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

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),一种选择性作用于 2 型神经降压素受体的神经降压素样非肽化合物

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

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.

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