5-I-R91150

drugbox
IUPAC_name = 4-amino-N- [1- [3-(4-fluorophenyl)propyl] -4-methylpiperidin-4-yl] -5-iodo-2-methoxybenzamide

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CAS_number = 155928-24-8
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PubChem = 132997
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C=23|H=29|F=1|I=1|N=3|O=2
molecular_weight = 525.398
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5-I-R91150 (or R93274) is a compound that acts as a potent and selective antagonist of 5-HT_2A receptors. [Peremans K, Audenaert K, Coopman F, Jacobs F, Dumont F, Slegers G, Verschooten F, van Bree H, Mertens J, Dierckx R. Regional binding index of the radiolabeled selective 5-HT2A antagonist 123I-5-I-R91150 in the normal canine brain imaged with single photon emission computed tomography. "Veterinary Radiology & Ultrasound". 2003 May-Jun;44(3):344-51. PMID 12816380] Its main application is as its iodine-123 radiolabeled form, in which it can be used in SPECT scanning [Cite journal
author = G. F. Busatto, L. S. Pilowsky, D. C. Costa, J. Mertens, D. Terriere, P. J. Ell, R. Mulligan, M. J. Travis, J. E. Leysen, D. Lui, S. Gacinovic, W. Waddington, A. Lingford-Hughes & R. W. Kerwin
title = Initial evaluation of 123I-5-I-R91150, a selective 5-HT2A ligand for single-photon emission tomography, in healthy human subjects
journal = European Journal of Nuclear Medicine
volume = 24
issue = 2
pages = 119–114
year = 1997
month = February
pmid = 9021107] in human neuroimaging studies, to examine the distribution of the 5-HT_2A receptor subtype in the brain, e.g. with respect to sex and age [Cite journal
author = C. Baeken, H. D'haenen, P. Flamen, J. Mertens, D. Terriere, K. Chavatte, R. Boumon & A. Bossuyt
title = 123I-5-I-R91150, a new single-photon emission tomography ligand for 5-HT2A receptors: influence of age and gender in healthy subjects
journal = European Journal of Nuclear Medicine
volume = 25
issue = 12
pages = 1617–1612
year = 1998
month = December
pmid = 9871092] and in adults with Asperger’s syndrome [Cite journal
author = Declan G. M. Murphy, Eileen Daly, Nicole Schmitz, Fiona Toal, Keiran Murphy, Sarah Curran, Kjell Erlandsson, Jos Eersels, Robert Kerwin, Peter Ell & Michael Travis
title = Cortical serotonin 5-HT2A receptor binding and social communication in adults with Asperger's syndrome: an in vivo SPECT study
journal = The American Journal of Psychiatry
volume = 163
issue = 5
pages = 934–936
year = 2006
month = May
doi = 10.1176/appi.ajp.163.5.934
pmid = 16648340
url = http://ajp.psychiatryonline.org/cgi/content/abstract/163/5/934] or Alzheimer's disease. [Cite journal
author = J. Versijpt, K. J. Van Laere, F. Dumont, Danny Decoo, Marleen Vandecapelle, Patrick Santens, Ingeborg Goethals, K. Audenaert, G. Slegers, Rudi A. Dierckx & Jakob Korf
title = Imaging of the 5-HT_2A system: age-, gender-, and Alzheimer's disease-related findings
journal = Neurobiology of Aging
volume = 24
issue = 4
pages = 553–551
year = 2003
month = July-August
pmid = 12714112
doi = 10.1016/S0197-4580(02)00137-9 ]

An alternative 5-HT_2A receptor ligand also used in neuroimaging is altanserin.

Reference

Further reading

* Cite journal
author = Ana M. Catafau, Monica Danus, Santiago Bullich, Jordi Llop, Javier Perich, Vincent J. Cunningham, Pedro Plaza, Maria M. Penengo, Jos L. H. Eersels, Lisa Squassante, Domenec Ros & Manel Barbanoj
title = Characterization of the SPECT 5-HT2A receptor ligand ¹²³I-R91150 in healthy volunteers: Part 1 — pseudoequilibrium interval and quantification methods
journal = Journal of Nuclear Medicine
volume = 47
issue = 6
pages = 919–918
year = 2006
month = June
pmid = 16741300
url = http://jnm.snmjournals.org/cgi/content/full/47/6/919
* Cite journal
author = Ana M. Catafau, Monica Danus, Santiago Bullich, Gianluca Nucci, Jordi Llop, Sergi Abanades, Vincent J. Cunningham, Jos L. H. Eersels, Javier Pavia & Magi Farre
title = Characterization of the SPECT 5-HT2A receptor ligand 123I-R91150 in healthy volunteers: part 2--ketanserin displacement
journal = Journal of Nuclear Medicine
volume = 47
issue = 6
pages = 929–927
year = 2006
month = June
pmid = 16741301