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

Trond Ulven; Michael J Gallen; Mads C Nielsen; Nicole Merten; Carola Schmidt; Klaus Mohr; Christian Tränkle; Evi Kostenis

doi:10.1016/j.bmcl.2007.07.080

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

Trond Ulven, Michael J Gallen, Mads C Nielsen, Nicole Merten, Carola Schmidt, Klaus Mohr, Christian Tränkle, Evi Kostenis

8 Citations (Scopus)

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

Original language	English
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	17
Issue number	21
Pages (from-to)	5924-5927
Number of pages	4
ISSN	0960-894X
DOIs	https://doi.org/10.1016/j.bmcl.2007.07.080
Publication status	Published - 1 Nov 2007

Keywords

Drug Evaluation, Preclinical
Indoles
Radioligand Assay
Receptors, Immunologic
Receptors, Prostaglandin
Sulfonamides

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10.1016/j.bmcl.2007.07.080

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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 et al.
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

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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",

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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

SN - 0960-894X

VL - 17

SP - 5924

EP - 5927

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 21

ER -

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

Abstract

Keywords

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