Sialogogic activities of SNI-2011 compared with those of pilocarpine and McN-A-343 in rat salivary glands: identification of a potential therapeutic agent for treatment of Sjörgen's syndrome.
作者信息
Iwabuchi Y, Masuhara T
机构信息
Department of Dental Pharmacology, School of Dentistry at Niigata, Nippon Dental University, Japan.
出版信息
Gen Pharmacol. 1994 Jan;25(1):123-9. doi: 10.1016/0306-3623(94)90021-3.
We examined the sialogogic activities in rat major salivary glands of SNI-2011, in comparison with those of pilocarpine and McN-A-343, and we characterized the subtypes of muscarine receptors that are involved in the sialogogic responses to SNI-2011 and McN-A-343. 2. SNI-2011 at doses ranging from 1 to 10 mg/kg (i.v.) increased the secretion of saliva in a dose-dependent manner. The dose-response curves for SNI-2011 were approximately parallel to curves for pilocarpine but the potency of SNI-2011 was about 25-fold lower than that of pilocarpine. 3. The total volume of saliva secreted in response to McN-A-343 was very much less than that secreted in response to SNI-2011. 4. The salivation induced by SNI-2011 and by McN-A-343 was inhibited by various antagonists with the following rank order of potency: 4-DAMP >> pirenzepine >> AF-DX 116. 5. Our results suggest that the sialogogic effects of SNI-2011 and McN-A-343 are mediated by direct stimulation of M3 receptors in salivary glands and that SNI-2011 may prove useful in the management of xerostomia in patients with Sjögren's syndrome.
摘要
我们研究了SNI - 2011对大鼠主要唾液腺的催涎活性，并与毛果芸香碱和McN - A - 343的催涎活性进行比较，同时我们还对参与SNI - 2011和McN - A - 343催涎反应的毒蕈碱受体亚型进行了表征。2. 静脉注射剂量为1至10 mg/kg的SNI - 2011可剂量依赖性地增加唾液分泌。SNI - 2011的剂量反应曲线与毛果芸香碱的曲线大致平行，但SNI - 2011的效力比毛果芸香碱低约25倍。3. 对McN - A - 343产生反应而分泌的唾液总体积远小于对SNI - 2011产生反应而分泌的唾液体积。4. SNI - 2011和McN - A - 343诱导的唾液分泌受到各种拮抗剂的抑制，其效力顺序如下：4 - DAMP >> 哌仑西平 >> AF - DX 116。5. 我们的结果表明，SNI - 2011和McN - A - 343的催涎作用是通过直接刺激唾液腺中的M3受体介导的，并且SNI - 2011可能被证明对干燥综合征患者口干症的治疗有用。
