Nagai H, Matsuura N, Sato N, Koda A, Kohno S
J Pharmacobiodyn. 1983 Nov;6(11):874-80. doi: 10.1248/bpb1978.6.874.
The antagonistic effect of 2,4'-dimethyl-3-piperidino propiophenone hydrochloride (Mydocalm) and its 15 derivatives against the activity of slow reacting substance of anaphylaxis (SRS-A) were examined in vitro. Mydocalm, 2-methyl-3-piperidino-beta-propionaphthone hydrochloride (As-5) and 2,3',4'-trimethyl-3 piperidinopropiophenone hydrochloride (As-14) were found to be potent antagonists to SRS-A. The above three compounds inhibited homologous passive cutaneous anaphylaxis (PCA) in rats and guinea pigs but not heterologous PCA in guinea pigs. As-5 inhibited the release of histamine from and the degranulation of rat mesenterium mast cells. As-14 also showed the inhibition of the degranulation. Mydocalm, however, showed no inhibition of these reactions. Experimental asthma in guinea pigs which were passively sensitized with guinea pig immunoglobulin E antibody was significantly inhibited by p.o. administration of Mydocalm, As-5 or As-14 respectively.
在体外研究了盐酸2,4'-二甲基-3-哌啶基苯丙酮（美多卡胺）及其15种衍生物对过敏反应慢反应物质（SRS-A）活性的拮抗作用。发现美多卡胺、盐酸2-甲基-3-哌啶基-β-丙酰萘（As-5）和盐酸2,3',4'-三甲基-3-哌啶基苯丙酮（As-14）是SRS-A的有效拮抗剂。上述三种化合物抑制大鼠和豚鼠的同种被动皮肤过敏反应（PCA），但不抑制豚鼠的异种PCA。As-5抑制大鼠肠系膜肥大细胞组胺释放和脱颗粒。As-14也显示出对脱颗粒的抑制作用。然而，美多卡胺对这些反应没有抑制作用。分别口服美多卡胺、As-5或As-14可显著抑制用豚鼠免疫球蛋白E抗体被动致敏的豚鼠的实验性哮喘。
Zotero 插件