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
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
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
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P08913 Gene ID: 150.0 Gene Symbol: ADRA2A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/16517171 |
0.13 nM [Ki] | ||
Target ID: P18825 Gene ID: 152.0 Gene Symbol: ADRA2C Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/16517171 |
0.15 nM [Ki] | ||
Target ID: P18089 Gene ID: 151.0 Gene Symbol: ADRA2B Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/16517171 |
1.0 nM [Ki] |
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NCI_THESAURUS |
C29710
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ACTIVE MOIETY