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

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

SN - 0960-894X

VL - 17

SP - 5924

EP - 5927

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 21

ER -