LENPERONE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H23F2NO2
Molecular Weight	371.4203
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

FC1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)C(=O)C3=CC=C(F)C=C3

InChI

InChIKey=WCIBOXFOUGQLFC-UHFFFAOYSA-N

InChI=1S/C22H23F2NO2/c23-19-7-3-16(4-8-19)21(26)2-1-13-25-14-11-18(12-15-25)22(27)17-5-9-20(24)10-6-17/h3-10,18H,1-2,11-15H2

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/559569 | https://www.ncbi.nlm.nih.gov/pubmed/561037 | https://www.ncbi.nlm.nih.gov/pubmed/6147806

Lenperone (AHR 2277), or 4’-fluoro-4 [4-(p-fluorobenzoyl) piperidino] butyrophenone hydrochloride, is an antipsychotic compound which has been shown in preliminary experiments to possess those features essential for neuroleptic activity. Dopamine antagonist.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 2 (5-HT2) receptor 87 Target ID: CHEMBL2093870 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1479590	Antagonist 2778		4.3 nM [Ki]
Dopamine receptor 60 Target ID: CHEMBL2096905 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1302433 \| https://www.ncbi.nlm.nih.gov/pubmed/6147806	Antagonist 2778

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 298 Sources: https://www.ncbi.nlm.nih.gov/pubmed/559569 https://www.ncbi.nlm.nih.gov/pubmed/1091666 https://www.ncbi.nlm.nih.gov/pubmed/812640 https://www.ncbi.nlm.nih.gov/pubmed/4209063	Primary		Approved 8429	Lenperone Approved Use Treatment of acute schizophrenia

PubMed

Title	Date	PubMed
Preliminary evaluation of a new psychotropic drug, lenperone, in the treatment of acute schizophrenia.	1977	559569
Antipsychotic effects, side effects and effective dosis of the butyrophenone lenperone (AHR 2277).	1977	561037

Patents

Sample Use Guides

In Vivo Use Guide

50 hospitalized schizophrenic patients were treated 20-30 days with Lenperone. The therapeutic effective dose was 30-50 mg/day. The highest daily dosage was 90 mg.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

LENPERONE

Official Name

English

LENPERONE [USAN]

Common Name

English

4'-FLUORO-4-(4-(P-FLUOROBENZOYL)PIPERIDINO)BUTYROPHENONE

Systematic Name

English

lenperone [INN]

Common Name

English

Lenperone [WHO-DD]

Common Name

English

1-BUTANONE, 4-(4-(4-FLUOROBENZOYL)-1-PIPERIDINYL)-1-(4-FLUOROPHENYL)-

Systematic Name

English

AHR-2277 FREE BASE

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C29710