479683-64-2

479683-64-2 structure
479683-64-2 structure
  • Name: CP-809101
  • Chemical Name: 2-[(3-chlorophenyl)methoxy]-6-piperazin-1-ylpyrazine
  • CAS Number: 479683-64-2
  • Molecular Formula: C15H17ClN4O
  • Molecular Weight: 304.77
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2016-03-05 06:13:00
  • Modify Date: 2024-01-10 17:40:05
  • 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.

Name 2-[(3-chlorophenyl)methoxy]-6-piperazin-1-ylpyrazine
Synonyms 2-[(3-Chlorobenzyl)oxy]-6-(1-piperazinyl)pyrazine
cs-1201
CP-809,101
Pyrazine, 2-[(3-chlorophenyl)methoxy]-6-(1-piperazinyl)-
CP-809101
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.
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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.

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
Storage condition 2-8℃