鉴定N-[(5-{[(4-甲基苯基)磺酰基]氨基}-3-(三氟乙酰基)-1H-吲哚-1-基)乙酰基]-L-亮氨酸（NTRC-824），一种对神经降压素2型受体具有选择性的神经降压素样非肽化合物。

Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.

作者信息

Thomas James B, Giddings Angela M, Wiethe Robert W, Olepu Srinivas, Warner Keith R, Sarret Philippe, Gendron Louis, Longpre Jean-Michel, Zhang Yanan, Runyon Scott P, Gilmour Brian P

机构信息

Center for Organic and Medicinal Chemistry, Research Triangle Institute , P.O. Box 12194, 3040 Cornwallis Road, Research Triangle Park, North Carolina 27709, United States.

出版信息

J Med Chem. 2014 Sep 11;57(17):7472-7. doi: 10.1021/jm500857r. Epub 2014 Aug 26.

DOI:10.1021/jm500857r

PMID:25157640

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4161155/

Abstract

Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay.

摘要

已知通过神经降压素2型受体（NTS2）起作用的化合物在急慢性疼痛的动物模型中具有活性。为了鉴定新型NTS2选择性镇痛药，我们使用荧光成像板读数器（FLIPR）检测法寻找NTS2选择性非肽化合物，并鉴定出标题化合物（NTRC - 824，5），据我们所知，它是第一个对NTS2比对NTS1具有选择性的非肽，并且在功能检测中表现得像内源性配体神经降压素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7df6/4161155/e0a7e185615c/jm-2014-00857r_0002.jpg

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鉴定N-[(5-{[(4-甲基苯基)磺酰基]氨基}-3-(三氟乙酰基)-1H-吲哚-1-基)乙酰基]-L-亮氨酸（NTRC-824），一种对神经降压素2型受体具有选择性的神经降压素样非肽化合物。

Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.

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鉴定N-[(5-{[(4-甲基苯基)磺酰基]氨基}-3-(三氟乙酰基)-1H-吲哚-1-基)乙酰基]-L-亮氨酸（NTRC-824），一种对神经降压素2型受体具有选择性的神经降压素样非肽化合物。

Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.

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