| Literature DB >> 30728111 |
Hiroyuki Tobinaga1, Takayuki Kameyama2, Kentarou Asahi3, Tohru Horiguchi3, Miho Oohara3, Yukio Tada3, Kouki Fuchino3, Sae Jikihara4, Takeshi Endoh5, Naoko Kurihara6, Yasuhiko Kanda3, Masayoshi Ogawa3, Naomi Tamura7, Shigenori Yagi8, Emiko Taniguchi6, Yukio Takahara6, Shinji Shimada9, Chie Takeyama9, Shoichi Yamamoto10, Shunji Shinohara9, Hiroyuki Kai11.
Abstract
Some P2X3 receptor antagonists have been developed as new therapeutic drugs for pain. We discovered a novel chemotype of P2X3 receptor antagonists with a pyrrolinone skeleton. Because of SAR studies to improve bioavailability of lead compound 2, compound (R)-24 was identified, which showed an analgesic effect against neuropathic pain by oral administration. We constructed a human P2X3 homology model as a template for the zebrafish P2X4 receptor, which agreed with SAR studies of pyrrolinone derivatives.Entities:
Keywords: Ion channels; P2X3 receptor antagonists; Pain; Purinergic receptors; Pyrrolinone derivatives
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Year: 2019 PMID： 30728111 DOI： 10.1016/j.bmcl.2019.01.039
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823