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  • Title: Phaclofen: a peripheral and central baclofen antagonist.
    Author: Kerr DI, Ong J, Prager RH, Gynther BD, Curtis DR.
    Journal: Brain Res; 1987 Mar 03; 405(1):150-4. PubMed ID: 3032346.
    Abstract:
    Phaclofen, the phosphonic acid derivative of baclofen, reversibly antagonized the depression of the cholinergic twitch response of the guinea pig ileum and distal colon by either baclofen or GABA. When administered microelectrophoretically, phaclofen reversibly blocked the presumed presynaptic reduction by baclofen of the monosynaptic excitation of spinal interneurones by impulses in primary afferent fibres of the cat but did not block the postsynaptic depressant action of baclofen on these neurones. Phaclofen may thus be useful in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact.
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