Identification | Back Directory | [Name]
2-[(3-CHLOROPHENYL)METHOXY]-6-(1-PIPERAZINYL)PYRAZINE HYDROCHLORIDE | [CAS]
479683-64-2 | [Synonyms]
CS-687 CP809101 CP-809101 CP 809101 CP809101/CP-809101 CP 809101 hydrochlor CP 809101 HYDROCHLORIDE Pyrazine, 2-[(3-chlorophenyl)methoxy]-6-(1-piperazinyl)- 6'-(3-Chlorobenzyloxy)-3,4,5,6-tetrahydro-2H-[1,2']bipyrazine 2-[(3-CHLOROPHENYL)METHOXY]-6-(1-PIPERAZINYL)PYRAZINE HYDROCHLORIDE | [Molecular Formula]
C15H17ClN4O | [MDL Number]
MFCD10687106 | [MOL File]
479683-64-2.mol | [Molecular Weight]
304.77 |
Chemical Properties | Back Directory | [Boiling point ]
486.6±45.0 °C(Predicted) | [density ]
1.265±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at RT | [solubility ]
DMSO | [form ]
powder | [pka]
8.24±0.10(Predicted) | [color ]
white to beige |
Hazard Information | Back Directory | [Uses]
CP 809101 is a potent and selective SR-2C and 5-HT2C agonist. | [Biological Activity]
Potent and selective 5-HT 2C receptor agonist (pEC 50 values are 9.96, 7.19 and 6.81 for human 5-HT 2C , 5-HT 2B and 5-HT 2A receptors respectively). Displays antipsychotic activity; suppresses condition avoidance responding (CAR) and inhibits PCP and amphetamine-stimulated hyperactivity in rats following subcutaneous administration. | [Biochem/physiol Actions]
CP-809,101 is a potent and high-affinity 5-hydroxytryptamine receptor 2C (5-HT2C) full agonist with only weaker partial agonist activity toward 5-HT2A & 5-HT2B (cellular Ca2+ mobilization EC50 in nM/efficiency = 0.11/93% and 0.06/97% with human and rat 5-HT2C, respectively; 153/67%/human 5HT2A, 65.3/57%/human 5HT2B, 119/79%/rat 5HT2A) and much reduced or little affinity toward other receptors, ion channels and uptake sites tested. CP-809,101 exhibits antipsychotic efficacy in reducing conditioned avoidance response/CAR (ED50 = 4.8 mg/kg s.c.) and locomotor activity (ED50 in mg/kg via s.c. = 2/rats, 1/mice; no effect up to 10 mg/kg in 5-HT2C-knockout mice), while oral administration is reported to suppress spontaneous and nocturnal food intake as well as fasting-induced refeeding in rats (~8% and ~24% reduction of cumulative food intake and body weight in 4 days, respectively; 30 mg/kg/day p.o.). |
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