Radiolabeling and in vivo evaluation of [11C]AGH-44: a potential lead structure to develop a positron emission tomography radioligand for the 5-HT7 receptor

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Radiolabeling and in vivo evaluation of [11C]AGH-44 : a potential lead structure to develop a positron emission tomography radioligand for the 5-HT7 receptor. / L’Estrade, Elina T.; Petersen, Ida N.; Xiong, Mengfei; Hogendorf, Adam S.; Hogendorf, Agata; Kristensen, Jesper L.; Kjær, Andreas; Bojarski, Andrzej J.; Erlandsson, Maria; Ohlsson, Tomas; Knudsen, Gitte M.; Herth, Matthias M.

In: Journal of Radioanalytical and Nuclear Chemistry, Vol. 322, No. 2, 01.11.2019, p. 847-851.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

L’Estrade, ET, Petersen, IN, Xiong, M, Hogendorf, AS, Hogendorf, A, Kristensen, JL, Kjær, A, Bojarski, AJ, Erlandsson, M, Ohlsson, T, Knudsen, GM & Herth, MM 2019, 'Radiolabeling and in vivo evaluation of [11C]AGH-44: a potential lead structure to develop a positron emission tomography radioligand for the 5-HT7 receptor', Journal of Radioanalytical and Nuclear Chemistry, vol. 322, no. 2, pp. 847-851. https://doi.org/10.1007/s10967-019-06687-3

APA

L’Estrade, E. T., Petersen, I. N., Xiong, M., Hogendorf, A. S., Hogendorf, A., Kristensen, J. L., Kjær, A., Bojarski, A. J., Erlandsson, M., Ohlsson, T., Knudsen, G. M., & Herth, M. M. (2019). Radiolabeling and in vivo evaluation of [11C]AGH-44: a potential lead structure to develop a positron emission tomography radioligand for the 5-HT7 receptor. Journal of Radioanalytical and Nuclear Chemistry, 322(2), 847-851. https://doi.org/10.1007/s10967-019-06687-3

Vancouver

L’Estrade ET, Petersen IN, Xiong M, Hogendorf AS, Hogendorf A, Kristensen JL et al. Radiolabeling and in vivo evaluation of [11C]AGH-44: a potential lead structure to develop a positron emission tomography radioligand for the 5-HT7 receptor. Journal of Radioanalytical and Nuclear Chemistry. 2019 Nov 1;322(2):847-851. https://doi.org/10.1007/s10967-019-06687-3

Author

L’Estrade, Elina T. ; Petersen, Ida N. ; Xiong, Mengfei ; Hogendorf, Adam S. ; Hogendorf, Agata ; Kristensen, Jesper L. ; Kjær, Andreas ; Bojarski, Andrzej J. ; Erlandsson, Maria ; Ohlsson, Tomas ; Knudsen, Gitte M. ; Herth, Matthias M. / Radiolabeling and in vivo evaluation of [11C]AGH-44 : a potential lead structure to develop a positron emission tomography radioligand for the 5-HT7 receptor. In: Journal of Radioanalytical and Nuclear Chemistry. 2019 ; Vol. 322, No. 2. pp. 847-851.

Bibtex

@article{889796bb9f654f0199f3e038832b93a9,
title = "Radiolabeling and in vivo evaluation of [11C]AGH-44: a potential lead structure to develop a positron emission tomography radioligand for the 5-HT7 receptor",
abstract = "AGH-44 is described as a selective low-basicity serotonin 7 receptor (5-HT7R) agonist. In this paper, we evaluate if AGH-44 can act as a lead structure to develop a 5-HT7R selective positron emission tomography (PET) tracer. 11C-labeling of AGH-44 succeeded in a two-step, one-pot procedure in good yields. Subsequent PET studies showed that [11C]AGH-44 displays low blood–brain-barrier passage in Long–Evans rats. Moreover, [11C]AGH-44 brain accumulation showed to be independent on permeability glycoprotein (P-gp) efflux inhibition. Results from biodistribution and metabolism studies could neither explain the observed low brain uptake. As such, we believe that this scaffold is not an optimal starting point to develop a 5-HT7R selective PET tracer.",
keywords = "5-HT, AGH-44, Carbon-11, PET",
author = "L{\textquoteright}Estrade, {Elina T.} and Petersen, {Ida N.} and Mengfei Xiong and Hogendorf, {Adam S.} and Agata Hogendorf and Kristensen, {Jesper L.} and Andreas Kj{\ae}r and Bojarski, {Andrzej J.} and Maria Erlandsson and Tomas Ohlsson and Knudsen, {Gitte M.} and Herth, {Matthias M.}",
year = "2019",
month = nov,
day = "1",
doi = "10.1007/s10967-019-06687-3",
language = "English",
volume = "322",
pages = "847--851",
journal = "Journal of Radioanalytical and Nuclear Chemistry",
issn = "0236-5731",
publisher = "Akad{\'e}miai Kiad{\'o}",
number = "2",

}

RIS

TY - JOUR

T1 - Radiolabeling and in vivo evaluation of [11C]AGH-44

T2 - a potential lead structure to develop a positron emission tomography radioligand for the 5-HT7 receptor

AU - L’Estrade, Elina T.

AU - Petersen, Ida N.

AU - Xiong, Mengfei

AU - Hogendorf, Adam S.

AU - Hogendorf, Agata

AU - Kristensen, Jesper L.

AU - Kjær, Andreas

AU - Bojarski, Andrzej J.

AU - Erlandsson, Maria

AU - Ohlsson, Tomas

AU - Knudsen, Gitte M.

AU - Herth, Matthias M.

PY - 2019/11/1

Y1 - 2019/11/1

N2 - AGH-44 is described as a selective low-basicity serotonin 7 receptor (5-HT7R) agonist. In this paper, we evaluate if AGH-44 can act as a lead structure to develop a 5-HT7R selective positron emission tomography (PET) tracer. 11C-labeling of AGH-44 succeeded in a two-step, one-pot procedure in good yields. Subsequent PET studies showed that [11C]AGH-44 displays low blood–brain-barrier passage in Long–Evans rats. Moreover, [11C]AGH-44 brain accumulation showed to be independent on permeability glycoprotein (P-gp) efflux inhibition. Results from biodistribution and metabolism studies could neither explain the observed low brain uptake. As such, we believe that this scaffold is not an optimal starting point to develop a 5-HT7R selective PET tracer.

AB - AGH-44 is described as a selective low-basicity serotonin 7 receptor (5-HT7R) agonist. In this paper, we evaluate if AGH-44 can act as a lead structure to develop a 5-HT7R selective positron emission tomography (PET) tracer. 11C-labeling of AGH-44 succeeded in a two-step, one-pot procedure in good yields. Subsequent PET studies showed that [11C]AGH-44 displays low blood–brain-barrier passage in Long–Evans rats. Moreover, [11C]AGH-44 brain accumulation showed to be independent on permeability glycoprotein (P-gp) efflux inhibition. Results from biodistribution and metabolism studies could neither explain the observed low brain uptake. As such, we believe that this scaffold is not an optimal starting point to develop a 5-HT7R selective PET tracer.

KW - 5-HT

KW - AGH-44

KW - Carbon-11

KW - PET

U2 - 10.1007/s10967-019-06687-3

DO - 10.1007/s10967-019-06687-3

M3 - Journal article

AN - SCOPUS:85074379944

VL - 322

SP - 847

EP - 851

JO - Journal of Radioanalytical and Nuclear Chemistry

JF - Journal of Radioanalytical and Nuclear Chemistry

SN - 0236-5731

IS - 2

ER -

ID: 231211017