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Cis-2-methylspiro hydrochloride, hemihydrate induces saliva and tear secretions in rats and mice The role of muscarinic acetylcholine receptors


, : Cis-2-methylspiro hydrochloride, hemihydrate induces saliva and tear secretions in rats and mice The role of muscarinic acetylcholine receptors. Japanese Journal of Pharmacology 78(3): 373-380, Nov

We investigated effects of (+-)-cis-2-methylspiro(1,3-oxathiolane-5,3-quinuclidine) hydrochloride, 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 Sjogren'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 muM. 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 Sjogren's syndrome and X-ray exposure in the head and neck.

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