1. 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.