259-67. doi: 10.1016/j.neuropharm.2009.05.011 [4]. Siuciak JA, Chapin DS, McCarthy SA, 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.

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 ReceptorCP-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.

Related Catalog

Signaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Neurological Disease

References

[1]. Higgins GA, Silenieks LB, Lau W, 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.

[2]. Strong PV, Christianson JP, Loughridge AB, et al. 5-hydroxytryptamine 2C receptors in the dorsal striatum mediate stress-induced interference with negatively reinforced instrumental escape behavior. Neuroscience. 2011 Dec 1;197:132-44. doi: 10.1016/j.neur

[3]. Fletcher PJ, Tampakeras M, Sinyard J et al. Characterizing the effects of 5-HT(2C) receptor ligands on motor activity and feeding behaviour in 5-HT(2C) receptor knockout mice. Neuropharmacology. 2009 Sep;57(3):259-67. doi: 10.1016/j.neuropharm.2009.05.011

[4]. Siuciak JA, Chapin DS, McCarthy SA, 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.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	486.6±45.0 °C at 760 mmHg
Molecular Formula	C₁₅H₁₇ClN₄O
Molecular Weight	304.77
Flash Point	248.1±28.7 °C
PSA	50.28000
LogP	3.02
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.597
InChIKey	PCWGGOVOEWHPMG-UHFFFAOYSA-N
SMILES	Clc1cccc(COc2cncc(N3CCNCC3)n2)c1
Storage condition	2-8℃

Synonyms

2-[(3-Chlorobenzyl)oxy]-6-(1-piperazinyl)pyrazine

cs-1201

CP-809,101

Pyrazine, 2-[(3-chlorophenyl)methoxy]-6-(1-piperazinyl)-

CP-809101

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