Altanserin hydrochloride
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MedKoo CAT#: 573701

CAS#: 1135280-78-2

Description: Altanserin hydrochloride is a compound that binds to the 5-HT2A receptor. Labeled with the isotope fluorine-18, it is used as a radioligand in positron emission tomography (PET) studies of the brain.

Chemical Structure

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Altanserin hydrochloride
CAS# 1135280-78-2
Instruction

Theoretical Analysis

MedKoo Cat#: 573701
Name: Altanserin hydrochloride
CAS#: 1135280-78-2
Chemical Formula: C22H23ClFN3O2S
Exact Mass: 447.12
Molecular Weight: 447.950
Elemental Analysis: C, 58.99; H, 5.18; Cl, 7.91; F, 4.24; N, 9.38; O, 7.14; S, 7.16

Price and Availability

Size Price Availability Quantity
10mg USD 330
50mg USD 1075
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Related CAS #: 79449-96-0 (tartrate)   76330-71-7 (free base)  

Synonym: Altanserin hydrochloride, Altanserin HCl

IUPAC/Chemical Name: 4(1H)-Quinazolinone, 3-(2-(4-(4-fluorobenzoyl)-1-piperidinyl)ethyl)-2,3-dihydro-2-thioxo-, hydrochloride (1:1)

InChi Key: JFPPLMAMMZZOEA-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: c1ccc2c(c1)c(=O)n(c(=S)[nH]2)CCN3CCC(CC3)C(=O)c4ccc(cc4)F.Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 447.95 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Kroll T, Elmenhorst D, Matusch A, Celik AA, Wedekind F, Weisshaupt A, Beer S, Bauer A. [¹⁸F]Altanserin and small animal PET: impact of multidrug efflux transporters on ligand brain uptake and subsequent quantification of 5-HT₂A receptor densities in the rat brain. Nucl Med Biol. 2014 Jan;41(1):1-9. doi: 10.1016/j.nucmedbio.2013.09.001. Epub 2013 Oct 9. PubMed PMID: 24120220.

2: Hansen HD, Ettrup A, Herth MM, Dyssegaard A, Ratner C, Gillings N, Knudsen GM. Direct comparison of [(18) F]MH.MZ and [(18) F] altanserin for 5-HT2A receptor imaging with PET. Synapse. 2013 Jun;67(6):328-37. doi: 10.1002/syn.21643. Epub 2013 Mar 7. PubMed PMID: 23390031.

3: Ettrup A, Svarer C, McMahon B, da Cunha-Bang S, Lehel S, Møller K, Dyssegaard A, Ganz M, Beliveau V, Jørgensen LM, Gillings N, Knudsen GM. Serotonin 2A receptor agonist binding in the human brain with [(11)C]Cimbi-36: Test-retest reproducibility and head-to-head comparison with the antagonist [(18)F]altanserin. Neuroimage. 2016 Apr 15;130:167-174. doi: 10.1016/j.neuroimage.2016.02.001. Epub 2016 Feb 11. PubMed PMID: 26876490.

4: Kroll T, Elmenhorst D, Matusch A, Wedekind F, Weisshaupt A, Beer S, Bauer A. Suitability of [18F]altanserin and PET to determine 5-HT2A receptor availability in the rat brain: in vivo and in vitro validation of invasive and non-invasive kinetic models. Mol Imaging Biol. 2013 Aug;15(4):456-67. doi: 10.1007/s11307-013-0621-3. Epub 2013 Mar 1. PubMed PMID: 23456885.

5: Quednow BB, Treyer V, Hasler F, Dörig N, Wyss MT, Burger C, Rentsch KM, Westera G, Schubiger PA, Buck A, Vollenweider FX. Assessment of serotonin release capacity in the human brain using dexfenfluramine challenge and [18F]altanserin positron emission tomography. Neuroimage. 2012 Feb 15;59(4):3922-32. doi: 10.1016/j.neuroimage.2011.09.045. Epub 2011 Oct 5. PubMed PMID: 21996132.

6: Martín A, Szczupak B, Gómez-Vallejo V, Plaza S, Padró D, Cano A, Llop J. PET imaging of serotoninergic neurotransmission with [(11)C]DASB and [(18)F]altanserin after focal cerebral ischemia in rats. J Cereb Blood Flow Metab. 2013 Dec;33(12):1967-75. doi: 10.1038/jcbfm.2013.156. Epub 2013 Aug 28. PubMed PMID: 23982048; PubMed Central PMCID: PMC3851906.

7: Ungersboeck J, Richter S, Collier L, Mitterhauser M, Karanikas G, Lanzenberger R, Dudczak R, Wadsak W. Radiolabeling of [18F]altanserin - a microfluidic approach. Nucl Med Biol. 2012 Oct;39(7):1087-92. doi: 10.1016/j.nucmedbio.2012.04.004. Epub 2012 May 23. PubMed PMID: 22633218.

8: Riss PJ, Hong YT, Williamson D, Caprioli D, Sitnikov S, Ferrari V, Sawiak SJ, Baron JC, Dalley JW, Fryer TD, Aigbirhio FI. Validation and quantification of [18F]altanserin binding in the rat brain using blood input and reference tissue modeling. J Cereb Blood Flow Metab. 2011 Dec;31(12):2334-42. doi: 10.1038/jcbfm.2011.94. Epub 2011 Jul 13. PubMed PMID: 21750562; PubMed Central PMCID: PMC3323196.

9: Pinborg LH, Adams KH, Yndgaard S, Hasselbalch SG, Holm S, Kristiansen H, Paulson OB, Knudsen GM. [18F]altanserin binding to human 5HT2A receptors is unaltered after citalopram and pindolol challenge. J Cereb Blood Flow Metab. 2004 Sep;24(9):1037-45. PubMed PMID: 15356424.

10: Hasler F, Kuznetsova OF, Krasikova RN, Cservenyak T, Quednow BB, Vollenweider FX, Ametamey SM, Westera G. GMP-compliant radiosynthesis of [18F]altanserin and human plasma metabolite studies. Appl Radiat Isot. 2009 Apr;67(4):598-601. doi: 10.1016/j.apradiso.2008.12.007. Epub 2008 Dec 24. PubMed PMID: 19162492.

11: Biver F, Lotstra F, Monclus M, Dethy S, Damhaut P, Wikler D, Luxen A, Goldman S. In vivo binding of [18F]altanserin to rat brain 5HT2 receptors: a film and electronic autoradiographic study. Nucl Med Biol. 1997 May;24(4):357-60. PubMed PMID: 9257335.

12: Price JC, Lopresti BJ, Meltzer CC, Smith GS, Mason NS, Huang Y, Holt DP, Gunn RN, Mathis CA. Analyses of [(18)F]altanserin bolus injection PET data. II: consideration of radiolabeled metabolites in humans. Synapse. 2001 Jul;41(1):11-21. PubMed PMID: 11354009.

13: Pinborg LH, Adams KH, Svarer C, Holm S, Hasselbalch SG, Haugbøl S, Madsen J, Knudsen GM. Quantification of 5-HT2A receptors in the human brain using [18F]altanserin-PET and the bolus/infusion approach. J Cereb Blood Flow Metab. 2003 Aug;23(8):985-96. PubMed PMID: 12902843.

14: Matusch A, Hurlemann R, Rota Kops E, Winz OH, Elmenhorst D, Herzog H, Zilles K, Bauer A. Acute S-ketamine application does not alter cerebral [18F]altanserin binding: a pilot PET study in humans. J Neural Transm (Vienna). 2007;114(11):1433-42. Epub 2007 Jun 1. PubMed PMID: 17541696.

15: Hautzel H, Müller HW, Herzog H, Grandt R. Cognition-induced modulation of serotonin in the orbitofrontal cortex: a controlled cross-over PET study of a delayed match-to-sample task using the 5-HT2a receptor antagonist [18F]altanserin. Neuroimage. 2011 Oct 1;58(3):905-11. doi: 10.1016/j.neuroimage.2011.06.009. Epub 2011 Jun 17. PubMed PMID: 21722741.

16: Kupers R, Frokjaer VG, Naert A, Christensen R, Budtz-Joergensen E, Kehlet H, Knudsen GM. A PET [18F]altanserin study of 5-HT2A receptor binding in the human brain and responses to painful heat stimulation. Neuroimage. 2009 Feb 1;44(3):1001-7. doi: 10.1016/j.neuroimage.2008.10.011. Epub 2008 Oct 28. PubMed PMID: 19007894.

17: Marner L, Frokjaer VG, Kalbitzer J, Lehel S, Madsen K, Baaré WF, Knudsen GM, Hasselbalch SG. Loss of serotonin 2A receptors exceeds loss of serotonergic projections in early Alzheimer's disease: a combined [11C]DASB and [18F]altanserin-PET study. Neurobiol Aging. 2012 Mar;33(3):479-87. doi: 10.1016/j.neurobiolaging.2010.03.023. Epub 2010 May 26. PubMed PMID: 20510480.

18: Kristiansen H, Elfving B, Plenge P, Pinborg LH, Gillings N, Knudsen GM. Binding characteristics of the 5-HT2A receptor antagonists altanserin and MDL 100907. Synapse. 2005 Dec 15;58(4):249-57. PubMed PMID: 16206185.

19: van Dyck CH, Tan PZ, Baldwin RM, Amici LA, Garg PK, Ng CK, Soufer R, Charney DS, Innis RB. PET quantification of 5-HT2A receptors in the human brain: a constant infusion paradigm with [18F]altanserin. J Nucl Med. 2000 Feb;41(2):234-41. PubMed PMID: 10688105.

20: Smith GS, Price JC, Lopresti BJ, Huang Y, Simpson N, Holt D, Mason NS, Meltzer CC, Sweet RA, Nichols T, Sashin D, Mathis CA. Test-retest variability of serotonin 5-HT2A receptor binding measured with positron emission tomography and [18F]altanserin in the human brain. Synapse. 1998 Dec;30(4):380-92. PubMed PMID: 9826230.