Source:http://linkedlifedata.com/resource/pubmed/id/11963642
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rdf:type | |
lifeskim:mentions |
umls-concept:C0007226,
umls-concept:C0009452,
umls-concept:C0013227,
umls-concept:C0034826,
umls-concept:C0039082,
umls-concept:C0043352,
umls-concept:C0205246,
umls-concept:C0205314,
umls-concept:C0205437,
umls-concept:C0205464,
umls-concept:C0243192,
umls-concept:C0245634,
umls-concept:C0521346,
umls-concept:C0679622,
umls-concept:C1280500,
umls-concept:C1979963,
umls-concept:C2003903
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pubmed:issue |
3
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pubmed:dateCreated |
2002-4-19
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pubmed:abstractText |
A novel muscarinic receptor agonist, SNI-2011 ((+/-)-cis-2-methylspiro[1,3-oxathiolane- 5,3'-quinuclidine]monohydrochloride hemihydrate, cevimeline, CAS 153504-70-2), is a candidate therapeutic drug for xerostomia in Sjögren's syndrome. The general pharmacological properties of this drug on the respiratory and cardiovascular systems were investigated in guinea pigs and dogs. SNI-2011 reduced the contractile force and beating rate of isolated right guinea pig atrium at 1 x 10(-6) mol/l or higher and 3 x 10(-6) mol/l or higher, respectively. SNI-2011 reduced the contractile force of isolated left atrium induced by electric stimulation at 1 x 10(-6) mol/l or higher. In anesthetized dogs, SNI-2011 caused a transient decrease in blood pressure, tachycardia and an increase in femoral arterial blood flow at 0.01 mg/kg i.v. or higher. At 1 mg/kg it caused continuous bradycardia, a decrease in femoral arterial blood flow and an increase in respiration rate in addition to the changes observed immediately after injection. A transient negative T-wave was observed as the only change in the ECG immediately after injection at 1 mg/kg. However, when SNI-2011 was injected intraduodenally, a decrease in femoral arterial blood flow, bradycardia and a tendency to increase respiration rate were observed at doses of 1 to 3 mg/kg. All these events in dogs were antagonized by atropine. These results suggest that oral administration of SNI-2011, that is the clinical administration route, can distinctly reduce the muscarinic effects on the respiratory and cardiovascular systems compared to intravenous administration.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Atropine,
http://linkedlifedata.com/resource/pubmed/chemical/Muscarinic Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Muscarinic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Quinuclidines,
http://linkedlifedata.com/resource/pubmed/chemical/Thiophenes,
http://linkedlifedata.com/resource/pubmed/chemical/cevimeline
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pubmed:status |
MEDLINE
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pubmed:issn |
0004-4172
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
162-7
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:11963642-Animals,
pubmed-meshheading:11963642-Atropine,
pubmed-meshheading:11963642-Dogs,
pubmed-meshheading:11963642-Electrocardiography,
pubmed-meshheading:11963642-Guinea Pigs,
pubmed-meshheading:11963642-Heart Atria,
pubmed-meshheading:11963642-Hemodynamics,
pubmed-meshheading:11963642-Male,
pubmed-meshheading:11963642-Muscarinic Agonists,
pubmed-meshheading:11963642-Muscarinic Antagonists,
pubmed-meshheading:11963642-Myocardial Contraction,
pubmed-meshheading:11963642-Quinuclidines,
pubmed-meshheading:11963642-Regional Blood Flow,
pubmed-meshheading:11963642-Respiratory Mechanics,
pubmed-meshheading:11963642-Sjogren's Syndrome,
pubmed-meshheading:11963642-Thiophenes,
pubmed-meshheading:11963642-Xerostomia
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pubmed:year |
2002
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pubmed:articleTitle |
General pharmacological profile of the novel muscarinic receptor agonist SNI-2011, a drug for xerostomia in Sjögren's syndrome. 3rd communication: effects on respiratory and cardiovascular systems.
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pubmed:affiliation |
Research Institute of Life Science, Snow Brand Milk Products Co., Ltd., Tochigi, Japan. hm-arisawa@sannet.ne.jp
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pubmed:publicationType |
Journal Article,
In Vitro
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