基于天然产物康奈辛的一类新型H3受体拮抗剂。
A new family of H3 receptor antagonists based on the natural product Conessine.
作者信息
Santora Vincent J, Covel Jonathan A, Hayashi Rena, Hofilena Brian J, Ibarra Jason B, Pulley Michelle D, Weinhouse Michael I, Sengupta Dipanjan, Duffield Jonathan J, Semple Graeme, Webb Robert R, Sage Carleton, Ren Albert, Pereira Guilherme, Knudsen Jens, Edwards Jeffrey E, Suarez Marissa, Frazer John, Thomsen William, Hauser Erin, Whelan Kevin, Grottick Andrew J
机构信息
Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2008 Feb 15;18(4):1490-4. doi: 10.1016/j.bmcl.2007.12.059. Epub 2007 Dec 25.
A new family of Histamine H(3) receptor antagonists (5a-t) has been prepared based on the structure of the natural product Conessine, a known H(3) antagonist. Several members of the new series are highly potent and selective binders of rat and human H(3) receptors and display inverse agonism at the human H(3) receptor. Compound 5n exhibited promising rat pharmacokinetic properties and demonstrated functional antagonism of the H(3) receptor in an in-vivo pharmacological model.
基于天然产物康奈辛（一种已知的H(3)拮抗剂）的结构，已制备出一类新的组胺H(3)受体拮抗剂（5a - t）。新系列中的几个成员是大鼠和人类H(3)受体的高效和选择性结合剂，并在人类H(3)受体上表现出反向激动作用。化合物5n表现出良好的大鼠药代动力学特性，并在体内药理学模型中证明了对H(3)受体的功能性拮抗作用。
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