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  • Title: Muscarinic agonists as analgesics. Antinociceptive activity versus M1 activity: SAR of alkylthio-TZTP's and related 1,2,5-thiadiazole analogs.
    Author: Sauerberg P, Olesen PH, Sheardown MJ, Suzdak PD, Shannon HE, Bymaster FP, Calligaro DO, Mitch CH, Ward JS, Swedberg MD.
    Journal: Life Sci; 1995; 56(11-12):807-14. PubMed ID: 10188779.
    Abstract:
    Alkylthio-TZTPs (3-(3-alkylthio-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-met hylpyridines) and corresponding azabicyclic analogs were tested for m1 efficacy in cloned human m1 receptors and for antinociceptive activity in the mouse grid shock assay. The m1 (%PI) SAR were distinctly different from the analgesia and the salivation SAR, suggesting that analgesia is mediated by neither m1 nor M3 muscarinic receptors.
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