Takayanagi I, Sone H, Kawashima K, Sohji Y, Kadokawa T
Jpn J Pharmacol. 1982 Dec;32(6):973-9. doi: 10.1254/jjp.32.973.
A newly synthesized drug, SX-284, depressed the twitch response of the ileum from guinea pig to electrical stimulation at 0.1 Hz. SX-284 proved to be almost as active as atropine on electrically stimulated ileum. The responses of guinea pig ileum to nicotine and serotonin were also inhibited by SX-284. However, SX-284 did not influence the release of transmitters from the motor, sympathetic, nonadrenergic inhibitory, noncholinergic excitatory nerves, and responses of various smooth muscles mediated through drug receptors, and at these doses, SX-284 inhibited the release of acetylcholine from the vagus nerve. These facts indicate that SX-284 specifically inhibits the acetylcholine release from the vagus nerve. Furthermore, spontaneous movement of the guinea pig ileum was dose-dependently depressed by SX-284. The potency ratio for SX-284 relative to atropine was 1.7.
一种新合成的药物SX - 284可抑制豚鼠回肠对0.1赫兹电刺激的抽搐反应。事实证明，SX - 284对电刺激回肠的作用几乎与阿托品一样有效。SX - 284也能抑制豚鼠回肠对尼古丁和血清素的反应。然而，SX - 284并不影响运动神经、交感神经、非肾上腺素能抑制神经、非胆碱能兴奋神经递质的释放，以及通过药物受体介导的各种平滑肌反应，在这些剂量下，SX - 284可抑制迷走神经乙酰胆碱的释放。这些事实表明，SX - 284能特异性抑制迷走神经乙酰胆碱的释放。此外，SX - 284可剂量依赖性地抑制豚鼠回肠的自发运动。SX - 284相对于阿托品的效价比为1.7。
