View source for 5-I-R91150

{{drugbox
| IUPAC_name        = 4-amino-N-[1-[3-(4-fluorophenyl)propyl]-4-methylpiperidin-4-yl]-5-iodo-2-methoxybenzamide
| image             = R93274.png
| width             = 280
| CAS_number        = 155928-24-8
| ATC_prefix        = 
| ATC_suffix        = 
| PubChem           = 132997
| DrugBank          = 
| C=23|H=29|F=1|I=1|N=3|O=2
| molecular_weight  = 525.398
| bioavailability   = 
| protein_bound     = 
| metabolism        = 
| elimination_half-life = 
| excretion         = 
| pregnancy_AU      =  <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US      =  <!-- A / B            / C / D / X -->
| pregnancy_category=  
| legal_AU          =  <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->
| legal_CA          =  <!--             / Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK          =  <!-- GSL         / P       / POM / CD / Class A, B, C -->
| legal_US          =  <!-- OTC                   / Rx-only  / Schedule I, II, III, IV, V -->
| legal_status      = 
| routes_of_administration = 
}}

'''5-I-R91150''' (or '''R93274''') is a compound that acts as a potent and selective [[Antagonist (pharmacology)|antagonist]] of [[5-HT2A receptor|5-HT<sub>2A</sub> receptors]].<ref>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</ref> Its main application is as its [[iodine-123]] [[isotopic labeling|radiolabeled]] form, in which it can be used in [[SPECT]] scanning<ref>{{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
| doi = 10.1007/BF02439542
}}</ref> in human [[neuroimaging]] studies, to examine the distribution of the 5-HT<sub>2A</sub> receptor subtype in the [[brain]], e.g. with respect to [[sex]] and [[ageing|age]]<ref>{{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
| doi = 10.1007/s002590050339
}}</ref>
and in adults with [[Asperger syndrome]]<ref>{{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
}}</ref>
or [[Alzheimer's disease]].<ref>{{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<sub>2A</sub> 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 
}}</ref>

An alternative 5-HT<sub>2A</sub> receptor ligand also used in neuroimaging is [[altanserin]].

==References==
{{Reflist}}

=== 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 <sup>123</sup>I-R91150 in healthy volunteers: Part 1 &mdash; pseudoequilibrium interval and quantification methods
| journal = [[Journal of Nuclear Medicine]]
| volume = 47
| issue = 6
| pages = 919–918
| date = 1 June 2006 
| 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
}}

{{Serotonergics}}

[[Category:Serotonin antagonists]]
[[Category:Organofluorides]]
[[Category:Piperidines]]
[[Category:Benzamides]]
[[Category:Organoiodides]]
[[Category:Phenol ethers]]


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[[Category:2Fix]]