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[Pharmacological studies on basic ethers (R111 and R97) with antispasmodic activity]

H Matsuda, T Kato, Y Yamamoto

    Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
    |May 1, 1976
    PubMed
    Summary

    This study investigated the pharmacological effects of R111 and R97, finding they possess strong cholinergic blocking and antispasmodic properties. These compounds demonstrated analgesic effects and protected against certain ulcers, with no significant central nervous system impact.

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    Area of Science:

    • Pharmacology
    • Medicinal Chemistry

    Background:

    • Novel ether methyl bromide (R111) and iodide (R97) compounds were synthesized.
    • Their pharmacological profiles and acute toxicity required thorough investigation.

    Purpose of the Study:

    • To evaluate the analgesic, antispasmodic, and other pharmacological properties of R111 and R97.
    • To assess the acute toxicity and central nervous system effects of these novel compounds.

    Main Methods:

    • Analgesic activity was tested using acetic acid-induced writhing and heat-induced pain models in mice.
    • Antispasmodic effects were examined against various spasmogens (acetylcholine, barium chloride, nicotine, histamine, serotonin).
    • Other effects studied included local anesthesia, mydriasis, gastrointestinal and secretory functions, ulcer protection, cardiovascular parameters, and anti-edema activity.

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    Main Results:

    • R111 and R97 showed significant analgesic effects against acetic acid-induced writhing but not heat-induced pain.
    • Both compounds exhibited potent antispasmodic activity, particularly against barium chloride-induced spasms, outperforming papaverine.
    • They displayed protective effects against Shay's ulcers, inhibited intestinal motility and salivation, and reduced carrageenan-induced edema, with minimal cardiovascular or CNS effects.

    Conclusions:

    • R111 and R97 possess significant cholinergic blocking and muscotropic antispasmodic effects.
    • These compounds demonstrate potential therapeutic applications in conditions involving smooth muscle spasms and certain types of ulcers.
    • The lack of significant central nervous system activity suggests a favorable safety profile for peripheral actions.