Snider R M, Constantine J W, Lowe J A, Longo K P, Lebel W S, Woody H A, Drozda S E, Desai M C, Vinick F J, Spencer R W
Department of Exploratory Medicinal Chemistry, Central Research Division, Pfizer Inc., Groton, CT 06340.
Science. 1991 Jan 25;251(4992):435-7. doi: 10.1126/science.1703323.
CP-96,345 [(2S, 3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)- methyl]-1-azabicyclo[2.2.2]octan-3-amine] is a potent nonpeptide antagonist of the substance P (NK1) receptor. CP-96,345 inhibited 3H-labeled substance P binding and was a classical competitive antagonist in the NK1 monoreceptor dog carotid artery preparation. CP-96,345 inhibited substance P-induced salivation in the rat, a classical in vivo bioassay, but did not inhibit NK2, NK3, or numerous other receptors; it is thus a selective NK1 antagonist. This compound may prove to be a powerful tool for investigation of the physiological properties of substance P and exploration of its role in diseases.
CP - 96,345 [（2S，3S）-顺式-2-（二苯基甲基）-N - [（2 - 甲氧基苯基）甲基]-1-氮杂双环[2.2.2]辛烷-3-胺]是一种有效的P物质（NK1）受体非肽拮抗剂。CP - 96,345抑制3H标记的P物质结合，并且在NK1单受体犬颈动脉制备中是经典的竞争性拮抗剂。CP - 96,345在大鼠体内经典生物测定中抑制P物质诱导的唾液分泌，但不抑制NK2、NK3或许多其他受体；因此它是一种选择性NK1拮抗剂。该化合物可能被证明是研究P物质生理特性及其在疾病中作用的有力工具。
