Takayanagi I, Nakazo K, Kizawa Y
Jpn J Pharmacol. 1980 Oct;30(5):647-54. doi: 10.1254/jjp.30.647.
A newly synthesized compound, BTM-1042 (cis-(--)-2,3-dihydro-3-(4-methyl-piperazinyl)methyl-2-phenyl-1,5-benzothiazepin-4(5H)-one dihydrochloride) depressed the twitch responses of the ileum from guinea pig to electrical stimulation at 0.1 Hz. This inhibitory action of BTM-1042 was not influenced by naloxone, a narcotic antagonist. BTM-1042 proved to be almost as active as atropine on electrically stimulated ileum. BTM-1042 also blocked muscarinic receptors but the potency was about 1/3 of that of atropine. The responses of the ileum of guinea pig to nicotine and 5-hydroxytryptamine also were inhibited by BTM-1042. However, BTM-1042 did not influence the release of transmitters from motor, sympathetic, nonadrenergic inhibitory (or purinergic nerve), noncholinergic excitatory nerves and responses of various smooth muscles mediated through drug receptors, except for the acetylcholine receptor. Spontaneous movement of the unanaesthetized rabbit stomach was dose dependently depressed by BTM-1042 (0.04--0.2 mg/kg, i.v.). The potency ratio for BTM-1042 relative to atropine was 7.4. BTM-1042 is apparently a new type of potent, antispasmodic drug.
一种新合成的化合物BTM - 1042（顺式 - （ - ） - 2,3 - 二氢 - 3 - （4 - 甲基 - 哌嗪基）甲基 - 2 - 苯基 - 1,5 - 苯并硫氮杂䓬 - 4（5H） - 酮二盐酸盐）可抑制豚鼠回肠对0.1Hz电刺激的抽搐反应。BTM - 1042的这种抑制作用不受麻醉拮抗剂纳洛酮的影响。事实证明，BTM - 1042对电刺激回肠的作用几乎与阿托品一样有效。BTM - 1042也能阻断毒蕈碱受体，但其效力约为阿托品的1/3。BTM - 1042还抑制了豚鼠回肠对尼古丁和5 - 羟色胺的反应。然而，BTM - 1042除了对乙酰胆碱受体外，并不影响运动神经、交感神经、非肾上腺素能抑制（或嘌呤能神经）、非胆碱能兴奋性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。未麻醉家兔胃的自发运动受到BTM - 1042（0.04 - 0.2mg/kg，静脉注射）剂量依赖性的抑制。BTM - 1042相对于阿托品的效价比为7.4。BTM - 1042显然是一种新型的强效解痉药物。
