5-I-R91150
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| Systematic (IUPAC) name | |
| 4-amino-N-[1-[3-(4-fluorophenyl)propyl]-4-methylpiperidin-4-yl]-5-iodo-2-methoxybenzamide | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 155928-24-8 |
| ATC code | ? |
| PubChem | CID 132997 |
| ChemSpider | 117371  |
| Chemical data | |
| Formula | C23H29FIN3O2 |
| Mol. mass | 525.398 |
| SMILES | eMolecules & PubChem |
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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.
[edit] References
- ^ Peremans, K; Audenaert, K; Coopman, F; Jacobs, F; Dumont, F; Slegers, G; Verschooten, F; Van Bree, H et al. (2003). "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 : the official journal of the American College of Veterinary Radiology and the International Veterinary Radiology Association 44 (3): 344–51. PMID 12816380.
- ^ Busatto, Geraldo F.; Pilowsky, Lyn S.; Costa, Durval C.; Mertehs, John; Terriere, Dirk; Ell, Peter J.; Mulligan, Rachel; Travis, Michael J. et al. (1997). "Initial evaluation of123". European Journal of Nuclear Medicine 24 (2): 119–124. doi:10.1007/BF02439542. PMID 9021107.
- ^ Baeken, Chris; d'Haenen, Hugo; Flamen, Patrick; Mertens, John; Terriere, Dirk; Chavatte, Kris; Boumon, Rony; Bossuyt, Axel (1998). "123 I-5-I-R91150, a new single-photon emission tomography ligand for 5-HT 2A receptors: Influence of age and gender in healthy subjects". European Journal of Nuclear Medicine and Molecular Imaging 25 (12): 1617–1622. doi:10.1007/s002590050339.
- ^ Murphy, D. G.M.; Daly, E.; Schmitz, N.; Toal, F.; Murphy, K.; Curran, S.; Erlandsson, K.; Eersels, J. et al. (2006). "Cortical Serotonin 5-HT2A Receptor Binding and Social Communication in Adults with Asperger's Syndrome: An in Vivo SPECT Study". 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.
- ^ Versijpt, J.; Van Laere, K.J.; Dumont, F.; Decoo, Danny; Vandecapelle, Marleen; Santens, Patrick; Goethals, Ingeborg; Audenaert, K. et al. (2003). "Imaging of the 5-HT2A system: Age-, gender-, and Alzheimer's disease-related findings". Neurobiology of Aging 24 (4): 553–561. doi:10.1016/S0197-4580(02)00137-9. PMID 12714112.
[edit] Further reading
- Catafau, AM; Danus, M; Bullich, S; Llop, J; Perich, J; Cunningham, VJ; Plaza, P; Penengo, MM et al. (2006). "Characterization of the SPECT 5-HT2A receptor ligand 123I-R91150 in healthy volunteers: Part 1--pseudoequilibrium interval and quantification methods". Journal of nuclear medicine : official publication, Society of Nuclear Medicine 47 (6): 919–28. PMID 16741300. http://jnm.snmjournals.org/cgi/content/full/47/6/919.
- Catafau, AM; Danus, M; Bullich, S; Nucci, G; Llop, J; Abanades, S; Cunningham, VJ; Eersels, JL et al. (2006). "Characterization of the SPECT 5-HT2A receptor ligand 123I-R91150 in healthy volunteers: Part 2--ketanserin displacement". Journal of nuclear medicine : official publication, Society of Nuclear Medicine 47 (6): 929–37. PMID 16741301.
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