LUSAPERIDONE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H21N3O2
Molecular Weight	359.421
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=C(CCN2CCC3=C(C2)C4=C(O3)C=CC=C4)C(=O)N5C=CC=CC5=N1

InChI

InChIKey=ZYXHQIPQIKTEDI-UHFFFAOYSA-N

InChI=1S/C22H21N3O2/c1-15-16(22(26)25-11-5-4-8-21(25)23-15)9-12-24-13-10-20-18(14-24)17-6-2-3-7-19(17)27-20/h2-8,11H,9-10,12-14H2,1H3

HIDE SMILES / InChI

Molecular Formula	C22H21N3O2
Molecular Weight	359.421
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/16517171 | https://www.sciencedirect.com/science/article/pii/S0960894X99005910

Lusaperidone (R107474) is a potent and relatively selective alpha(2)-adrenoceptor antagonist. It was under clinical evaluation for the treatment of depression, characterized by anergia and lack of drive. However, further clinical development has been stopped. Radiolabeled lusaperidone may be used as a potential radioligand for studying alpha(2)-adrenoceptors using PET.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Alpha-2A adrenergic receptor 26 Target ID: P08913 Gene ID: 150.0 Gene Symbol: ADRA2A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/16517171	Antagonist 2778	0.13 nM [Ki]
Alpha-2C adrenergic receptor 11 Target ID: P18825 Gene ID: 152.0 Gene Symbol: ADRA2C Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/16517171	Antagonist 2778	0.15 nM [Ki]
Alpha-2B adrenergic receptor 13 Target ID: P18089 Gene ID: 151.0 Gene Symbol: ADRA2B Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/16517171	Antagonist 2778	1.0 nM [Ki]

PubMed

Title	Date	PubMed
Synthesis and biodistribution of [11C]R107474, a new radiolabeled alpha2-adrenoceptor antagonist.	2006 Jul 1	16517171

Substance Class	Chemical Created by `admin` on `Sat Dec 16 16:19:41 GMT 2023` Edited by `admin` on `Sat Dec 16 16:19:41 GMT 2023`
Record UNII	5KTD2O86CB
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LUSAPERIDONE

Official Name

English

3-(2-(3,4-DIHYDROBENZOFURO(3,2-C)PYRIDIN-2(1H)-YL)ETHYL)-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ONE

Systematic Name

English

lusaperidone [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29710