Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H22FN3O2S.ClH |
| Molecular Weight | 447.953 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.FC1=CC=C(C=C1)C(=O)C2CCN(CCN3C(=S)NC4=C(C=CC=C4)C3=O)CC2
InChI
InChIKey=JFPPLMAMMZZOEA-UHFFFAOYSA-N
InChI=1S/C22H22FN3O2S.ClH/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);1H
| 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 |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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
PubMed
| Title | Date | PubMed |
|---|---|---|
| Disturbance of serotonin 5HT2 receptors in remitted patients suffering from hereditary depressive disorder. | 2001 Aug |
|
| Distribution of 5HT2A receptors in the human brain: comparison of data in vivo and post mortem. | 2002 |
|
| Reduced 5-HT2A receptor binding after recovery from anorexia nervosa. | 2002 Nov 1 |
|
| Increase in prefrontal cortex serotonin 2A receptors following estrogen treatment in postmenopausal women. | 2003 Aug |
|
| Influence of synaptic serotonin level on [18F]altanserin binding to 5HT2 receptors in man. | 2003 Feb 17 |
|
| Binding characteristics of the 5-HT2A receptor antagonists altanserin and MDL 100907. | 2005 Dec 15 |
|
| No-carrier-added nucleophilic 18F-labelling in an electrochemical cell exemplified by the routine production of [18F]altanserin. | 2006 Sep |
|
| Cerebral 5-HT2A receptor binding is increased in patients with Tourette's syndrome. | 2007 Apr |
|
| Reproducibility of 5-HT2A receptor measurements and sample size estimations with [18F]altanserin PET using a bolus/infusion approach. | 2007 Jun |
|
| 5HT2A receptor binding is increased in borderline personality disorder. | 2007 Sep 15 |
|
| Assessment of the Potential Role of Tryptophan as the Precursor of Serotonin and Melatonin for the Aged Sleep-wake Cycle and Immune Function: Streptopelia Risoria as a Model. | 2009 |
|
| Time-efficient and convenient synthesis of [(18)F]altanserin for human PET imaging by a new work-up procedure. | 2009 Nov |
|
| Gender, personality, and serotonin-2A receptor binding in healthy subjects. | 2010 Jan 30 |
|
| Cerebral 5-HT2A receptor and serotonin transporter binding in humans are not affected by the val66met BDNF polymorphism status or blood BDNF levels. | 2010 Nov |
|
| Evaluation of [(11)C]metergoline as a PET radiotracer for 5HTR in nonhuman primates. | 2010 Nov 15 |
|
| Structural combination of established 5-HT(2A) receptor ligands: new aspects of the binding mode. | 2010 Oct |
|
| Endogenous plasma estradiol in healthy men is positively correlated with cerebral cortical serotonin 2A receptor binding. | 2010 Oct |
Patents
Sample Use Guides
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
Sat Dec 16 01:27:28 GMT 2023
by
admin
on
Sat Dec 16 01:27:28 GMT 2023
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| Record UNII |
XUL9717F5K
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| Record Status |
Validated (UNII)
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| Record Version |
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