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123I-5-I-R91150, a new-single-photon emission tomography ligand for 5-HT2A receptors: influence of age and gender in healthy subjects

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Abstract
5-HT2A receptors have been implicated in the pathophysiology of mood disorders and in the therapeutic effect of the so-called atypical antipsychotics. Recently, a new radioiodinated ligand with high affinity and selectivity for serotonin 5-HT2A receptors, (123)iodinated 4-amino-N-1-[3 -(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl] 5-iodo-2-methoxybenzamide (I-123-5-I-R91150), has been developed and has been shown to be suitable for single-photon emission tomography (SPET) imaging. In this study the influence of age and gender on the ligand binding was investigated in normal volunteers. One hundred and fifty MBq of I-123-5-I-R91150 was administered to 26 normal volunteers (13 females and 13 males) with an age range of 23-60 years. SPET imaging was performed with a triple-headed gamma camera. For semi-quantitative analysis, ratios of ligand binding in different regions of interest to the binding in the cerebellum were calculated. Mean ratios of 1.7 were obtained. No gender difference was demonstrated. 5-HT2A binding was shown to decline with age. Over an age range of 40 years a reduction in ligand binding of 42%+/-7% was found. These results are in agreement with in vitro and positron emission tomography findings of a decline in 5-HT2A receptor binding with age. The findings confirm the suitability of I-123-5-I-R91150 for SPET imaging of 5-HT2A receptors, and highlight the necessity for age-matched controls in clinical studies.
Keywords
new tracer, 5-HT2A receptors, I-123-5-I-R91150, single-photon emission tomography, HUMAN BRAIN POSTMORTEM, ALZHEIMERS-DISEASE, AUTORADIOGRAPHIC ANALYSIS, H-3 KETANSERIN, SEROTONIN, BINDING, DEPRESSION, DEMENTIA, SUICIDE, CORTEX

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MLA
Baeken, Chris, Hugo D’Haenen, John Mertens, et al. “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 (1998): 1617–1622. Print.
APA
Baeken, C., D’Haenen, H., Mertens, J., Terriere, D., Chavatte, K., Boumon, R., & Bossuyt, A. (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), 1617–1622.
Chicago author-date
Baeken, Chris, Hugo D’Haenen, John Mertens, Dirk Terriere, Kris Chavatte, Rony Boumon, and Axel Bossuyt. 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): 1617–1622.
Chicago author-date (all authors)
Baeken, Chris, Hugo D’Haenen, John Mertens, Dirk Terriere, Kris Chavatte, Rony Boumon, and Axel Bossuyt. 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): 1617–1622.
Vancouver
1.
Baeken C, D’Haenen H, Mertens J, Terriere D, Chavatte K, Boumon R, et al. 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. 1998;25(12):1617–22.
IEEE
[1]
C. Baeken et al., “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, vol. 25, no. 12, pp. 1617–1622, 1998.
@article{4222727,
  abstract     = {5-HT2A receptors have been implicated in the pathophysiology of mood disorders and in the therapeutic effect of the so-called atypical antipsychotics. Recently, a new radioiodinated ligand with high affinity and selectivity for serotonin 5-HT2A receptors, (123)iodinated 4-amino-N-1-[3 -(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl] 5-iodo-2-methoxybenzamide (I-123-5-I-R91150), has been developed and has been shown to be suitable for single-photon emission tomography (SPET) imaging. In this study the influence of age and gender on the ligand binding was investigated in normal volunteers. One hundred and fifty MBq of I-123-5-I-R91150 was administered to 26 normal volunteers (13 females and 13 males) with an age range of 23-60 years. SPET imaging was performed with a triple-headed gamma camera. For semi-quantitative analysis, ratios of ligand binding in different regions of interest to the binding in the cerebellum were calculated. Mean ratios of 1.7 were obtained. No gender difference was demonstrated. 5-HT2A binding was shown to decline with age. Over an age range of 40 years a reduction in ligand binding of 42%+/-7% was found. These results are in agreement with in vitro and positron emission tomography findings of a decline in 5-HT2A receptor binding with age. The findings confirm the suitability of I-123-5-I-R91150 for SPET imaging of 5-HT2A receptors, and highlight the necessity for age-matched controls in clinical studies.},
  author       = {Baeken, Chris and D'Haenen, Hugo and Mertens, John and Terriere, Dirk and Chavatte, Kris and Boumon, Rony and Bossuyt, Axel},
  issn         = {0340-6997},
  journal      = {EUROPEAN JOURNAL OF NUCLEAR MEDICINE},
  keywords     = {new tracer,5-HT2A receptors,I-123-5-I-R91150,single-photon emission tomography,HUMAN BRAIN POSTMORTEM,ALZHEIMERS-DISEASE,AUTORADIOGRAPHIC ANALYSIS,H-3 KETANSERIN,SEROTONIN,BINDING,DEPRESSION,DEMENTIA,SUICIDE,CORTEX},
  language     = {eng},
  number       = {12},
  pages        = {1617--1622},
  title        = {123I-5-I-R91150, a new-single-photon emission tomography ligand for 5-HT2A receptors: influence of age and gender in healthy subjects},
  url          = {http://dx.doi.org/10.1007/s002590050339},
  volume       = {25},
  year         = {1998},
}

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