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Merck
CN

PZ0378

CP-809,101 fumarate

≥98% (HPLC)

Synonym(s):

2-(3-Chlorobenzyloxy)-6-(piperazin-1-yl)pyrazine fumarate

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About This Item

Empirical Formula (Hill Notation):
C15H17ClNO4 · C4H4O4
CAS Number:
Molecular Weight:
426.82
UNSPSC Code:
12352202
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
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assay

≥98% (HPLC)

form

powder

color

white to beige

storage temp.

−20°C

SMILES string

Clc1cc(ccc1)COc2nc(cnc2)N3CCNCC3

InChI

1S/C15H17ClN4O/c16-13-3-1-2-12(8-13)11-21-15-10-18-9-14(19-15)20-6-4-17-5-7-20/h1-3,8-10,17H,4-7,11H2

InChI key

PCWGGOVOEWHPMG-UHFFFAOYSA-N

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.).


pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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