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  • Title: Demonstration of the partial agonist profiles of Ro 16-6028 and Ro 17-1812 in mice in vivo.
    Author: Potier MC, Prado de Carvalho L, Venault P, Chapouthier G, Rossier J.
    Journal: Eur J Pharmacol; 1988 Oct 26; 156(1):169-72. PubMed ID: 2850207.
    Abstract:
    Benzodiazepine receptor occupancy by the full agonist, diazepam, and by the two putative partial agonists, Ro 16-6028 and Ro 17-1812, was measured by inhibition of in vivo [3H]Ro 15-1788 binding in mouse brain and was correlated with their pharmacological effects. The anticonvulsant effects of Ro 16-6028, Ro 17-1812 and diazepam (ED50 values) appeared at receptor occupancies of 40, 20 and less than 5%, respectively. Moreover, at the highest measurable receptor occupancy (90-100%), Ro 16-6028 and Ro 17-1812 did not induce any rotarod deficit whereas a complete deficit was observed with diazepam at 35% receptor occupancy.
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