Long-lasting salivation induced by a novel muscarinic receptor agonist SNI-2011 in rats and dogs

European Journal of Pharmacology
H MasunagaY Takeshita

Abstract

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...Continue Reading

References

Mar 13, 1990·European Journal of Pharmacology·A LaniyonuN Fleming
Dec 1, 1989·Journal of Surgical Oncology·D E SchullerM Martin
Jul 1, 1987·Archives of Internal Medicine·L M Sreebny, A Valdini
Mar 1, 1986·Oral Surgery, Oral Medicine, and Oral Pathology·P C FoxI D Mandel
Mar 15, 1987·Cancer·D Greenspan, T E Daniels
Dec 1, 1980·British Journal of Pharmacology·D A BrownR D White
Nov 1, 1981·Journal of Pharmacobio-dynamics·K YamaokaT Uno

❮ Previous
Next ❯

Citations

Feb 22, 2005·Pharmacology·Kimihiro SuzukiFumitaka Ohsuzu
Aug 7, 2008·Drugs·Juliane Weber, Gillian M Keating
Jan 10, 2001·Journal of the American Veterinary Medical Association·S O CanappD P O'Brien
Oct 20, 2006·Archives of Oral Biology·Nao SatoKiyotoshi Inenaga
Oct 30, 2001·The Journal of the American Dental Association·I al-Hashimi
Dec 1, 2001·Clinical Immunology : the Official Journal of the Clinical Immunology Society·R I FoxA Fisher
Sep 15, 2007·International Journal of Radiation Oncology, Biology, Physics·Mark S ChambersRobert Haddad
Nov 9, 2017·Expert Opinion on Pharmacotherapy·Candela Rodríguez-PomarGonzalo Carracedo
Aug 20, 2005·Pharmacological Reviews·Noboru Toda, Arnold G Herman
Jun 7, 2006·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·Gota ChoYasuko Ishikawa

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.