Long-lasting salivation induced by a novel muscarinic receptor agonist SNI-2011 in rats and dogs.
Long-lasting salivation induced by a novel muscarinic receptor agonist SNI-2011 in rats and dogs.
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新型毒蕈碱受体激动剂 SNI-2011 在大鼠和狗体内诱导持久流涎。
DOI：
10.1016/s0014-2999(97)01338-1
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发表时间：
1997
影响因子：
5
通讯作者：
Y. Takeshita
中科院分区：
文献类型：
--
作者：
H. Masunaga;H. Ogawa;Y. Uematsu;T. Tomizuka;H. Yasuda;Y. Takeshita
将新型毒蕈碱受体激动剂SNI-2011（（±）-顺式-2-甲基斯皮洛[1，3-氧硫杂环戊烷-5，3 '-奎宁环]盐酸盐半水合物）的促唾液分泌作用与盐酸毛果芸香碱在两种毒蕈碱受体激动剂在引发唾液分泌方面表现出大致相似功效的剂量范围内进行了比较。毛果芸香碱（0.66-2.0 mg/kg，i.d.）在大鼠中诱导显著但短暂的流涎，而由SNI-2011（20-60 mg/kg，i.d.）持续了1.4到1.8倍。在狗中，SNI-2011（1-3 mg/kg，i. v.）持续时间也比毛果芸香碱（0.1- 0.3mg/kg，i. v.）长约2倍。以0.4 ml/min速率引起流涎的血浆SNI-2011水平约为100 ng/ml，1 mg/kg SNI-2011诱导的更高流涎速率（超过0.4 ml/min）在犬中持续约90 min。以0.4ml/min的速率引起流涎的血浆毛果芸香碱浓度约为25 ng/ml，0.1mg/kg毛果芸香碱引起的较高流涎速率（超过0.4ml/min）仅持续20 min。SNI-2011的有效血浆水平持续时间长于毛果芸香碱。这些结果表明，SNI-2011可能是有用的，因为其持久的催涎作用在口干症的治疗。
The sialogogic effect of SNI-2011, a novel muscarinic receptor agonist, (±)-cis-2-methylspilo [1,3-oxathiolane-5,3′-quinuclidine] hydrochloride, hemihydrate, was compared with that of pilocarpine hydrochloride in a dose range in which the two muscarinic agonists exhibited approximately similar efficacy in eliciting salivation. Pilocarpine (0.66–2.0 mg/kg, i.d.) induced a marked but short-lasting salivation in rats, whereas the salivation induced by SNI-2011 (20–60 mg/kg, i.d.) lasted 1.4- to 1.8-fold longer. In dogs, the sialogogic effect of SNI-2011(1-3 mg/kg, i.v.) also lasted about 2-fold longer than that of pilocarpine (0.1–0.3 mg/kg, i.v.). The plasma SNI-2011 level that caused salivation at a rate of 0.4 ml/min was about 100 ng/ml and higher rates of salivation (over 0.4 ml/min) induced by 1 mg/kg SNI-2011 lasted for about 90 min in dogs. The plasma pilocarpine level that caused salivation at a rate of 0.4 ml/min was about 25 ng/ml and the higher rate of salivation (over 0.4 ml/min) induced by 0.1 mg/kg pilocarpine lasted only for 20 min in dogs. Effective plasma levels of SNI-2011 persisted longer than those of pilocarpine. These results indicate that SNI-2011 may be useful in the treatment of xerostomia because of its long-lasting sialogogic action.
DOI：
10.1248/bpb1978.4.879
发表时间：
1981-01-01
期刊：
JOURNAL OF PHARMACOBIO-DYNAMICS
影响因子：
--
作者：
YAMAOKA, K;TANIGAWARA, Y;UNO, T
通讯作者：
UNO, T