CP-809101

Details

Stereochemistry	ACHIRAL
Molecular Formula	C15H17ClN4O
Molecular Weight	304.775
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=PCWGGOVOEWHPMG-UHFFFAOYSA-N

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

HIDE SMILES / InChI

Molecular Formula	C15H17ClN4O
Molecular Weight	304.775
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16949622
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23049953

CP-809101 is a potent, functionally selective 5-HT(2C) agonist that displays approximately 100% efficacy in vitro. CP-809101 has a pharmacological profile similar to that of the atypical antipsychotics with low extrapyramidal symptom liability. CP-809101 was active in novel object recognition, an animal model of cognitive function. It had promising results in animal models of obesity and psychosis.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 2c (5-HT2c) receptor 124 Target ID: CHEMBL225 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16949622	Agonist 2678		0.11 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Psychosis 16 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27085605 https://www.ncbi.nlm.nih.gov/pubmed/16949622	Primary		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity.	2007 Feb	16949622
Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation.	2007 Jun	17344339

Patents

Sample Use Guides

In Vivo Use Guide

Rats: rats were used to test the effect of varying doses of CP-809101 (1–3 mg/kg SC) on nicotine self-administration according to a repeated-measures design, with each animal receiving each dose and vehicle in a counterbalanced sequence, with 2–4 days between cycles.

Route of Administration: Other

In Vitro Use Guide

CP-809101 increased mouse renal proximal tubular cells (RPTCs) respiration and peroxisome proliferator-activated receptor γ coactivator-1α (PGC-1α) mRNA expression in RPTCs at 1-10 nM.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 08:18:39 UTC 2023` Edited by `admin` on `Sat Dec 16 08:18:39 UTC 2023`
Record UNII	A2EXW95647
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CP-809101

Common Name

English

PYRAZINE, 2-((3-CHLOROPHENYL)METHOXY)-6-(1-PIPERAZINYL)-

Systematic Name

English

6'-(3-CHLOROBENZYLOXY)-3,4,5,6-TETRAHYDRO-2H-(1,2')BIPYRAZINE

Systematic Name

English

Code System Code Type Description

WIKIPEDIA

CP-809101