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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.

Abstract
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.
AuthorsY Iwabuchi, T Masuhara
JournalGeneral pharmacology (Gen Pharmacol) Vol. 25 Issue 1 Pg. 123-9 (Jan 1994) ISSN: 0306-3623 [Print] England
PMID7517901 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Adrenergic Antagonists
  • Cholinergic Antagonists
  • Quinuclidines
  • Receptors, Muscarinic
  • Thiophenes
  • Pilocarpine
  • (4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride
  • cevimeline
Topics
  • (4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride (pharmacology)
  • Adrenergic Antagonists
  • Animals
  • Cholinergic Antagonists
  • Male
  • Pilocarpine (pharmacology)
  • Quinuclidines (pharmacology)
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Muscarinic (classification, drug effects, physiology)
  • Salivary Glands (drug effects, metabolism)
  • Salivation (drug effects)
  • Sjogren's Syndrome (drug therapy, physiopathology)
  • Thiophenes

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