Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2

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

Standard

Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2. / Ulven, Trond; Gallen, Michael J; Nielsen, Mads C; Merten, Nicole; Schmidt, Carola; Mohr, Klaus; Tränkle, Christian; Kostenis, Evi.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 17, No. 21, 01.11.2007, p. 5924-5927.

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

Harvard

Ulven, T, Gallen, MJ, Nielsen, MC, Merten, N, Schmidt, C, Mohr, K, Tränkle, C & Kostenis, E 2007, 'Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2', Bioorganic & Medicinal Chemistry Letters, vol. 17, no. 21, pp. 5924-5927. https://doi.org/10.1016/j.bmcl.2007.07.080

APA

Ulven, T., Gallen, M. J., Nielsen, M. C., Merten, N., Schmidt, C., Mohr, K., Tränkle, C., & Kostenis, E. (2007). Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2. Bioorganic & Medicinal Chemistry Letters, 17(21), 5924-5927. https://doi.org/10.1016/j.bmcl.2007.07.080

Vancouver

Ulven T, Gallen MJ, Nielsen MC, Merten N, Schmidt C, Mohr K et al. Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2. Bioorganic & Medicinal Chemistry Letters. 2007 Nov 1;17(21):5924-5927. https://doi.org/10.1016/j.bmcl.2007.07.080

Author

Ulven, Trond ; Gallen, Michael J ; Nielsen, Mads C ; Merten, Nicole ; Schmidt, Carola ; Mohr, Klaus ; Tränkle, Christian ; Kostenis, Evi. / Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2. In: Bioorganic & Medicinal Chemistry Letters. 2007 ; Vol. 17, No. 21. pp. 5924-5927.

Bibtex

@article{9ff171bfb3bf49308ab9bd719892f386,
title = "Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2",
abstract = "Synthesis and preliminary in vitro biological evaluation of a selective high-affinity CRTH2 antagonist is described. The stability of an N-benzyl group facilitated synthesis of the corresponding radioligand by tritiation of a brominated precursor. The compound [(3)H]TRQ11238 represents the first selective CRTH2 antagonist radioligand and exhibited a specific radioactivity of 52 Ci/mmol and a pK(d) of 9.0 Udgivelsesdato: 2007-Nov-1",
keywords = "Drug Evaluation, Preclinical, Indoles, Radioligand Assay, Receptors, Immunologic, Receptors, Prostaglandin, Sulfonamides",
author = "Trond Ulven and Gallen, {Michael J} and Nielsen, {Mads C} and Nicole Merten and Carola Schmidt and Klaus Mohr and Christian Tr{\"a}nkle and Evi Kostenis",
year = "2007",
month = nov,
day = "1",
doi = "10.1016/j.bmcl.2007.07.080",
language = "English",
volume = "17",
pages = "5924--5927",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "21",

}

RIS

TY - JOUR

T1 - Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2

AU - Ulven, Trond

AU - Gallen, Michael J

AU - Nielsen, Mads C

AU - Merten, Nicole

AU - Schmidt, Carola

AU - Mohr, Klaus

AU - Tränkle, Christian

AU - Kostenis, Evi

PY - 2007/11/1

Y1 - 2007/11/1

N2 - Synthesis and preliminary in vitro biological evaluation of a selective high-affinity CRTH2 antagonist is described. The stability of an N-benzyl group facilitated synthesis of the corresponding radioligand by tritiation of a brominated precursor. The compound [(3)H]TRQ11238 represents the first selective CRTH2 antagonist radioligand and exhibited a specific radioactivity of 52 Ci/mmol and a pK(d) of 9.0 Udgivelsesdato: 2007-Nov-1

AB - Synthesis and preliminary in vitro biological evaluation of a selective high-affinity CRTH2 antagonist is described. The stability of an N-benzyl group facilitated synthesis of the corresponding radioligand by tritiation of a brominated precursor. The compound [(3)H]TRQ11238 represents the first selective CRTH2 antagonist radioligand and exhibited a specific radioactivity of 52 Ci/mmol and a pK(d) of 9.0 Udgivelsesdato: 2007-Nov-1

KW - Drug Evaluation, Preclinical

KW - Indoles

KW - Radioligand Assay

KW - Receptors, Immunologic

KW - Receptors, Prostaglandin

KW - Sulfonamides

U2 - 10.1016/j.bmcl.2007.07.080

DO - 10.1016/j.bmcl.2007.07.080

M3 - Journal article

VL - 17

SP - 5924

EP - 5927

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 21

ER -

ID: 189158552