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5-I-R91150
Systematic (IUPAC) name
4-amino-N-[1-[3-(4-fluorophenyl)propyl]-4-methylpiperidin-4-yl]-5-iodo-2-methoxybenzamide
Identifiers
CAS number 155928-24-8
ATC code  ?
PubChem 132997
Chemical data
Formula C 23H29FIN3O2  
Mol. mass 525.398
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

5-I-R91150 (or R93274) is a compound that acts as a potent and selective antagonist of 5-HT2A receptors.[1] Its main application is as its iodine-123 radiolabeled form, in which it can be used in SPECT scanning[2] in human neuroimaging studies, to examine the distribution of the 5-HT2A receptor subtype in the brain, e.g. with respect to sex and age[3] and in adults with Asperger syndrome[4] or Alzheimer's disease.[5]

An alternative 5-HT2A receptor ligand also used in neuroimaging is altanserin.

References

  1. ^ 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
  2. ^ 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 (February 1997). "Initial evaluation of 123I-5-I-R91150, a selective 5-HT2A ligand for single-photon emission tomography, in healthy human subjects". European Journal of Nuclear Medicine 24 (2): 119–114. doi:10.1007/BF02439542. PMID 9021107.  
  3. ^ C. Baeken, H. D'haenen, P. Flamen, J. Mertens, D. Terriere, K. Chavatte, R. Boumon & A. Bossuyt (December 1998). "123I-5-I-R91150, a new single-photon emission tomography ligand for 5-HT2A receptors: influence of age and gender in healthy subjects". European Journal of Nuclear Medicine 25 (12): 1617–1612. doi:10.1007/s002590050339. PMID 9871092.  
  4. ^ Declan G. M. Murphy, Eileen Daly, Nicole Schmitz, Fiona Toal, Keiran Murphy, Sarah Curran, Kjell Erlandsson, Jos Eersels, Robert Kerwin, Peter Ell & Michael Travis (May 2006). "Cortical serotonin 5-HT2A receptor binding and social communication in adults with Asperger's syndrome: an in vivo SPECT study". The American Journal of Psychiatry 163 (5): 934–936. doi:10.1176/appi.ajp.163.5.934. PMID 16648340. http://ajp.psychiatryonline.org/cgi/content/abstract/163/5/934.  
  5. ^ 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 (July-August 2003). "Imaging of the 5-HT2A system: age-, gender-, and Alzheimer's disease-related findings". Neurobiology of Aging 24 (4): 553–551. doi:10.1016/S0197-4580(02)00137-9. PMID 12714112.  
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