Development of 2, 4-diaminopyrimidine derivatives as novel SNSR4 antagonists

M Bayrakdarian, J Butterworth, YJ Hu…

Index: Bayrakdarian, Malken; Butterworth, Joanne; Hu, Yun-Jin; Santhakumar, Vijayaratnam; Tomaszewski, Miroslaw J. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 2102 - 2105

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Citation Number: 8

Abstract

Human sensory neuron specific receptor 4 (SNSR4 or MrgX1) is restricted to a subpopulation of sensory neurons in both humans and rat. These neurons are known to express other nociceptive markers such as IB4 and SNSR4 agonists such as BAM 8-22 are pro-nociceptive in rodents. SNSR4 activation might have a pro-nociceptive role in pain, and an antagonist may, therefore, have therapeutic value as an analgesic. 4a There is also a contradictory ...