PF-00217830

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C26H30N4O2
Molecular Weight	430.542
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O=C1CCC2=CC=C(OCCCCN3CCN(CC3)C4=CC=CC5=C4C=CC=C5)N=C2N1

InChI

InChIKey=QGNOXTFZOLDODX-UHFFFAOYSA-N

InChI=1S/C26H30N4O2/c31-24-12-10-21-11-13-25(28-26(21)27-24)32-19-4-3-14-29-15-17-30(18-16-29)23-9-5-7-20-6-1-2-8-22(20)23/h1-2,5-9,11,13H,3-4,10,12,14-19H2,(H,27,28,31)

HIDE SMILES / InChI

Molecular Formula	C26H30N4O2
Molecular Weight	430.542
Charge	0
Count

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

Description
Sources: https://adisinsight.springer.com/drugs/800025560 | https://www.pfizer.com/sites/default/files/research/pipeline/2010_0927/pipeline_2010_0927.pdf | https://www.ncbi.nlm.nih.gov/pubmed/21353774

Pfizer was developing NPBN (PF 217830), an orally administered dopamine D2 and serotonin 5-HT1A partial agonist and 5-HT2A antagonist, for the treatment of schizophrenia. PF-217830 was discontinued from development due to either non-optimal pharmacokinetic properties or insufficient therapeutical efficacy.

CNS Activity

Originator

Approval Year

PubMed

Title	Date	PubMed
Comparative pharmacology of antipsychotics possessing combined dopamine D2 and serotonin 5-HT1A receptor properties.	2011 Aug	21394633
Metabolism of a dopamine receptor partial agonist in rats, including an unusual N-dearylation reaction.	2011 Jun	21383524
Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents.	2014	24164194

Patents

Sample Use Guides

In Vivo Use Guide

Schizophrenia: PF 217830 2 mg, oral capsule, once daily for 21 days PF 217830 5 mg, oral capsule, once daily for 21 days PF 217830 15 mg, oral capsule, once daily for 21 days

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 11:06:00 GMT 2023` Edited by `admin` on `Sat Dec 16 11:06:00 GMT 2023`
Record UNII	8BC08N1MS5
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PF-00217830

Common Name

English

1,8-NAPHTHYRIDIN-2(1H)-ONE, 3,4-DIHYDRO-7-(4-(4-(1-NAPHTHALENYL)-1-PIPERAZINYL)BUTOXY)-

Systematic Name

English

NPBN

Common Name

English

3,4-DIHYDRO-7-(4-(1-NAPHTHALENYL)-1-PIPERAZINYL)BUTOXY)-1,8-NAPHTHYRIDIN-2(1H)-ONE

Systematic Name

English

3,4-DIHYDRO-7-(4-(4-(1-NAPHTHYL)PIPERAZINO)BUTOXY)-1,8-NAPHTHYRIDINE-2(1H)-ONE

Systematic Name

English

PF-217830

Code

English

J2.975.999E

Code

English

Code System Code Type Description

DRUG BANK

DB12998