Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H22FN3O2S |
Molecular Weight | 411.492 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC=C(C=C1)C(=O)C2CCN(CCN3C(=S)NC4=C(C=CC=C4)C3=O)CC2
InChI
InChIKey=SMYALUSCZJXWHG-UHFFFAOYSA-N
InChI=1S/C22H22FN3O2S/c23-17-7-5-15(6-8-17)20(27)16-9-11-25(12-10-16)13-14-26-21(28)18-3-1-2-4-19(18)24-22(26)29/h1-8,16H,9-14H2,(H,24,29)
Molecular Formula | C22H22FN3O2S |
Molecular Weight | 411.492 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/21996132
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21996132
Altanserin is a potent and selective 5-HT2A receptor antagonist. Serotonin (5-HT) system functioning have been proposed for a variety of psychiatric disorders, but a direct method quantitatively assessing 5-HT release capacity in the living human brain is still lacking. It was suggested that the combination of a dexfenfluramine-induced 5-HT release and subsequent assessment of 5-HT(2A) receptor availability with [(18)F]altanserin by positron emission tomography (PET) was suitable to measure cortical 5-HT release capacity in the human brain. Besides human neuroimaging studies altanserin has also been used in the study of rats.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P28223 Gene ID: 3356.0 Gene Symbol: HTR2A Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/15006678 |
0.3 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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PubMed
Title | Date | PubMed |
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Disturbance of serotonin 5HT2 receptors in remitted patients suffering from hereditary depressive disorder. | 2001 Aug |
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Altered serotonin 2A receptor activity in women who have recovered from bulimia nervosa. | 2001 Jul |
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Analyses of [(18)F]altanserin bolus injection PET data. II: consideration of radiolabeled metabolites in humans. | 2001 Jul |
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Distribution of 5HT2A receptors in the human brain: comparison of data in vivo and post mortem. | 2002 |
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[18F]altanserin binding to human 5HT2A receptors is unaltered after citalopram and pindolol challenge. | 2004 Sep |
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Binding characteristics of the 5-HT2A receptor antagonists altanserin and MDL 100907. | 2005 Dec 15 |
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MR-based automatic delineation of volumes of interest in human brain PET images using probability maps. | 2005 Feb 15 |
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Frontolimbic serotonin 2A receptor binding in healthy subjects is associated with personality risk factors for affective disorder. | 2008 Mar 15 |
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Nigrostriatal upregulation of 5-HT2A receptors correlates with motor dysfunction in progressive supranuclear palsy. | 2009 Jun 15 |
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Time-efficient and convenient synthesis of [(18)F]altanserin for human PET imaging by a new work-up procedure. | 2009 Nov |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21996132
Thirteen healthy male subjects received placebo and single oral doses of 40 mg (n = 6) or 60 mg (n = 7) of the potent 5-HT releaser dexfenfluramine separated by an interval of 14 days. Three further subjects received placebo on both days. Two hours after placebo/drug administration, 250 MBq of the 5-HT(2A) receptor selective PET-radiotracer [(18)F]altanserin was administered intravenously as a 30s bolus.
Route of Administration:
Intravenous
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Apr 02 07:55:24 GMT 2025
by
admin
on
Wed Apr 02 07:55:24 GMT 2025
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Record UNII |
5015H744JQ
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C66885
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C77258
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SUB05375MIG
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DTXSID5043891
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ALTANSERIN
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Related Record | Type | Details | ||
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LABELED -> NON-LABELED | |||
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LABELED -> NON-LABELED | |||
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |