(.+-.)-cis-2-Methylspiro (1,3-oxathiolane-5,3'-quinuclidine) Hydrochloride, Hemihydrate (SNI-2011, Cevimeline Hydrochloride) Induces Saliva and Tear Secretions in Rats and Mice: The Role of Muscarinic Acetylcholine Receptors.
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- Iga Yoshinori
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
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- Arisawa Hirohiko
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
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- Ogane Nobuo
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
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- Saito Yasunari
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
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- Tomizuka Toshie
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
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- Nakagawa-Yagi Yuzo
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
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- Masunaga Hiroaki
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
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- Yasuda Hiroshi
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
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- Miyata Nobuo
- Research Institute of Life Science, Snow Brand Milk Products Co., Ltd.
Bibliographic Information
- Other Title
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- (±)-cis-2-Methylspiro[1,3-oxathiolane-5,3′-quinuclidine] Hydrochloride, Hemihydrate(SNI-2011, Cevimeline Hydrochloride) Induces Saliva and Tear Secretions in Rats and Mice:The Role of Muscarinic Acetylcholine Receptors
- プラスマイナス cis 2 Methylspiro 1 3 oxathiola
- (±)-cis-2-Methylspiro[1,3-oxathiolane-5,3-quinuclidine] Hydrochloride, Hemihydrate (SNI-2011, Cevimeline Hydrochloride) Induces Saliva and Tear Secretions in Rats and Mice: The Role of Muscarinic Acetylcholine Receptors
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Abstract
We investigated effects of (±)-cis-2-methylspiro[1, 3-oxathiolane-5, 3′-quinuclidine] hydrochlo- ride, hemihydrate (SNI-2011, cevimeline hydrochloride), a rigid analogue of acetylcholine, on saliva and tear secretions in rats and mice to evaluate its therapeutical efficacy for xerostomia and xerophthalmia in patients with Sjögren’s syndrome and X-ray exposure in the head and neck. Intraduodenal administrations of SNI-2011 increased saliva secretion in a dose-dependent manner at doses ranging from 3 to 30 mg/kg in normal rats and mice, two strains of autoimmune disease mice and X-irradiated saliva secretion defective rats. The salivation elicited by SNI-2011 was completely inhibited by atropine. A similar atropine-sensitive response was observed in tear secretion. In rat submandibular/sublingual gland membranes, [3H]quinuclidinyl benzilate (QNB) binding was saturable, and Scatchard plot analysis revealed a single population of binding sites with a Kd of 22 pM and a maximal binding capacity of 60 fmol/mg protein. The competitive inhibition curve of the [3H]QNB binding by SNI-2011 was obtained, and its dissociation constant value calculated from IC50 was 1 - 2 μM. These results suggest that SNI-2011 increases saliva and tear secretions through a direct stimulation to muscarinic receptors in salivary and lacrimal glands, and they suggest that SNI-2011 should be beneficial to patients with Sjögren’s syndrome and X-ray exposure in the head and neck.
Journal
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- The Japanese Journal of Pharmacology
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The Japanese Journal of Pharmacology 78 (3), 373-380, 1998
The Japanese Pharmacological Society
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Details 詳細情報について
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- CRID
- 1390001204286086144
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- NII Article ID
- 10008681425
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- NII Book ID
- AA00691188
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- COI
- 1:CAS:528:DyaK1cXnslyktbw%3D
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- ISSN
- 13473506
- 00215198
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- NDL BIB ID
- 4610827
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- PubMed
- 9869272
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- Web Site
- https://ndlsearch.ndl.go.jp/books/R000000004-I4610827
- https://api.elsevier.com/content/article/PII:S0021519819310376?httpAccept=text/xml
- https://api.elsevier.com/content/article/PII:S0021519819310376?httpAccept=text/plain
- https://www.jstage.jst.go.jp/article/jjp/78/3/78_3_373/_pdf
- https://search.jamas.or.jp/link/ui/1999089001
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed