Altanserin

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Altanserin
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PubChem CID
E number{{#property:P628}}
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FormulaC22H22FN3O2S
Molar mass411.49[1]

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Altanserin is a compound that binds to the 5-HT2A receptor (serotonin 2A receptor). It is a yellowish solid.[1] Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain, i.e., studies of the serotonin-2A neuroreceptors. Besides human neuroimaging studies altanserin has also been used in the study of rats.[2][3]

An alternative for PET imaging the 5-HT2A receptor is the [11C]MDL 100,907 radioligand. Fluorine-18-altanserin and tritium-MDL 100,907 have shown very comparable binding.[4] Both altanserin and MDL 100,907 are 5-HT2A receptor antagonists.[4] [18F]-setoperone can also be used in PET.

An alternative SPECT radioligand is the [123I]-5-I-R91150 receptor antagonist.[5]

A rapid chemical synthesis of fluorine-18 and H-2 dual-labeled altanserin has been described.[6]

Other ligands for other parts of the serotonin system used in PET studies are, e.g., DASB, ketanserin and WAY-100635.

Human brain mapping studies with altanserin

A PET scanner. Human experiments with fluorine-18 altanserin are performed in these types of brain scanners.

As of 2007 altanserin is probably not used in clinical routine. However, there have been performed several research-based neuroimaging studies with the compound in humans since the 1990s.[7][8] Some of these studies have considered methodogical issues such as the reproducibility of the method[9][10] or whether to use constant infusion[11] or bolus-infusion[12] delivery of altanserin. Other studies have compared altanserin binding to subject variables such as age, personality trait and neuropsychiatric disorder.

The altanserin PET scan shows high binding in neocortex. The cerebellum is often regarded as a region with no specific 5-HT2A binding and the brain region is used as a reference in some studies, even though an autoradiography study has found nonnegligible levels of 5-HT2A binding in the human cerebellum,[13] and another type of study have observed strong immunoreaction against 5-HT2A receptor protein in rat Purkinje cells.[14]

In the table below is an overview of the results of altanserin binding seen in human PET-studies. A consistent finding across altanserin studies has been that the binding decreases with age. This is in line with in vitro studies of the 5-HT2A receptor,[15] as well as PET studies with other radioligands that binds to the receptor.[16]

The result for recovered bulimia-type anorexia nervosa[17] is in line with a SPECT study of anorexia nervosa patients, that found a decrease in frontal, occipital and parietal cortices.[5] The results of PET studies of the 5-HT2A in depression has been mixed.[18]

Altanserin binding has also been examine in twins, where one study showed higher correlation between monozygotic twin pairs than between dizygotic twin pairs, giving evidence that the binding is "strongly genetically determined".[19]

Altanserin neuroimaging studies
What Result Reference
Sex Higher binding in men [20]
Neuroticism (NEO PI-R) Increase in frontolimbic region [21]
Tourette syndrome Increase [22]
Obsessive-compulsive disorder Increase in caudate nuclei [23]
(Recovered) bulimia-type anorexia nervosa Decrease in left subgenual cingulate, left parietal cortex and right occipital cortex [17]
Unipolar depression Decrease in a region in right hemisphere (posterolateral orbitofrontal cortex and the anterior insular cortex) [24]
Major depressive disorder Decrease in hippocampus [25]
Older depressed patients Decrease in hippocampus [26]
Borderline personality disorder Increase in hippocampus [27]
Schizophrenia No significant cortical difference, higher binding in caudate [28]
At-risk mental state Decrease [29] See also [30]
Age Decrease [31]
Age Decrease [32]
Age Decrease in cortical regions (except occipital), increase in cerebellum [33]
Mild cognitive impairment Decrease [34]
Alzheimer's disease Decrease in amygdalo-hippocampal complex and cortical regions, such as anterior cingulate, lateral temporal cortex, prefrontal cortex and sensorimotor cortex [35]

References

  1. ↑ 1.0 1.1 ABX, Altanserin, Radeberg, Germany.
  2. ↑ Christian Lemaire, R. Cantineau, M. Guillaume, A. Plenevaux, Leon Christiaens (1991). "Fluorine-18-altanserin: a radioligand for the study of serotonin receptors with PET: radiolabeling and in vivo biologic behavior in rats". Journal of Nuclear Medicine. 32: 2266&ndash, 2277. PMID 1744713. Unknown parameter |month= ignored (help)
  3. ↑ F. Biver, F. Lotstra, M. Monclus, S. Dethy, P. Damhaut, D. Wikler, A. Luxen and S. Goldman (1997). "In vivo binding of [18F]altanserin to rat brain 5HT2 receptors: A film and electronic autoradiographic study". Nuclear Medicine and Biology. 24 (4): 357&ndash, 360. doi:10.1016/S0969-8051(97)00054-1. PMID 9257335. Unknown parameter |month= ignored (help)
  4. ↑ 4.0 4.1 Heidi Kristiansen, Bettina Elfving, Per Plenge, Lars H. Pinborg, Nic Gillings & Gitte Moos Knudsen (2005). "Binding characteristics of the 5-HT2A receptor antagonists altanserin and MDL 100907". Synapse. 58 (4): 249&ndash, 257. doi:10.1002/syn.20205. Unknown parameter |month= ignored (help)
  5. ↑ 5.0 5.1 Kurt Audenaert, Koen Van Laere, Filip Dumont, Miriam Vervaet, Ingeborg Goethals, Guido Slegers, John Mertens, Cees van Heeringen, Rudi A. Dierckx. "Decreased 5-HT2A Receptor Binding in Patients with Anorexia Nervosa". Journal of Nuclear Medicine. 44: 163&ndash, 169.
  6. ↑ Ping-Zhong Tan, Ronald M. Baldwin, Tao Fu, Dennis S. Charney, Robert B. Innis (1999). "Rapid synthesis of F-18 and H-2 dual-labeled altanserin, a metabolically resistant PET ligand for 5-HT2a receptors". Journal of Labelled Compounds and Radiopharmaceuticals. 42 (5): 457&ndash, 467. doi:10.1002/(SICI)1099-1344(199905)42:5<457::AID-JLCR206>3.0.CO;2-0. Unknown parameter |doilabel= ignored (help); Unknown parameter |month= ignored (help)
  7. ↑ Frangoise Biver, Serge Goldman, André Luxen, Michel Monclus, Manuel Forestini, Julien Mendlewicz and Françoise Lotstra (1994). "Multicompartmental study of fluorine-18 altanserin binding to brain 5HT2 receptors in humans using positron emission tomography". European Journal of Nuclear Medicine and Molecular Imaging. 21 (9): 937&ndash, 946. doi:10.1007/BF00238117. Unknown parameter |month= ignored (help)
  8. ↑ Sadzot B, Lemaire C, Maquet P, Salmon E, Plenevaux A, Degueldre C, Hermanne JP, Guillaume M, Cantineau R, Comar D; et al. (1995). "Serotonin 5HT2 receptor imaging in the human brain using positron emission tomography and a new radioligand, [18F]altanserin: results in young normal controls". Journal of Cerebral Blood Flow and Metabolism. 15 (5): 787&ndash, 797. PMID 7673371. Unknown parameter |month= ignored (help)
  9. ↑ Gwenn S. Smith, Julie C. Price, Brian J. Lopresti, Yiyun Huang, Norman Simpson, Daniel Holt, N. Scott Mason, Carolyn Cidis Meltzer, Robert A. Sweet, Thomas Nichols, Donald Sashin, Chester A. Mathis (1998). "Test-retest variability of serotonin 5-HT2A receptor binding measured with positron emission tomography and [18F]altanserin in the human brain". Synapse. 30 (4): 380&ndash, 392. doi:10.1002/(SICI)1098-2396(199812)30:4<380::AID-SYN5>3.0.CO;2-U. Unknown parameter |doilabel= ignored (help)
  10. ↑ Steven Haugbøl, Lars H. Pinborg, Haroon M. Arfan, Vibe Frøkjær, Jacob Madsen, Tim B. Dyrby, Claus Svarer and Gitte M. Knudsen (2007). "Reproducibility of 5-HT2A receptor measurements and sample size estimations with [18F]altanserin PET using a bolus/infusion approach". European Journal of Nuclear Medicine and Molecular Imaging. 34 (6): 910&ndash, 915. doi:10.1007/s00259-006-0296-y. Unknown parameter |month= ignored (help)
  11. ↑ Christopher H. van Dyck, Ping-Zhong Tan, Ronald M. Baldwin, Louis A. Amici, Pradeep K. Garg, Chin K. Ng, Robert Soufer, Dennis S. Charney and Robert B. Innis. "PET Quantification of 5-HT2A Receptors in the Human Brain: A Constant Infusion Paradigm with [18F]Altanserin". The Journal of Nuclear Medicine. 41 (2): 234&ndash, 241. PMID 10688105.
  12. ↑ Lars H Pinborg, Karen H Adams, Claus Svarer, Søren Holm*, Steen G Hasselbalch, Steven Haugbøl, Jacob Madsen and Gitte M Knudsen (2003). "Quantification of 5-HT2A Receptors in the Human Brain Using [18F]Altanserin-PET and the Bolus/Infusion Approach". Journal of Cerebral Blood Flow & Metabolism. 23: 985&ndash, 996. doi:10.1097/01.WCB.0000074092.59115.23.
  13. ↑ Sharon L. Eastwood, Philip W. J. Burnet, Rebecca Gittins, Kate Baker, Paul J. Harrison (2001). "Expression of serotonin 5-HT2A receptors in the human cerebellum and alterations in schizophrenia". Synapse. 42 (2): 104&ndash, 114. doi:10.1002/syn.1106. Unknown parameter |month= ignored (help)
  14. ↑ Toru Maeshima, Fumihiro Shutoh, Shun Hamada, Kouji Senzaki, Kayoko Hamaguchi-Hamada, Ryuzo Ito, Nobuo Okado (1998). "Serotonin2A receptor-like immunoreactivity in rat cerebellar Purkinje cells". Neuroscience Letters. 252 (1): 72&ndash, 74. doi:10.1016/S0304-3940(98)00546-1. PMID 9756362. Unknown parameter |month= ignored (help)
  15. ↑ Jan O. Marcusson, David G. Morgan, Bengt Winblad, Caleb E. Finch (1984). "Serotonin-2 binding sites in human frontal cortex and hippocampus. Selective loss of S-2A sites with age". Brain Research. 311 (1): 51&ndash, 56. doi:10.1016/0006-8993(84)91397-0. PMID 6488044. Unknown parameter |month= ignored (help)
  16. ↑ D. F. Wong, H. N. Wagner Jr, R. F. Dannals, J. M. Links, J. J. Frost, H. T. Ravert, A. A. Wilson, A. E. Rosenbaum, Albert Gjedde, K. H. Douglass; et al. (1984). "Effects of age on dopamine and serotonin receptors measured by positron tomography in the living human brain". Science. 226 (4681): 1393&ndash, 1396. doi:10.1126/science.6334363. Unknown parameter |month= ignored (help)
  17. ↑ 17.0 17.1 Ursula F. Bailer, Julie C. Price, Carolyn C. Meltzer, Chester A. Mathis, Guido K. Frank, Lisa Weissfeld, Claire W. McConaha, Shannan E. Henry, Sarah Brooks-Achenbach, Nicole C. Barbarich, and Walter H. Kaye (2004). "Altered 5-HT2A receptor binding after recovery from bulimia-type anorexia nervosa: Relationships to harm avoidance and drive for thinness" (PDF). Neuropsychopharmacology. 29: 1143&ndash, 1155. doi:10.1038/sj.npp.1300430.
  18. ↑ Masahiro Fujita, Dennis S. Charneya, c and Robert B. Innis (2000). "Imaging serotonergic neurotransmission in depression: hippocampal pathophysiology may mirror global brain alterations". Biological Psychiatry. 48 (8): 801&ndash, 812. doi:10.1016/S0006-3223(00)00960-4. Unknown parameter |month= ignored (help)
  19. ↑ Lars H. Pinborg, Haroon Arfan, Steven Haugbol, Kirsten Ohm Kyvik, Jacob V. B. Hjelmborg, Claus Svarer, Vibe G. Frokjaer, Olaf B. Paulson, Soren Holm & Gitte M. Knudsen (2008). "The 5-HT2A receptor binding pattern in the human brain is strongly genetically determined". NeuroImage. 40 (3): 1175–1170. doi:10.1016/j.neuroimage.2007.09.019. PMID 18291676. Unknown parameter |month= ignored (help)
  20. ↑ Françoise Biver, Françoise Lotstra, Michel Monclus, David Wikler, Philippe Damhaut, Julien Mendlewicz and Serge Goldman (1996). "Sex difference in 5HT2 receptor in the living human brain". Neuroscience Letters. 204: 25&ndash, 28. doi:10.1016/0304-3940(96)12307-7. PMID 8929969. Unknown parameter |month= ignored (help); Unknown parameter |issues= ignored (help)
  21. ↑ Vibe G. Frøkjær, Erik Lykke Mortensen, Finn Årup Nielsen, Steven Haugbøl, Lars H Pinborg, Karen H. Adams, Claus Svarer, Steen G. Hasselbalch, Søren Holm, Olaf B. Paulson, Gitte Moos Knudsen (2008). "Frontolimbic Serotonin 2A Receptor Binding in Healthy Subjects Is Associated with Personality Risk Factors for Affective Disorder". Biological Psychiatry. 63: 569. doi:10.1016/j.biopsych.2007.07.009. PMID 17884017.
  22. ↑ Steven Haugbøl, Lars H. Pinborg, Lisbeth Regeur, Elsebet S. Hansen, Tom G. Bolwig, Finn Årup Nielsen, Claus Svarer, Lene T. Skovgaardand Gitte M. Knudsen (2008). "Cerebral 5-HT2A receptor binding is increased in patients with Tourette's syndrome". The International Journal of Neuropsychopharmacology. 63: 569. doi:10.1017/S1461145706006559.
  23. ↑ K. H. Adams, E. S. Hansen, L. H. Pinborg, S. G. Hasselbalch, C. Svarer, S. Holm, Tom G. Bolvig & Gitte Moos Knudsen (2005). "Patients with obsessive-compulsive disorder have increased 5-HT2A receptor binding in the caudate nuclei". International Journal of Neuropsychopharmacology. 8 (3): 391&ndash, 401. doi:10.1017/S1461145705005055. PMID 15801987. Unknown parameter |month= ignored (help)
  24. ↑ F. Biver, D. Wikler, F. Lotstra, P. Damhaut, S. Goldman, J. Mendlewicz (1997). "Serotonin 5-HT2 receptor imaging in major depression: focal changes in orbito-insular cortex". British Journal of Psychiatry. 171: 444&ndash, 448. PMID 9463603. Unknown parameter |month= ignored (help)
  25. ↑ Mark A. Mintun, Yvette I. Sheline, Stephen M. Moerlein, Andrei G. Vlassenko, Yiyun Huang and Abraham Z. Snyder (2004). "Decreased hippocampal 5-HT2A receptor binding in major depressive disorder: in vivo measurement with [18F]altanserin positron emission tomography". Biological Psychiatry. 55 (3): 217&ndash, 224. doi:10.1016/j.biopsych.2003.08.015. Unknown parameter |month= ignored (help)
  26. ↑ Yvette I. Sheline, Mark A Mintun, Deanna M. Barch, Consuelo Wilkins, Abraham Z. Snyder & Stephen M. Moerlein (2004). "Decreased hippocampal 5-HT2A receptor binding in older depressed patients using [18F]altanserin positron emission tomography". Neuropsychopharmacology. 29 (12): 2235&ndash, 2241. doi:10.1038/sj.npp.1300555. Unknown parameter |month= ignored (help)
  27. ↑ P. Soloff, J. Price, C. Meltzer, A. Fabio, G. Frank, W. Kaye (2007). "5HT2A Receptor Binding is Increased in Borderline Personality Disorder". Biological Psychiatry. 62 (6): 580–587. doi:10.1016/j.biopsych.2006.10.022.
  28. ↑ David Erritzoe, Hans Rasmussen, Klaus T. Kristiansen, Vibe G. Frøkjær, Steven Haugbøl, Lars Pinborg, William Baaré, Claus Svarer, Jacob Madsen, Henrik Lublin, Gitte Moos Knudsen & Birte Y. Glenthøj (2008). "Cortical and Subcortical 5-HT2A Receptor Binding in Neuroleptic-Naive First-Episode Schizophrenic Patients". Neuropsychopharmacology. 62: 580. doi:10.1038/sj.npp.1301656. PMID 18288096. Unknown parameter |month= ignored (help) Electronic publication ahead of print
  29. ↑ René Hurlemann, Andreas Matusch, Kai-Uwe Kuhn, Julia Berning, David Elmenhorst, Oliver Winz, Heike Kolsch, Karl Zilles, Michael Wagner, Wolfgang Maier and Andreas Bauer (2008). "5-HT2A receptor density is decreased in the at-risk mental state". Psychopharmacology. 195 (4): 579&ndash, 590. doi:10.1007/s00213-007-0921-x. PMID 17899021. Unknown parameter |month= ignored (help)
  30. ↑ René Hurlemann, Christian Boy, Philipp T. Meyer, Harald Scherk, Michael Wagner, Hans Herzog, Heinz H. Coenen, Kai Vogeley, Peter Falkai, Karl Zilles, Wolfgang Maier and Andreas Bauer (2005). "Decreased prefrontal 5-HT2A receptor binding in subjects at enhanced risk for schizophrenia". Anatomy and Embryology. 210 (5–6): 519&ndash, 523. doi:10.1007/s00429-005-0036-2. PMID 16187138. Unknown parameter |month= ignored (help)
  31. ↑ A. Rosier, P. Dupont, J. Peuskens, G. Bormans, R. Vandenberghe, M. Maes, T. de Groot, C. Schiepers, A. Verbruggen, L. Mortelmans (1996). "Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using [18F]altanserin and positron emission tomographic imaging". Psychiatry Research. 68 (1): 11&ndash, 22. doi:10.1016/S0925-4927(96)02806-5. PMID 9027929. Unknown parameter |month= ignored (help)
  32. ↑ Carolyn Cidis Meltzer, Gwenn Smith, Julie C. Price, Charles F. Reynolds III, Chester A. Mathis, , Phil Greer, Brian Lopresti, Mark A. Mintun, Bruce G. Pollock, Doron Ben-Eliezer, Michael N. Cantwell, Walter Kaye and Steven T. DeKosky (1998). "Reduced binding of [18F]altanserin to serotonin type 2A receptors in aging: persistence of effect after partial volume correction". Brain Research. 813 (1): 167&ndash, 171. doi:10.1016/S0006-8993(98)00909-3. Unknown parameter |month= ignored (help)
  33. ↑ K. H. Adams, Lars H. Pinborg, Claus Svarer, S. G. Hasselbalch, Søren Holm, S. Haugbøl, K. Madsen, Vibe G. Frøkjaer, L. Martiny, Olaf B. Paulson, Gitte Moos Knudsen (2004). "A database of [18F]-altanserin binding to 5-HT2A receptors in normal volunteers: normative data and relationship to physiological and demographic variables". Neuroimage. 21 (3): 1105&ndash, 1113. doi:10.1016/j.neuroimage.2003.10.046. PMID 15006678. Unknown parameter |month= ignored (help)
  34. ↑ Hasselbalch SG, Madsen K, Svarer C, Pinborg LH, Holm S, Olaf B. Paulson, Waldemar G, Gitte Moos Knudsen (2007). "Reduced 5-HT2A receptor binding in patients with mild cognitive impairment". Neurobiology of Aging. doi:10.1016/j.neurobiolaging.2007.04.011. PMID 17544547.
  35. ↑ Carolyn Cidis Meltzer, Julie C. Price, Chester A. Mathis, Phil J. Greer, Michael N. Cantwell, Patricia R. Houck, Benoit H. Mulsant, Doron Ben-Eliezer, Brian Lopresti, Steven T. DeKosky, and Charles F. Reynolds, III (1999). "PET Imaging of Serotonin Type 2A Receptors in Late-Life Neuropsychiatric Disorders". The American Journal of Psychiatry. 156: 1871&ndash, 1878. PMID 10588399. Unknown parameter |month= ignored (help)

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